59 results on '"Iqbal, Zeenat"'
Search Results
2. QbD-Assisted Development and Optimization of Doxycycline Hyclate- and Hydroxyapatite-Loaded Nanoparticles for Periodontal Delivery.
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Jain, Pooja, Mirza, Mohd. Aamir, Reyaz, Enam, Beg, Mirza Adil, Selvapandiyan, Angamuthu, Hasan, Nazeer, Naqvi, Akbar, Punnoth Poonkuzhi, Naseef, Kuruniyan, Mohammad Saheer, Yadav, Harlokesh Narayan, Ahmad, Farhan J., and Iqbal, Zeenat
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- 2024
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3. Daidzein from Dietary Supplement to a Drug Candidate: An Evaluation of Potential.
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Ubaid, Mohammed, Salauddin, Shadani, Md Andalib, Kawish, S. M., Albratty, Mohammed, Makeen, Hafiz A., Alhazmi, Hassan A., Najmi, Asim, Zoghebi, Khalid, Halawi, Maryam A., Ali, Abuzer, Alam, Md Shamsher, Iqbal, Zeenat, and Mirza, Mohd. Aamir
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- 2023
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4. Rapid Analytical Method Development and Validation of RP-HPLC Method for the Simultaneous Estimation of Exemestane and Genistein with Specific Application in Lipid-Based Nanoformulations.
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Sharma, Shwetakshi, Gupta, Priya, Gupta, Annie, Kawish, S.M, Iqbal, Zeenat, Vohora, Divya, and Kohli, Kanchan
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- 2023
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5. QbD-Engineered Development and Validation of a RP-HPLC Method for Simultaneous Estimation of Rutin and Ciprofloxacin HCl in Bilosomal Nanoformulation.
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Shamim, Athar, Ansari, Mohammad Javed, Aodah, Alhussain, Iqbal, Muzaffar, Aqil, Mohd., Mirza, Mohd. Aamir, Iqbal, Zeenat, and Ali, Asgar
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- 2023
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6. In Silico Guided Nanoformulation Strategy for Circumvention of Candida albicans Biofilm for Effective Therapy of Candidal Vulvovaginitis.
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Hassan, Nazia, Farooq, Uzma, Das, Ayan Kumar, Sharma, Kalicharan, Mirza, Mohd. Aamir, Fatima, Suhail, Singh, Omana, Ansari, Mohammad Javed, Ali, Asgar, and Iqbal, Zeenat
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- 2023
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7. Exploration of a W/O Nanoemulsion for Antibiofilm Activity against Cariogenic Enterococcus faecalis.
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Singh, Manvi, Rehman, Abdul, Hassan, Nazia, Anfey Faheem, Abdul, Das, Ayan, Rahman, MohammadAkhlaquer, Ansari, Mohammad Javed, Sharma, Nilima, Dudeja, Mridu, Aqil, Mohd, Mirza, Mohd. Aamir, and Iqbal, Zeenat
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- 2023
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8. COVID 19 pandemic challenges and their management: A review of medicines, vaccines, patents and clinical trials with emphasis on psychological health issues.
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Mohapatra, Sradhanjali, Ayash Kumar, P., Farooq, Uzma, Jain, Pooja, Khan, Rahmuddin, Hassan, Nazia, Shamim, Athar, Javed Ansari, Mohammad, Alalaiwe, Ahmed S., Aldawsari, Mohammed F., Aamir Mirza, Mohd, and Iqbal, Zeenat
- Abstract
The SARS‐CoV‐2 (COVID 19) paroxysm is a dominant health exigency that caused significant distress, affecting physical and mental health. Increased mortality, a stressed healthcare system, financial crisis, isolation, and new living and working styles enhanced societal commiseration leading to poor health outcomes. Though people try to maintain good physical health but unfortunately the mental affliction is still ignored. Poor psychological health has emerged as a burgeoning social issue and demands attention. Henceforth, the fundamental objective of this review article is to collate information about COVID-linked physical and psychological agony in diverse population groups with related symptoms and accessible diagnosis techniques. Recent studies have unraveled the fragile mental states of people who have either contracted COVID 19 or had near and dear ones falling prey to it. The impact of the epidemic on the human mind both in short and long-term, with possible risk and preventive factors together with suggested solutions for maintaining good health have also been discussed here. It also enlists the available medications, vaccines and investigational research in the form of patents and clinical trials. This article can be taken as an updated information sheet for COVID 19, accompanied by its management techniques with special emphasis on coping strategies for mental health. Further, it may also assist the policymakers to devise approaches that could enable the public to overcome the pandemic-driven adversity not only in the given situation but also futuristically. [ABSTRACT FROM AUTHOR]
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- 2022
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9. A Novel Approach of Targeting Linezolid Nanoemulsion for the Management of Lymph Node Tuberculosis.
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Choudhary, Anam, Jain, Pooja, Mohapatra, Sradhanjali, Mustafa, Gulam, Ansari, Mohammad Javed, Aldawsari, Mohammed F., Alalaiwe, Ahmed S., Mirza, Mohd. Aamir, and Iqbal, Zeenat
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- 2022
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10. Carbopol 934-based transethosomal gel of Glycyrrhizic acid for the management of skin cancer
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Yasmeen, Khan, Mohd Ashif, Iqbal, Zeenat, and Aqil, Mohd
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Glycyrrhizic acid (GA) exhibited potential anti-cancer efficacy and was used for the treatment of skin cancer. Transethosomes were developed to improve the solubility, bioavailability, and permeability of GA since it shows high solubility in ethanol. The topical route offers the benefits of higher patient compliance, easy administration, and withdrawal in case of any side effects. The GA loaded transethosome (GA-TE) was optimized by using the Box-Behnken design. The optimized GA-TE formulation was characterized for vesicle size, and zeta potential, which were 127.6 ± 0.8 nm and −24.41 ± 0.7 mV respectively. The % entrapment efficiency and % drug loading of the optimized GA-TE formulation were found to be 85.22 ± 0.94 % and 6.22 ± 0.43 % respectively. The prepared GA-TE formulation was converted to topical gel by incorporating 1 % Carbopol 934 as a gelling agent. The texture analysis of GA-TE gel showed that the values of cohesiveness, work of cohesion, consistency, and firmness were suitable for the topical delivery system for skin cancer as compared to the conventional gel. The results of ex-vivoand in-vitropermeation of GA-TE gel showed better and enhanced permeation than conventional gel. The confocal laser scanning microscopy results showed better permeation, retention, deposition, and distribution of rhodamine B-loaded GA-TE gel formulation into the skin as compared to conventional gel. The produced GA-TE formulation was proven to be beneficial in treating skin cancer based on the in-vivoresults.
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- 2024
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11. Nanotechnology interventions as a putative tool for the treatment of dental afflictions
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Jain, Pooja, Farooq, Uzma, Hassan, Nazia, Albratty, Mohammed, Alam, Md. Shamsher, Makeen, Hafiz A., Mirza, Mohd. Aamir, and Iqbal, Zeenat
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Advancement in nanotechnology and its intervention into the medical field has led to significant development in the field of oral health. Also, the combination of nanomaterial science and biotechnology in dental nanorobotics has enthralled us by adding momentum to contemporary dental practices. The progressive nature of dental afflictions often requires an umbrella approach for their prevention, diagnosis, and complete treatment. Furthermore, the complex nature of dental diseases entails customized treatment modalities, which provides the development of various nanotechnology armamentariums. Furthermore, with the objective of controlled drug delivery, researchers have done a plethora of work to apply nanomaterials such as nanospheres, nanotubes, and nanocomposites for dental infections. However, the fundamental concern with nanotechnology is cost involvement and scaleup hurdles which limits its commercialization. Nevertheless, we hope that optimal utilization of the available nanotechnological interventions for modern dental practice will shortly improve oral health. Hence, this review primarily focuses on the types of nanotechnological interventions explored for various dental afflictions. Also, the authors have attempted to enlighten the readers about the practical aspects of nanotherapeutics for dental disease, that is, a journey from laboratory to product commercialization.
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- 2022
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12. Preparation and quality by design assisted (Qb-d) optimization of bioceramic loaded microspheres for periodontal delivery of doxycycline hyclate.
