Search

Women face a significant change in their reproductive health as menopause sets in. It is marred with numerous physiological changes that negatively impact their quality of life. This universal, transition phase is associated with menopausal and postmenopausal syndrome, which may spread over 2–10 years. This creates a depletion of female hormones causing physical, mental, sexual and social problems and may, later on, manifest as postmenopausal osteoporosis leading to weak bones, causing fractures and ultimately morbidity and mortality. Menopausal hormone therapy generally encompasses the correction of hormone balance through various pharmacological agents, but the associated side effects often lead to cessation of therapy with poor clinical outcomes. However, it has been noticed that phytotherapeutics is trusted by women for the amelioration of symptoms related to menopause and for improving bone health. This could primarily be due to their reduced side effects and lesser costs. This review attempts to bring forth the suitability of phytotherapeutics/herbals for the management of menopausal, postmenopausal syndrome, and menopausal osteoporosis through several published research. It tries to enlist the available botanicals with their key constituents and mechanism of action for mitigating symptoms associated with menopause as well as osteoporosis. It also includes a list of a few herbal commercial products available for these complications. The article also intends to collate the findings of various clinical trials and patents available in this field and provide a window for newer research avenues in this highly important yet ignored health segment. [ABSTRACT FROM AUTHOR]

Objectives: The main objective of the study was to assess Knowledge of oral hygiene practices during the pandemic and its post-COVID-19 impact among the community of Delhi and NCR region. Materials and Methods: A cross-sectional online survey was conducted among the local population of