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Jain, Pooja, Garg, Abhinav, Farooq, Uzma, Panda, Amulya K., Mirza, Mohd. Aamir, Noureldeen, Ahmed, Darwish, Hadeer, and Iqbal, Zeenat
- Abstract
PLGA (Lactic- co-glycolic acid) coated chitosan microspheres loaded with hydroxyapatite and doxycycline hyclate complex were developed in the present study for periodontal delivery. A modified single emulsion method was adopted for the development of microspheres. Formulation was optimized on the basis of particle size, drug loading and encapsulation efficiency with the central composite design using 2
3 factorial design. Microspheres were optimized and electron microscopy revealed their spherical shape and porous nature. In-vitro study showed initial burst and then sustained release behavior of the formulation for 14 days. Further, in-vitro antibacterial study performed on E. coli (ATCC-25922) and S. aureus (ATCC-29213) revealed concentration dependent activity. Also, in-vitro cyto-toxicity assessment ensures biocompatibility of the formulation with the fibroblast's cells. Overall, the quality by design assisted PLGA microspheres, demonstrated the desired attributes and were found suitable for periodontal drug delivery. [ABSTRACT FROM AUTHOR]- Published
- 2021
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13. FbD directed fabrication and investigation of luliconazole based SLN gel for the amelioration of candidal vulvovaginitis: a 2 T (thermosensitive & transvaginal) approach.
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Firdaus, Salma, Hassan, Nazia, Mirza, Mohd. Aamir, Ara, Tabasum, El-Serehy, Hamed A., Al-Misned, Fahad A., and Iqbal, Zeenat
- Abstract
Candidal vulvovaginitis (CVV), is the second most leading vaginal infection (global prevalence > 75%), caused due to excessive growth of Candida spp. , predominantly Candida albicans (>95% cases). The current treatment regimens for CVV are marred with the challenges of fungal resistance & infection recurrence, subsequently leading to the compromised therapeutic efficacy of anti-fungal drugs, prolonged treatment and low patient compliance. The core of the present research was the fabrication & investigation of 2 T-SLN (solid lipid nanoparticles) gel carrying luliconazole for the amelioration of CVV. '2T' symbolizes transvaginal & thermosensitive attributes of the present formulation. SLNs were prepared by a modified melt emulsification-ultra sonication method using a combination of solid lipids (Gelucire 50/13 & Precirol ATO 5), surfactant (Tween 80) and co-surfactant (Kolliphor). Formulation by design (FbD) approach was adopted to obtain appropriately screened and tailored SLNs. The optimized SLNs yielded a particle size, polydispersity index & entrapment efficiency of 62.18 nm, 0.263 & 81.5% respectively. To formulate the 2 T-gel, the final SLNs were loaded into Carbopol 971P-NF and Triethanolamine based gel. The 2 T-SLN gel was found to be easily spreadable and homogenous with mean extrudability (15 ± 0.4 g/cm
2 ), viscosity (696.42 ± 2.34 Pa·s) and %drug content (93.24 ± 0.73%) values.. The pH of the prepared 2 T-SLN gel (4.5 ± 0.5) was in concordance with the vaginal pH (normal conditions). For in-vitro characterization of an optimized 2 T-SLN gel the release kinetics & anticandidal activity were assessed which offers a %cumulative drug release of 62 ± 0.5% in 72 h and 37.3 ± 1.5 mm zone of inhibition in 48 h. The visual appearance & dimensions were determined using fluorescent microscopy (spherical shape) & transmission electron microscopy (90–120 nm) respectively. The optimized 2 T-SLN gel showcases a skin-friendly profile with no significant signs of erythema and oedema and was found to be stable at room temperature for 2 months without any visual non-uniformity/cracking/breaking. In conclusion, the current research serves a new therapeutic perspective in assessing the activity of luliconazole for vaginal drug delivery using a 2 T-SLN gel system. [ABSTRACT FROM AUTHOR]- Published
- 2021
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14. Design and development of novel bioadhesive niosomal formulation for the transcorneal delivery of anti-infective agent: In-vitroand ex-vivoinvestigations
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Zubairu, Yahaya, Negi, Lalit Mohan, Iqbal, Zeenat, and Talegaonkar, Sushama
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Gatifloxacin eye drops are frequently used in eye infections. However such formulations have a major drawback i.e. short duration of action and usually require 4–6 times installations daily. A chitosan coated niosomal formulation of gatifloxain was purposed to show a longer retention time on eyes and subsequent reduction in dosing frequency. Vesicles were prepared by solvent injection method using cholesterol and Span-60. An extensive optimization of formulation was done using different ratios of cholesterol, Span-60 and drug, revealed NS60-5 (cholesterol: span-60 50: 50 and drug content of 20 mg) to be the optimized niosome formulation. NS60-5 had shown a highest entrapment efficiency of 64.9 ± 0.66% with particle size 213.2 ± 1.5 nm and zeta potential −34.7 ± 2.2 mV. Optimized niosomes were also coated with different concentrations of chitosan and evaluated. Permeation studies had revealed that optimized niosomes (86.77 ± 1.31%) had increased the transcorneal permeation of Gatifloxacin more than two fold than simple drug solution (37.19 ± 1.1%). Longer retention potential of the coated niosomes was further verified by fluorescence microscopy. Study revealed that simple dye solution got easily washed out with in 6 h. The uncoated niosomes (NS60-5) showed a longer retention (more than 6 h), which was further enhanced in case of coated niosomes i.e. CNS60-1 (more than 12 h). Antimicrobial studies had shown the better efficacy of CNS60-1 (zone of inhibition) when compared to marketed formulation. The final chitosan formulation was found to have shown better ocular tolerability as demonstrated by corneal hydration test histopathology investigations.
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- 2024
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15. Design of expert guided investigation of native L-asparaginase encapsulated long-acting cross-linker-free poly (lactic-co-glycolic) acid nanoformulation in an Ehrlich ascites tumor model.
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Singh, Manvi, Hassan, Nazia, Verma, Devina, Thakur, Pragya, Panda, Bibhu Prasad, Panda, Amulya Kumar, Sharma, Rakesh Kumar, Mirza, Aamir, Mansoor, Sheikh, Alrokayan, Salman H., Khan, Haseeb A., Ahmad, Parvaiz, and Iqbal, Zeenat
- Abstract
Present study explores native L-asparaginase encapsulated long-acting cross-linker-free PLGA-nanoformulation in an Ehrlich ascites tumor model. L-asparaginase-PLGA nanoparticles for tumor were prepared using a double emulsion solvent evaporation technique, optimized and validated by Box-Behnken Design. L-ASN-PNs showed a particle size of 195 nm ± 0.2 nm and a PDI of 0.2. Scanning Electron Microscopy (SEM) and Transmission Electron Microscopy (TEM) techniques revealed its smooth morphology and elicited an in-vitro release of 80% of the drug, following the Higuchi drug release model. In-vivo studies of L-ASN-PNs on an Ehrlich ascites tumor (EAT) model were completed and compared with the standard medication of 5-fluorouracil (5-FU) treatment. L-ASN-PN treated mice showed a 51.15% decrease in tumor volume and 100% survival rate with no reduction in body weight, no haemotoxicity and no hepatotoxicity, as evident from the hematological parameters, and liver enzyme parameters that were well within the prescribed limits. Chemotherapy has severe side effects and restricted therapeutic success. Henceforth, the purported L-Asparaginase PLGA nanoparticles are a suitable entity for better tumor regression, intra-tumor accumulation and no hematological side-effects. [ABSTRACT FROM AUTHOR]
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- 2020
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16. Exploration of Nanoethosomal Transgel of Naproxen Sodium for the Treatment of Arthritis
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Anjum, Farzana, Zakir, Foziyah, Verma, Devina, Aqil, Mohd, Singh, Manvi, Jain, Pooja, Mirza, Mohd Aamir, Anwer, Md. Khalid, and Iqbal, Zeenat
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Background: The present work aimed to develop an ethosomal gel of naproxen sodium for the amelioration of rheumatoid arthritis. Objective: In the present work, we have explored the potential of ethosomes to deliver naproxen into deeper skin strata. Further, the anti-inflammatory efficacy of naproxen ethosomal formulation was assessed using the carrageenan-induced rat paw edema model. Methods: Naproxen sodium nanoethosomes were prepared using different proportions of lipoid S100 (50mg-200mg), ethanol (20-50%) and water, and were further characterized on the basis of vesicle morphology, entrapment efficiency, zeta potential, in-vitro drug release and ex-vivo permeation studies. Results: The optimized ethosomal formulation was found to have 129 ± 0.01 nm particle size, 0.295 Polydispersity Index (PDI), -3.29 mV zeta potential, 88% entrapment efficiency and 96.573% drug release in 24 hours. TEM and SEM analysis of the optimized formulation showed slightly smooth spherical structures. The Confocal laser scanning microscopy showed that ethosomes could easily infiltrate into deeper dermal layers (upto 104.9μm) whereas the hydroalcoholic solution of the drug could penetrate up to 74.9μm. Further, the optimized ethosomal formulation was incorporated into 1% carbopol 934 gel base and optimized wherein the transdermal flux was found to be approximately 10 times more than the hydroethanolic solution. Also, the in-vivo pharmacodynamic study of the optimized ethosomal gel exhibited a higher percentage inhibition of swelling paw edema than marketed diclofenac gel. Conclusion: The ethosomal gel was successfully developed and has shown the potential to be a good option for the replacement of conventional therapies of rheumatoid arthritis.
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- 2020
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17. Molecular Docking-Guided Ungual Drug-Delivery Design for Amelioration of Onychomycosis.
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Hassan, Nazia, Singh, Manvi, Sulaiman, Sufiyanu, Jain, Pooja, Sharma, Kalicharan, Nandy, Shyamasree, Dudeja, Mridu, Ali, Asgar, and Iqbal, Zeenat
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- 2019
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18. Novel 4-in-1 strategy to combat colon cancer, drug resistance and cancer relapse utilizing functionalized bioinspiring lignin nanoparticle.
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Siddiqui, Lubna, Mishra, Harshita, Mishra, Pawan Kumar, Iqbal, Zeenat, and Talegaonkar, Sushama
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COLON cancer prevention ,DRUG resistance in cancer cells ,CANCER relapse ,LIGNINS ,ADENOMATOUS polyposis coli ,CARCINOGENESIS ,ANIMALS ,ANTINEOPLASTIC agents ,ANTIOXIDANTS ,APOPTOSIS ,BIOLOGICAL products ,CELL cycle ,COLON tumors ,DNA ,NANOPARTICLES ,RATS ,OXIDATIVE stress ,RELATIVE medical risk ,SEQUENCE analysis ,PREVENTION - Abstract
Colon cancer is one of the fatal forms of cancer all round the world with a equal frequency of occurrence in both male and female population. Mutational changes and defects in APC (Adenomatous Polyposis Coli) and DNA mismatch repair genes accompanied by genetic chaos in oncogenic pathways leads to colon cancer. Intensive study on pathogenesis of colon cancer has been made to decipher the mechanisms underlying the development and progress of the disease so as to develop effective treatment. However, a complete therapeutic regimen is still not available for combating this deadly disease. Hurdles faced by chemotherapy include drug resistance due to P-glycoprotein transporters, untoward effects on normal cells, high cost, bio-burden of the therapy, and the most dreadful drawback is cancer relapse. The concept of cancer relapse is related to development of oxidative stress that causes cell apoptosis. If the level of oxidative stress is inadequate to cause apoptosis then it leads to cell dormancy which may revive post chemotherapy. This hypothesis aims to put forward a combinatorial approach that includes utilizing a cost effective, biocompatible and environmentally benign nanoparticulate carrier made up of lignin, loaded with anti-cancer agent and P-gp modulator, and functionalized with ligand for CD44 receptors that are over expressed on cancer cells. Antioxidant effect of lignin will overcome dormancy of cancer cells making it possible for cell cycle specific drugs to kill them and prevent relapse and active targeting will prevent untoward effects on normal cells. Thus a robust and wholesome formulation can be developed to combat colon cancer. [ABSTRACT FROM AUTHOR]
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- 2018
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19. Functionalized nanoliposomes loaded with anti survivin and anti angiogenic agents to enhance the activity of chemotherapy against melanoma by 4-pronged action.
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Mishra, Harshita, Iqbal, Zeenat, Talegaonkar, Sushama, Mishra, Pawan Kumar, Ekielski, Adam, and Jaggi, Manu
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DOXORUBICIN ,LIPOSOMES ,CANCER chemotherapy ,TUMORS ,MELANOMA ,CELECOXIB ,MELANOCYTES - Abstract
Melanoma is one of the most aggressive cancers which has very low response rate and survival rate. Melanoma cells are known to be inherently resistant to the chemotherapy which results in poor outcomes and even failure of the therapy. For this reason, a better understanding of underlying mechanism of melanoma pathogenesis and resistance is required, so that more efficient and novel therapeutic strategies can be developed. Survivin is a protein which is overexpressed in melanoma cells and is known to impart resistance to them against apoptosis. Also, melanoma cells overexpress Vascular Endothelial Growth Factor (VEGF) and basic Fibroblast Growth Factor (bFGF) angiogenic growth factors which lead to aggressive angiogenesis in melanoma cells thereby making the treatment more challenging. This hypothesis presents a combinatorial approach against melanoma where an anti-survivin agent and an anti-angiogenic agent are combined with a chemotherapeutic drug and loaded in surface functionalized liposomes in order to target specific mechanisms of melanoma, thus overcoming its resistance. Thus, the study aims to overcome the resistance of melanoma cells by developing a wise combination of drugs and achieve a higher response rate in resistant melanoma model, which is usually not achieved with the existing treatment modalities. [ABSTRACT FROM AUTHOR]
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- 2018
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20. Improved bioavailability of raloxifene hydrochloride using limonene containing transdermal nano-sized vesicles
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Waheed, Ayesha, Aqil, Mohd, Ahad, Abdul, Imam, Syed Sarim, Moolakkadath, Thasleem, Iqbal, Zeenat, and Ali, Asgar
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The present investigation was carried out with the aim of optimization of raloxifene hydrochloride-entrapped, limonene containing transfersomes for transdermal delivery. Several formulations were prepared by varying independent variables such as Phospholipid, sodium cholate and limonene while vesicles size, entrapment efficiency and polydispersity index were the dependent variables for Box-Behnken Design. Further, bioavailability assessment of raloxifene in Wistar rats was evaluated after transdermal application and compared with its oral formulation. It was observed that the optimized raloxifene loaded transfersomes formulation showed vesicle size of 107.8 nm, polydispersity index of 0.252 and entrapment efficiency of 90.2% which is close to the predicted values of 114.45 nm, 0.251 and 82.82% respectively generated by the Design Expert software. The TEM image shows the outline and the core of the well identified sealed spherical structure. Confocal laser microscopy study demonstrated that the prepared transfersomes formulation was capable to increase the permeation of probe dye into deeper layer of rat's skin in comparison to the control dye solution. The transdermal flux presented by the transfersomes gel formulation was found to be 13.20 μg/cm2/h whereas the control gel showed the transdermal flux of 2.35 μg/cm2/h across rat skin. Further the in vivo pharmacokinetic study revealed that the relative bioavailability following application of transfersomes gel in Wistar rats was found be increased by 2.71 times as compared to the oral suspension of raloxifene. It was concluded that the prepared transfersomes formulation was found to be a potentially useful drug carrier for the enhancement of raloxifene bioavailability in rats.
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- 2019
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21. Nanocarriers For Vaginal Drug Delivery
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Iqbal, Zeenat and Dilnawaz, Fahima
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Background: Vaginal drug delivery approach represents one of the imperative strategies for local and systemic delivery of drugs. The peculiar dense vascular networks, mucus permeability, and range of physiological characteristics of the vaginal cavity have been exploited for therapeutic benefit. Furthermore, the vaginal drug delivery has been curtailed due to the influence of different physiological factors like acidic pH, constant cervical secretion, microflora, cyclic changes during periods along with turnover of mucus of varying thickness. Objective: This review highlights advancement of nanomedicine and its prospective progress towards the clinic. Methods: Relevant literature reports and patents related to topics are retrieved and used. Result: The extensive literature search and patent revealed that nanocarriers are efficacious over conventional treatment approaches. Conclusion: Recently, nanotechnology based drug delivery approach has promised better therapeutic outcomes by providing enhanced permeation and sustained drug release activity. Different nanoplatforms based on drugs, peptides, proteins, antigens, hormones, nucleic material, and microbicides are gaining momentum for vaginal therapeutics.
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- 2019
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22. Development of NIPAAm-PEG acrylate polymeric nanoparticles for co-delivery of paclitaxel with ellagic acid for the treatment of breast cancer
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Suri, Suruchi, Mirza, Mohd. Aamir, Anwer, Md. Khalid, Alshetaili, Abdullah S., Alshahrani, Saad M., Ahmed, Farhan Jalees, and Iqbal, Zeenat
- Abstract
The aim of the current study was to develop a dual-loaded core shell nanoparticles encapsulating paclitaxel (PTX) and ellagic acid (EA) by membrane dialysis method. Based on particle size, polydispersity index (PDI), and entrapment efficiency, the dual drug-loaded nanoparticles (F2) was optimized. The optimized nanoparticles (F2) showed a particle size of 140±2 nm and a PDI of 0.23±3. The size and the morphology were confirmed by transmission electron microscopy (TEM) and found agreement with the results of dynamic light scattering. The entrapment efficiencies of total drug (PTX and EA), PTX, and EA in the nanoparticles (F2) were measured as 80%, 62.3%, and 37.7%, respectively. The in vitrorelease profile showed a controlled release pattern for 48 h. A higher cytotoxicity was observed with nanoparticles (F2) in comparison to free PTX. The results revealed that co-delivery of PTX and EA could be used for its oral delivery for the effective treatment of breast cancer.
- Published
- 2019
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23. Mesoporous Silica Nanoparticles: A Versatile Platform for Biomedical Applications
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Jain, Pooja, Hassan, Nazia, Iqbal, Zeenat, and Dilnawaz, Fahima
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Background: Nanotechnology-based drug delivery approach has emerged as a promising field, where different kinds of formulations are developed for therapeutic applications. Inflowing of nanomedicine developed through various biomaterials appears to be a game changer in the domain of pharmaceutical and biotechnological industries. Nanomedicines propose to overcome the major constraints of conventional medicine of low solubility and stability, non-adequate pharmacokinetic profiles and side effects. Objectives: Mesoporous Silica Nanoparticles (MSNs) have garnered significant attention in biomedical applications for its multifunctionality. The porous structure of MSNs provides the opportunity for heavy drug loading, controlled release and ligand functionality. From last decades, a lot of interest has been generated owing to the better drug delivery attributes of MSNs to introduce unique biological effects for its suitable therapeutic application. Methods: The review article gives an insight into the current advancement of usage of MSNs in drug delivery for cancer, non-cancer and biosensors based biomedical applications along with technology that is protected by patents. Conclusion: The future success of MSNs is widened because of their valuable characteristic that easily combines with various functionalities which would display enormous potential translational possibilities.
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- 2018
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24. Development and pharmacokinetic evaluation of spray-dried self-nanoemulsifying drug delivery system of sertraline.
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Rahman, Md., Mujahid, Md., Hussain, Arshad, and Iqbal, Zeenat
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- 2017
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25. Box-Behnken Design of Experiment Assisted Development and Optimization of Bendamustine HCl loaded Hydroxyapatite Nanoparticles
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Thomas, Shindu C., Madaan, Tushar, Iqbal, Zeenat, and Talegaonkar, Sushama
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Background: Bendamustine HCl, an antineoplastic drug, has a very short life of about 40 minutes which necessitates administration of large doses which leads to increased side effects as well as costs. Objective: The present work describes the fabrication, optimization, and evaluation of bioactive hydroxyapatite nanoparticles to achieve sustained delivery of bendamustine HCl. Methods: Hydroxyapatite nanoparticles (NPs) were prepared by the wet chemical precipitation method by reacting a calcium and phosphate precursor and the reaction was optimized via Box-Behnken DOE. The drug was loaded on particles by physical adsorption. Various analytical studies were performed on the fabricated nanoparticles in addition to biodistribution studies to establish the physicochemical and biological characteristics of the designed formulation. Results: pH of the reactant solution was found to have a more profound effect on the particle size and size distribution in comparison to reactant concentration. The particles were found to have a spherical morphology by SEM. Size of the blank and drug-loaded nanoparticles was found to be 130±20 nm by TEM. Energy Dispersive X-ray Spectroscopy (EDS) studies confirmed the presence of hydroxyapatite as the dominant phase while DSC studies indicated the presence of the drug in its amorphous form after its adsorption on NPs. Tissue distribution studies further suggested that the majority of drug concentration was released in blood rather than the other organs implying low organ toxicity. Conclusion: Bendamustine loaded hydroxyapatite nanoparticles were successfully optimized and fabricated. Favorable results were obtained in in vitro, in vivo, and analytical studies.
- Published
- 2018
26. An Overview of the Regulatory and Developmental Strategies of Chronotherapeutics.
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Mirza, Mohd. Aamir, Shakeel, Faiyaz, and Iqbal, Zeenat
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ANTIHYPERTENSIVE agents ,BIOAVAILABILITY ,CIRCADIAN rhythms ,CLINICAL chronobiology ,DRUG delivery systems ,PHARMACEUTICAL chemistry ,PHARMACEUTICAL technology ,STRATEGIC planning ,DRUG development ,GOVERNMENT regulation ,DRUG approval - Abstract
The pivotal idea toward the development of chronotherapeutics is synchronizing the in vivo drug bioavailability with the rhythms of the disease to optimize therapeutic outcomes and minimize side effects, which is contrary to the homeostatic theory of drug delivery. The advent of formulation technologies, marketing exclusivities of innovative products, and provisions/amendments in regulatory frameworks have led to the development of commercial chronotherapeutic products, but their numbers are few and are confined mainly to diseases of the cardiovascular system. A major bottleneck for its development would be the understanding of rhythmic variations of disease, but following regulatory pathways for commercial development has always been challenging. In this article, a few commercial products have been investigated in view of their developmental strategies in order to find out the minimum preclinical and clinical studies needed for the development of chronotherapeutics. [ABSTRACT FROM AUTHOR]
- Published
- 2016
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27. Development and pharmacokinetic evaluation of spray-dried self-nanoemulsifying drug delivery system of sertraline
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Rahman, Md., Mujahid, Md., Hussain, Arshad, and Iqbal, Zeenat
- Abstract
The objective of the present study was to develop solid self-nanoemulsifying drug delivery system (SNEDDS) of poorly absorbed drug sertraline (SRT) and evaluation of its pharmacokinetic parameters in rats. The composition of optimized liquid SNEDDS was (25.42 % v/v) Labrafil M 2125 CS and Maisine 35-1 (1:1), (49.72 % v/v) Tween 80 and (24.86 % v/v) Lauroglycol 90 containing 25 mg SRT. Solid SNEDDS was prepared by spray-drying the liquid SNEDDS using dextran 40 as solid carrier. There was no significant difference (p > 0.05) in the droplet size of reconstituted nanoemulsion between both liquid and solid SNEDDS. The surface characterization of spray-dried powder showed a satisfactory regular spherical shape of particles. The internal physical state of SRT was verified by X-ray diffraction analysis indicated the transformation of crystalline structure of SRT to amorphous and molecularly dispersed state. In vitro release of SRT from solid SNEDDS was highly significant (p < 0.01) as compared to unformulated SRT. After oral administration of solid SNEDDS to adult Sprague–Dawley (SD) rats, the area under the curve (AUC) were 2.8- and 6.8-folds and the maximum plasma concentration (Cmax) were 3.5 -and 13-folds higher, respectively compared to those of conventional capsule and unformulated drug suspension. These results reveal that solid SNEDDS results in a significantly increased absorption of SRT compared with that from the marketed conventional capsule and aqueous suspension of SRT. Thus, this solid SNEDDS may provide a useful solid dosage form for oral delivery of poorly-water soluble lipophilic compounds.
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- 2017
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28. Development and optimization of ketoconazole loaded nano-transfersomal gel for vaginal delivery using Box-Behnken design: In vitro, ex vivocharacterization and antimicrobial evaluation
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Singh, Shalu, Verma, Devina, Mirza, Mohd. Aamir, Das, Ayan Kumar, dudeja, Mridu, Anwer, Md. Khalid, Sultana, Yasmin, Talegaonkar, Sushama, and Iqbal, Zeenat
- Abstract
In the present study, Ketoconazole loaded transfersomal formulation was developed using 3-factor, 3-level Box-Behnken design to find out the best formulation. Optimized transfersomal formulation was prepared by solvent evaporation method and evaluated in vitrofor vesicle size (126.9 ± 5.45 nm) and entrapment efficiency (82.6%). Transfersomal gel were developed by incorporation of optimized transfersomal formulation into 1% carbopol gel base and characterized by physical evaluation and rheological studies. The cumulative release of drug were shown at 72 h approximately 74% and 97% of ketoconazole from suspension and transfersomal gels respectively. The flux for transfersomal gel was found to be about 3 times that of drug suspension gel. Results of the histopathological studies of gel treated skin indicated negligible sign of toxicity and irritation. The prepared transfersomal gel showed antimicrobial activity against Candida albicans with MIC 4.57–4.6 μg/mL and better zone of inhibition as compared to reference standard. The developed gel showed promising antimicrobial activity. These overall findings suggested that transfersomal gel holds an excellent potential for ketoconazole delivery.
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- 2017
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29. Biosimilars: Scientific Consideration and Regulatory Frameworks
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Mirza, Mohd. Aamir, Ray, Anmol Kumar, and Iqbal, Zeenat
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Background: In order to establish safety and efficacy, generic medicines are required to prove bioequivalence with the innovator product while in case of Biosimilars (copy version innovator biologicals) requirements are product specific (case by case basis) and there is no common data requirement to establish the safety and efficacy. The challenge is to determine the nature of clinical and non-clinical studies required. Methods: The major causes of variability are its large size, complicated structure, stability issues, microheterogeneity involved and manufacturing process, etc. It is also difficult to draw a common regulatory pathway which covers all possible complex products. So, in this article we discuss the technicalities involved with this complex therapeutics (emphasizing on biosimilars) and look into regulatory frameworks for market authorization, keeping USFDA, EMA and ICH guidelines as standards. Results: Regulatory authorities have identified three main characteristics of a protein that must be considered during development i.e., 3D structures, post translational modifications (PTMs) and protein aggregation. Agencies generally consider the totality of the evidence to support a demonstration of biosimilarity, and recommend that sponsors should use a stepwise approach in the development of biosimilar products which may include a comparison of the proposed product and RBP with respect to Structure, Function, Animal Toxicity, Human Pharmacokinetics (PK) and Pharmacodynamics (PD), Clinical Immunogenicity, and Clinical Safety and effectiveness. Conclusion: There is also ambivalence about its future market considering the complicated development process involved. Its market growth has been alluring for pharmaceutical companies so far. An in-depth understanding of science involved and technologies available to explore may lead us to an affable regulatory pathway. In this review we put an effort to touch upon these aspects of biopharmaceuticals.
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- 2016
30. 3D Printing in Pharmaceuticals: Regulatory Perspective
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Mirza, Mohd. A. and Iqbal, Zeenat
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Background: The last few decades have witnessed enormous advancements in the field of Pharmaceutical drug, design and delivery. One of the recent developments is the advent of 3DP technology. It has earlier been successfully employed in fields like aerospace, architecture, tissue engineering, biomedical research, medical device and others, has recently forayed into the pharmaceutical industry.Commonly understood as an additive manufacturing technology, 3DP aims at delivering customized drug products and is the most acceptable form of“personalized medicine”. Methods: Data bases and search engines of regulatory agencies like USFDA and EMA have been searched thoroughly for relevant guidelines and approved products. Other portals like PubMed and Google Scholar were also ferreted for any relevant repository of publications are referred to wherever required. Results: So far only one pharmaceutical product has been approved in this category by USFDA and stringent regulatory agencies are working over the drafting of guidelines and technical issues. Major research of this category belongs to the academic domain. Conclusion: It is also implicit to such new technologies that there would be numerous challenges and doubts before these are accepted as safe and efficacious. The situation demands concerted and cautious efforts to bring in foolproof regulatory guidelines which would ultimately lead to the success of this revolutionary technology.
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- 2018
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31. Qbd based and Box-Behnken design assisted Oral delivery of stable lactone (active) form of Topotecan as PLGA nanoformulation: Cytotoxicity, pharmacokinetic, in vitro,and ex vivogut permeation studies
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Khuroo, Tahir, Khuroo, Arshad, Hussain, Afzal, Mirza, Mohd Aamir, Panda, Amulya K., Wani, Javid, and Iqbal, Zeenat
- Abstract
Topotecan being highly water-soluble drug with a property of getting converted from biologically active lactone form to biologically inactive carboxylate form, thus making it a candidate with very less bioavailability; so, our approach was to develop a stable Topotecan lactone (active) form nanoparticles (TNPs). TNPs were developed and optimized successfully with size of 130.0 ± 3.9 nm, 0.102 ± 0.009 PDI and zeta potential of −18.0 ± 2.1 mV. The percent entrapment efficiency of active lactone form of Topotecan (TOP) in optimized formulation of TNPs was 65.72 ± 1.9%, that was enhanced by approximately 15% from 65.72 ± 1.9% to 73.27 ± 2.1% by using Zn2+ions as a complexing agent between PLGA polymer and Topotecan drug. Lyophilized TNPs under DSC study showed the entrapment of TOP in amorphous or solution form, which was further confirmed by XRD studies. In vitrorelease study depicts that the drug TOP in TNPs showed initial burst release followed by sustained release for up to 72 h in PBS (pH 7.4). Ex-vivogut permeation study revealed that TNPs enhanced the permeation of TOP through the gut. Further, in vivopharmacokinetic data showed that the oral bioavailability of TOP was increased by four folds from TNPs. TNPs in comparison to TOP drug also showed a significant reduction in IC50in cell line studies on MCF-7/Adr resistant cells.
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- 2022
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32. An Overview of the Regulatory and Developmental Strategies of Chronotherapeutics
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Mirza, Mohd. Aamir, Shakeel, Faiyaz, and Iqbal, Zeenat
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The pivotal idea toward the development of chronotherapeutics is synchronizing the in vivo drug bioavailability with the rhythms of the disease to optimize therapeutic outcomes and minimize side effects, which is contrary to the homeostatic theory of drug delivery. The advent of formulation technologies, marketing exclusivities of innovative products, and provisions/amendments in regulatory frameworks have led to the development of commercial chronotherapeutic products, but their numbers are few and are confined mainly to diseases of the cardiovascular system. A major bottleneck for its development would be the understanding of rhythmic variations of disease, but following regulatory pathways for commercial development has always been challenging. In this article, a few commercial products have been investigated in view of their developmental strategies in order to find out the minimum preclinical and clinical studies needed for the development of chronotherapeutics.
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- 2016
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33. An Overview of the Regulatory and Developmental Strategies of Chronotherapeutics
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Mirza, Mohd. Aamir, Shakeel, Faiyaz, and Iqbal, Zeenat
- Abstract
The pivotal idea toward the development of chronotherapeutics is synchronizing the in vivo drug bioavailability with the rhythms of the disease to optimize therapeutic outcomes and minimize side effects, which is contrary to the homeostatic theory of drug delivery. The advent of formulation technologies, marketing exclusivities of innovative products, and provisions/amendments in regulatory frameworks have led to the development of commercial chronotherapeutic products, but their numbers are few and are confined mainly to diseases of the cardiovascular system. A major bottleneck for its development would be the understanding of rhythmic variations of disease, but following regulatory pathways for commercial development has always been challenging. In this article, a few commercial products have been investigated in view of their developmental strategies in order to find out the minimum preclinical and clinical studies needed for the development of chronotherapeutics.
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- 2016
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34. Investigative Approaches for Oral Delivery of Anticancer Drugs: A Patent Review
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Tariq, Mohammad, T. Singh, Anu, Iqbal, Zeenat, J. Ahmad, Farhan, and Talegaonkar, Sushama
- Abstract
Typically, chemotherapy has been dominated by intravenous administration. Though, inclination towards oral ingestion of chemotherapeutics is increasing since it offers ample of fascinating opportunities including better quality of life, treatment advantages and low healthcare cost. However, low or moderate bioavailability along with significant inter-patient variability and narrow therapeutic window challenges their oral administration. Thus, optimization of oral route with maximized efficacy and miniminal adverse events is a challenging area. To surmount the challenges, a number of strategies like P-glycoprotein (P-gp) modulation, colloidal carrier etc. have been under investigation and scientists are exploring the utility of solid dispersions, prodrugs, biconjugates, complexes, microparticulate, and nanoparticulate systems (liposome, SLN, dendrimers, SEDDS, nanoparticles). Among these, nanoparticulate systems have shown promising results due to their targeting potential and ability to alter absorption pathways. Functional excipients with P-gp modulating activity are also being explored for more effective oral delivery of chemotherapeutics. This article explores the encouraging reports, recent patents and inventions on the feasibility and applicability of oral administration of chemotherapeutics.
- Published
- 2016
35. Enhanced transdermal delivery of lutein via nanoethosomal gel: Formulation optimization, in-vitroevaluation, and in-vivoassessment
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Nikhat, Andleeb, Hasan, Nazeer, Iqbal, Zeenat, Kesharwani, Prashant, and Talegaonkar, Sushama
- Abstract
Lutein has low oral bioavailability and penetration through the skin. Therefore, the major objective is the development of ethosomal gel loaded with lutein to enhance dermal deposition of lutein. Lutein-loaded formulation (Lut-eth) was developed and optimized using QbD software. The characterization of Lut-eth formulation was performed using zeta sizing (131.3 ± 1.10 nm) and zeta potential (−21.9 mV) which was later validated by electron microscopy. The lut-eth gel was prepared and values for content uniformity, spreadability, consistency, firmness, and toughness were found to be 97.89 ± 1.05%, 7.29 ± 0.015 gcm/s, 2.495 ± 0.24 g s, 0.210 ± 0.01g, and 0.37 ± 0.01 respectively. Rheological investigation reveals viscosity was 2.56.2 mPa s (millipascal second) and shows high elasticity and stability. whereas, consistency, firmness, toughness, the force of adhesion, and work of adhesion was found to be 2.495 ± 0.24 g s, 0.210 ± 0.01g, 0.37 ± 0.01, −0.23 ± 0.05 N, and −55.61 ± 0.11 N s respectively. The lut-eth gel had a maximum plasma concentration of 9.428 ± 3.5 ng/mL in 4 h with AUC0-1279. 679 ± 9.87 ng h mL−1. The drug release study shows sustain release behavior of prepared formulation and a similar sustain release pattern was observed in and Ex-vivo release studies. Confocal laser microscopy, In-vitro,antioxidant study shows better deposition and improved antioxidant effect of formulation which was further validated by Ex-vivoantioxidant assay. Therefore, bearing in mind all these findings, it can be said that Lut-eth gel could be a novel formulation to improve lutein deposition on skin.
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- 2022
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36. A validated HPTLC method for determination of terbutaline sulfate in biological samples: Application to pharmacokinetic study.
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Faiyazuddin, Md., Rauf, Abdul, Ahmad, Niyaz, Ahmad, Sayeed, Iqbal, Zeenat, Talegaonkar, Sushma, Bhatnagar, Aseem, Khar, Roop K., and Ahmad, Farhan J.
- Abstract
Abstract: Terbutaline sulfate (TBS) was assayed in biological samples by validated HPTLC method. Densitometric analysis of TBS was carried out at 366nm on precoated TLC aluminum plates with silica gel 60F
254 as a stationary phase and chloroform–methanol (9.0:1.0, v/v) as a mobile phase. TBS was well resolved at RF 0.34±0.02. In all matrices, the calibration curve appeared linear (r2 ⩾0.9943) in the tested range of 100–1000ngspot−1 with a limit of quantification of 18.35ngspot−1 . Drug recovery from biological fluids averaged ⩾95.92%. In both matrices, rapid degradation of drug favored and the T0.5 of drug ranged from 9.92 to 12.41h at 4°C and from 6.31 to 9.13h at 20°C. Frozen at −20°C, this drug was stable for at least 2months (without losses >10%). The maximum plasma concentration (Cpmax ) was found to be 5875.03±114ngmL−1 , which is significantly higher than the maximum saliva concentration (Csmax , 1501.69±96ngmL−1 ). Therefore, the validated method could be used to carry out pharmacokinetic studies of the TBS from novel drug delivery systems. [Copyright &y& Elsevier]- Published
- 2011
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37. Development and clinical trial of nano-atropine sulfate dry powder inhaler as a novel organophosphorous poisoning antidote.
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Ali, Raisuddin, Jain, Gaurav K., Iqbal, Zeenat, Talegaonkar, Sushma, Pandit, Pragati, Sule, Sunita, Malhotra, Geena, Khar, Roop K., Bhatnagar, Aseem, and Ahmad, Farhan J.
- Subjects
CLINICAL trials ,ATROPINE ,SULFATES ,MEDICAL research - Abstract
Abstract: The aim of the work was to develop, characterize, and carry out a clinical trial with nano–atropine sulfate (nano-AS) dry powder inhaler (DPI), because this route may offer several advantages over the conventional intramuscular route as an emergency treatment, including ease of administration and more rapid bioavailability. Different batches of nanoparticles of AS were produced using variants of nanoprecipitation method. The influence of the process parameters, such as the types and quantity of solvent and nonsolvent, the stirring speed, the solvent-to-nonsolvent volume ratio, and the drug concentration, was investigated. The methodology resulted in optimally sized particles. Bulk properties of the particles made by the chosen methodology were evaluated. A clinical trial was conducted in six healthy individuals using a single DPI capsule containing 6 mg nano-AS DPI in lactose. Early blood bioavailability and atropinization pattern confirmed its value as a potential replacement to parenteral atropine in field conditions. The formulation seems to have the advantage of early therapeutic drug concentration in blood due to absorption through the lungs as well as sustained action due to absorption from the gut of the remaining portion of the drug. [Copyright &y& Elsevier]
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- 2009
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38. Development and Validation of a Stability-Indicating High-Performance Thin-Layer Chromatographic Method for the Simultaneous Quantification of Sparfloxacin and Flurbiprofen in Nanoparticulate Formulation
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Tariq, Mohammad, Iqbal, Zeenat, Ali, Javed, Baboota, Sanjula, Parveen, Rabea, Mirza, Mohd. Aamir, Ahmad, Sayeed, and Sahni, Jasjeet Kaur
- Abstract
A simple, sensitive, precise, rapid, and reliable high-performance thin-layer chromatographic (HPTLC) method for the simultaneous estimation of sparfloxacin (SPF) and flurbiprofen (FLB) in bulk drug as well as in dual drug loaded poly-(lactic-co-glycolic acid) (PLGA) nanoparticles was developed. In this method, aluminumbacked silica gel 60 F254plates (20 × 10 cm: 200 µm thickness) were used as stationary phase and chloroform-methanol-formic acid (7.5:1:1, v/v) as an optimized mobile phase. Developed chromatogram was scanned at 258 nm, the wavelength of maximum absorption SPF and FLB. Regression analysis of the calibration data showed an excellent linear relationship between peak area versus drug concentration. Linearity was found to be in the range of 100–600 ng spot−1and 40–800 ng spot−1for SPF and FLB, respectively. The suitability of the developed HPTLC method for simultaneous estimation of SPF and FLB was established by validating it as per the ICH guidelines. The limits of detection (LOD) and quantification (LOQ) for SPF were found to be ≈13 and ≈40 ng spot−1, respectively, and those for FLB ≈27 ng spot−1and ≈82 ng spot−1, respectively. The developed method was found to be linear (r2= 0.999), precise (% RSD < 1.5% repeatability and <2.55% for intermediate precision), accurate (mean recovery of within the range of 98–102%), specific, and robust. Stress-induced degradation studies revealed the suitability of method for the quantitative determination of drugs in the presence of degradants. The developed method has been successfully applied for the determination of entrapment efficiency, drug loading, in vitrodrug release profile and stability assessment of dual drug loaded PLGA nanoparticles (NPs).
- Published
- 2014
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39. Nanopotentiated combination cancer therapy: Chemotherapeutic and chemosensitizer (2C approach).
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Verma, Devina, Khuroo, Tahir, Talegaonkar, Sushama, and Iqbal, Zeenat
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PATHOLOGICAL physiology ,CANCER treatment ,DRUG delivery systems ,CARCINOGENS ,BIOACTIVE compounds - Abstract
An insight into the complex cancer pathophysiology reveals that a dependable amelioration of the disease could only be envisaged with a multipronged treatment approach. It is highly evident that singular chemotherapeutic agents used in clinical practice have shown limitations like severe side effects, MDR and are often associated with poor QOL while combinations of drugs have yielded better therapeutic outcomes. The current hypothesis takes it a step forward wherein a chemotherapeutic agent is combined with a natural chemosensitizer, both loaded into a nanopotentiated particulate system, which would eventually deliver the drug cargo at the target site with certitude. The encapsulated natural bioactive would then favorably act on the tumor milieu through multiple portals and chemosensibilize the cells towards cytotoxic action of the synthetic drug moiety. This 2C (chemotherapeutic and chemosensitizer) approach along with nanosystem’s attributes like high payload, prolonged action and diminished side effects would proffer a more dependable treatment modality. In conclusion, the proposed system would be a value addition to the currently available armamentarium of cancer treatment tools. [ABSTRACT FROM AUTHOR]
- Published
- 2015
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40. Nanopotentiation of Propolis for Revocation of Enzyme Imbalance in UVB Induced Cutaneous Toxicity in Murine Model: a Preliminary Study for Chemoprotection of Skin Cancer
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Verma, Devina, Mirza, Mohd. Aamir, Talegaonkar, Sushama, Ahmed, Farhan Jalees, and Iqbal, Zeenat
- Abstract
Indian Propolis, a resin-like substance obtained from plants and modified by bees is a blend of various naturalcomponents and a potential candidate for topical application for chemoprevention of skin cancer. In the present study, thepotential role of propolis loaded ethosomal transgel for the chemoprevention of skin cancer was investigated. Ethosomalvesicular systems were optimized by varying the proportions of lecithin and ethanol taking vesicle size, polydispersity index(PDI) and entrapment efficiency as dependent variables. The vesicles were found to be unilamellar spherical shapedentities with size varying from 100 nm to 300 nm and entrapment efficiency in a range of 48% to 84%. The permeationand extent of penetration of the optimized formulation were evaluated by Franz diffusion cell and Confocal scanning lasermicroscopy (CSLM) respectively. It showed a sustained mode of release and remarkable penetration capacity of vesicles(133µm) as compared to hydroethanolic solution of the drug. Histopathological evaluation of the formulation treated skinrevealed the interaction of vesicles with the skin which was further supported by FTIR analysis reflecting the mechanismof vesicle permeation via skin. Propolis loaded ethosomal vesicles were then incorporated into carbopol gel and characterizedusing a texture profile analyzer. The optimized gel so obtained was then finally evaluated for its chemo preventiveactivity by exposing Swiss albino mice to UVB radiation. The study indicated the possible use of propolis for the preventionof skin cancer through a deep-rooted delivery via ethosomal system eventually circumventing the problem of poorpenetrability of topical preparations.
- Published
- 2013
41. Thymoquinone: Major Molecular Targets, Prominent Pharmacological Actions and Drug Delivery Concerns
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Singh, Anjali, Ahmad, Iqbal, Akhter, Sohail, Zaki Ahmad, Mohammad, Iqbal, Zeenat, and J. Ahmad, Farhan
- Abstract
The oil of black seed (Nigella sativa) has been used as a folk medicine to treat a number of physiological disorders such as epilepsy, gastric problems, allergic conditions and various hepato-biliary ailments. Despite being unaware of the underlying phenomena for the cure of these diseases, people especially in the Mediterranean region have been using this ancient herb since ages. Researches in the 20th century conducted with the aim of tracking molecular pathways of anti-oxidant and anti-inflammatory mechanisms disclosed a great deal of information pertaining to the structural-activity relationships. Rigorous studies revealed that the major active constituent of Nigella sativa oil (NSO) is Thymoquinone (THQ) which exerts the majority of pharmacological actions observed by the essential oil. Since then, a large number of investigator groups have identified numerous molecular pathways of almost all major diseases which can be cured by THQ. Being a phytochemical, THQ has a high lipophilicity which makes it a poorly soluble agent in aqueous fluids restricting its systemic bioavailability. Also, THQ is highly light and heat-sensitive which further complicates its successful formulation for drug delivery. This review thus offers an insight to adequately comprehend the large number of pharmacological actions along with general mechanisms and major molecular targets pertaining to THQ. Additionally, a section dealing with the application of nanotechnological approaches to appropriately deliver the drug to its intended site of action has been elaborated.
- Published
- 2012
42. Solid Nanoemulsion Preconcentrate (NanOsorb) for Oral Delivery of Sertraline: Development and Characterization
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Akhlaquer Rahman, Md., Iqbal, Zeenat, and Hussain, Arshad
- Abstract
The purpose of this study was to develop a solid nanoemulsion preconcentrate (NanOsorb) for poorly watersoluble drug sertraline (SRT). The liquid SNEDDS consisted of LabrafilM 2125 CS and Maisine 35-1 in 1:1 ratio as oil phase, Tween 80 as surfactant, Lauroglycol 90 as co-surfactant and active constituent sertraline free base. SRT free base, rather than commercially available hydrochloride salts (SRT.HCl) was used due to its much higher solubility in lipidic solvents. The NanOsorb formulation was prepared by adsorbing the liquid SNEDDS on different solid adsorbents. Reconstitution properties of both liquid and solid formulation demonstrate insignificant difference (p 0.05) in the globule size. External morphology and physical state of sertraline in NanOsorb formulation were examined by TEM, DSC, and X-ray powder diffraction. In vitro release profile of NanOsorb was found to be significant (p < 0.001) in comparison to the plane SRT in pH 1.2, 4.5 and 6.8 buffers. Formulation was subjected to stability studies as per International Conference on Harmonization (ICH) guidelines and was found to be stable. No significant variations were observed in the formulation over a period of 3 months at accelerated conditions. Results deduced that NanOsorb formulation may provide an improvement in dissolution profile of poorly water-soluble drugs in the form of solid dosage form.
- Published
- 2012
43. Formulation optimization and in vitro characterization of sertraline loaded self-nanoemulsifying drug delivery system (SNEDDS) for oral administration
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Rahman, Md., Iqbal, Zeenat, and Hussain, Arshad
- Abstract
Sertraline is a selective serotonin reuptake inhibitors used as major therapeutic advances in psychiatry and is drug of choice for treatment of major depressive disorders. The drug (free base) encounters problem of poor aqueous solubility and vulnerability to enzymatic degradation in liver. The hydrochloride salts of free base revert back to its original form in gastrointestinal tract leading to slow/poor absorption. In the current study, sertraline loaded self-nanoemulsifying drug delivery systems (SNEDDS) were prepared in an attempt to circumvent the problems associated with poor aqueous solubility, vulnerability to enzymatic degradation in liver and to sort out the problems associated with salt formation. Preliminary screening was carried out to select proper ingredient combinations. Ternary phase diagrams were then constructed and an optimum system was designated. Formulations selected were then compared for optimization. The systems were assessed for robustness, globule size, cloud point, percentage transmittance, surface morphology and drug release. An optimum system composed of oil (25.42 %), surfactant (49.72 %), and co-surfactant (24.86 %). It possessed a mean globule size, cloud point and percentage transmittance of 63.5 nm, 90 °C and 82.43 %, respectively. Transmission electron microscopy demonstrated spherical particle morphology. The drug release from the selected formulation was significantly higher than other SNEDDS and drug suspension as well. Optimized formulation was subjected to stability studies at different temperature and relative humidity and was found to be stable. No significant variations were observed in the formulation over a period of 3 months at accelerated conditions.Sertraline is a selective serotonin reuptake inhibitors used as major therapeutic advances in psychiatry and is drug of choice for treatment of major depressive disorders. The drug (free base) encounters problem of poor aqueous solubility and vulnerability to enzymatic degradation in liver. The hydrochloride salts of free base revert back to its original form in gastrointestinal tract leading to slow/poor absorption. In the current study, sertraline loaded self-nanoemulsifying drug delivery systems (SNEDDS) were prepared in an attempt to circumvent the problems associated with poor aqueous solubility, vulnerability to enzymatic degradation in liver and to sort out the problems associated with salt formation. Preliminary screening was carried out to select proper ingredient combinations. Ternary phase diagrams were then constructed and an optimum system was designated. Formulations selected were then compared for optimization. The systems were assessed for robustness, globule size, cloud point, percentage transmittance, surface morphology and drug release. An optimum system composed of oil (25.42 %), surfactant (49.72 %), and co-surfactant (24.86 %). It possessed a mean globule size, cloud point and percentage transmittance of 63.5 nm, 90 °C and 82.43 %, respectively. Transmission electron microscopy demonstrated spherical particle morphology. The drug release from the selected formulation was significantly higher than other SNEDDS and drug suspension as well. Optimized formulation was subjected to stability studies at different temperature and relative humidity and was found to be stable. No significant variations were observed in the formulation over a period of 3 months at accelerated conditions.
- Published
- 2012
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44. Development and Validation of UHPLC/ESI-Q-TOF-MS Method for Terbutaline Estimations in Experimental Rodents: Stability Effects and Plasma Pharmacokinetics
- Author
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Faiyazuddin, Md., Ahmad, Niyaz, Iqbal, Zeenat, Talegaonkar, Sushma, Bhatnagar, Aseem, Krishen Khar, Roop, and Jalees Ahmad, Farhan
- Abstract
An ultra high performance liquid chromatography-electrospray ionization-tandem mass spectrometric method (UHPLC/ESI-Q-TOF-MS) for the analysis of terbutaline (TB) in Wistar rat plasma has been developed and validated. The chromatographic separation was achieved on a Waters ACQUITY UPLCTM BEH C18 (100.0 mmx2.1 mm; 1.7 μm) column using isocratic mobile phase, consisting of 2 mM ammonium acetate and acetonitrile (90: 10; v/v), at a flow rate of 0.25 mL min-1. The transitions occurred at m/z 226.19→152.12 for TB, and m/z 260.34→183.11 for the internal standard. The recovery of the analytes from Wistar rat plasma was optimized using liquid- liquid extraction technique (LLE) in ethyl acetate. The total run time was 3.0 min and the elution of TB occurred at 1.85±0.05 min. The linear dynamic range was established over the concentration range 1–1000 ng mL-1 (r2; 0.9938±0.0005) for TB. The intra-assay and inter-assay accuracy in terms of CV was in between 1.8–3.5. The lower limit of quantitation (LLOQ) for TB was 1.0 ng mL-1. Analytes were stable under various conditions (in autosampler, during freeze–thaw, at room temperature, and under deepfreeze conditions). The developed method was successfully applied for pharmacokinetic profiling in rodents.
- Published
- 2012
45. The emerging role of P-glycoprotein inhibitors in drug delivery: a patent review
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Akhtar, Naseem, Ahad, Abdul, Khar, Roop Kishan, Jaggi, Manu, Aqil, Mohammed, Iqbal, Zeenat, Ahmad, Farhan Jalees, and Talegaonkar, Sushama
- Abstract
Introduction:The ATP-binding cassette superfamily contains membrane transporter proteins that transport a wide range of diverse compounds across cellular membranes. The P-glycoprotein (P-gp) is an important member of this family and a multi-specific drug efflux transporter that plays a significant role in governing the bioavailability of many clinically active drugs. The inhibition of this efflux transporter by various P-gp inhibitors forms a distinctive approach in improving bioavailability and conquering drug resistance. Most P-gp inhibitors exhibit limitations associated with their safety and unwanted pharmacokinetic interactions, thereby restraining their clinical applicability.Areas covered:This review explores the investigations on the feasibility and applicability of various classes of P-gp inhibitors as described in recent patents for enhanced drug delivery.Expert opinion:Several candidates presently under development look promising as P-gp inhibitors, e.g., tariquidar and elacridar. Pharmaceutical excipients currently constitute the most promising class of P-gp inhibitors and are considered safe and pharmaceutically acceptable for use in formulations. In addition, lipid-based excipients and thiolated polymers play an active role in affecting P-gp-mediated transport not only by altering the membrane fluidity or ATPase activity but by down regulating P-gp expression. An additional overture such as the prodrug derivatization of P-gp substrates is a feasible approach to bypass P-gp-mediated efflux.
- Published
- 2011
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46. Stability indicating HPTLC method for determination of terbutaline Sulfate in bulk and from Submicronized dry Powder inhalers
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Faiyazuddin, Md., Ahmad, Sayeed, Iqbal, Zeenat, Talegaonkar, Sushma, Ahmad, Farhan Jalees, Bhatnagar, Aseem, and Khar, Roop Krishen
- Abstract
A stability-indicating high-performance thin-layer chromatographic (HPTLC) method has been developed for the determination of terbutaline sulfate (TBS) as a bulk drug and in pharmaceutical formulations (submicronized dry powder inhalers). The separation was achieved on TLC aluminum plates precoated with silica gel 60F-254 using chloroform-methanol (9.0:1.0 v/v) as mobile phase. The densitometric analysis was carried out at 366 nm wavelength. Compact spots appeared at Rf= 0.34 ± 0.02. For the proposed procedure, linearity (r2= 0.9956 ± 0.0015), limit of quantification (28.35 ng spot−1), limit of detection (9.41 ng spot−1), recovery (97.06 - 99.56%), and precision (≤1.86) were found to be satisfactory. TBS was subjected to acid and alkali hydrolyses, oxidation and photodegradation treatments. The degraded products were well separated from the pure drug. Statistical analysis reveals that the developed method has potential for routine analysis and stability testing of terbutaline sulfate in pharmaceutical drug delivery systems.
- Published
- 2010
- Full Text
- View/download PDF
47. Impact of Magnetic Nanoparticles in Biomedical Applications
- Author
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Naqvi, Saba, Samim, Mohammad, Dinda, Amit, Iqbal, Zeenat, Telagoanker, Sushma, Ahmed, Farhan, and Maitra, Amaranth
- Abstract
In the recent years, there has been a growing interest in the development of nanoparticles based targeting agents for the tumor diagnostics and therapeutics. This is because of their potential to detect the tumor and treat the diseased tissue at the cellular and molecular level. In this respect nanoscale magnetic materials have shown a very promising therapeutic concept and offer a new perspective for the diagnostic and target drug delivery approach. The magnetic nanocarriers have the ability to accumulate at any desired pharmacological site just by the guidance of external magnetic field. But, the interactions of these magnetic nanocarriers with the biological environment are rare and depend largely upon their surface chemistry and size. To increase the interactions and achieve the desired pharmaceutically acceptable delivery system, the surface of magnetic nanocarriers is modified in various ways by coating with organic polymers and inorganic metals or oxides. On the basis of surface characteristics, a number of effective magnetically driven therapies have been proposed by many researchers and protected through patents time to time.
- Published
- 2009
48. Components Screening and Influence of Surfactant and Cosurfactant on Nanoemulsion Formation
- Author
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Azeem, Adnan, Rizwan, Mohammad, Ahmad, Farhan, Khar, Roop, Iqbal, Zeenat, and Talegaonkar, Sushama
- Abstract
Proper selection of oils, surfactants and cosurfactants along with their optimum concentration is crucial to obtain stable, mild and clinically acceptable nanoemulsions. The focus of the present study was, therefore, to provide an efficient screening approach for the excipients selection for the optimum nanoemulsion formulation development. The oils studied included Lauroglycol 90, Capryol 90, olive oil, jojoba oil, oleic acid and Labrafil M1944. The drug solubility in the oil was taken as the criterion for oil selection. Labrasol, Cremophor EL, Tween 60 and Tween 80 were the surfactants evaluated for determining the solubilizing capacity for the oil. Among them Cremophor EL was found to be an efficient emulsifier for the oil phase. The effect of different cosurfactants such as ethanol, isopropyl alcohol, butanol, propylene glycol, PEG 400 and Carbitol on the phase behaviour of the pseudoternary system Capryol 90/Cremophor EL/cosurfactant/water was investigated. Nanoemulsion region obtained was used as an assessment criterion to evaluate the cosurfactants. The effect of Cremophor EL/carbitol mass ratio on the nanoemulsion formation was also studied by varying the ratio from 3:1 to 1:3 for the further optimization of the system. The highest nanoemulsion region was obtained at Cremophor EL: Carbitol in the mass ratio of 1:1. Formulations were selected from the phase diagram at this mass ratio at a fixed concentration of surfactant mixture (i.e. 45 wt/wt) with increasing concentration of oil (5, 10, 15, 20 wt/wt) and subjected to thermodynamic stability tests. The optimized formulations were characterized for particle size, viscosity, pH and refractive index measurements. The droplet size of all the selected formulations was found to be less than 100 nm. The formulations were thermodynamically stable and can be effectively used for the drug delivery applications.
- Published
- 2009
49. CNS Drug Delivery Systems: Novel Approaches
- Author
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Pathan, Shadab, Iqbal, Zeenat, Zaidi, Syed, Talegaonkar, Sushma, Vohra, Divya, Jain, Gaurav, Azeem, Adnan, Jain, Nitin, Lalani, Jigar, Khar, Roop, and Ahmad, Farhan
- Abstract
The brain is a delicate organ, and nature has very efficiently protected it. The brain is shielded against potentially toxic substances by the presence of two barrier systems: the blood brain barrier (BBB) and the blood cerebrospinal fluid barrier (BCSFB). Unfortunately, the same mechanisms that protect it against intrusive chemicals can also frustrate therapeutic interventions. Despite aggressive research, patients suffering from fatal and/or debilitating central nervous system (CNS) diseases, such as brain tumours, HIV encephalopathy, epilepsy, cerebrovascular diseases and neurodegenerative disorders, far outnumber those dying of all types of systemic cancers or heart diseases. The abysmally low number of potential therapeutics reaching commercial success is primarily due to the complexity of the CNS drug development. The clinical failure of many probable candidates is often, ascribable to poor delivery methods which do not pervade the unyielding BBB. It restricts the passive diffusion of many drugs into the brain and constitutes a significant obstacle in the pharmacological treatment of central nervous system (CNS) disorders. General methods that can enhance drug delivery to the brain are, therefore, of great pharmaceutical interest. Various strategies like non-invasive methods, including drug manipulation encompassing transformation into lipophilic analogues, prodrugs, chemical drug delivery, carrier-mediated drug delivery, receptor/vector mediated drug delivery and intranasal drug delivery, which exploits the olfactory and trigeminal neuronal pathways to deliver drugs to the brain, are widely used. On the other hand the invasive methods which primarily rely on disruption of the BBB integrity by osmotic or biochemical means, or direct intracranial drug delivery by intracerebroventricular, intracerebral or intrathecal administration after creating reversible openings in the head, are recognised. Extensive review pertaining specifically, to the patents relating to drug delivery across the CNS is currently available. However, many patents e.g. US63722506, US2002183683 etc., have been mentioned in a few articles. It is the objective of this article to expansively review drug delivery systems for CNS by discussing the recent patents available.
- Published
- 2009
50. An HPTLC Method for the Determination of Minocycline in Human Plasma, Saliva, and Gingival Fluid after Single Step Liquid Extraction
- Author
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Jain, Nilu, Jain, Gaurav Kumar, Iqbal, Zeenat, Talegaonkar, Sushma, Ahmad, Farhan Jalees, and Khar, Roop Krishen
- Abstract
A rapid, sensitive and specific high-performance thin-layer chromatographic (HPTLC) method was developed and validated for determination of minocycline in human plasma, saliva, and gingival fluid samples. Densitometric analysis of minocycline was carried out at 345 nm after single step extraction with methanol. The method uses TLC aluminium plates pre-coated with silica gel 60F-254 as a stationary phase and methanol–acetonitrile–isopropyl alcohol–water (5:4:0.5:0.5, v/v/v/v) as mobile phase. In all the three matrices, the calibration curve was linear (r2≥ 0.9958) in the tested range of 100 – 1200 ng spot−1with a limit of quantification of 15.4 ng spot–1. Drug recovery from plasma, saliva and gingival fluid averaged 97.7%. Intra- and inter-day accuracies, determined at three different concentrations, were 95.08 to 100.6% and the corresponding precision (% CV) values were < 4.61%. In all the three matrices, rapid degradation of drug occurred and the half-life of drug ranged from 9.9 to 16.1 h at 4˚C and from 6.3 to 11.5 h at 20˚C. Frozen at −20˚C, this drug was stable for at least 2 months and can tolerate two freeze-thaw cycles without losses higher than 10%. The method’s ability to quantify minocycline with precision, accuracy and sensitivity makes it useful in pharmacokinetic studies.
- Published
- 2009
- Full Text
- View/download PDF
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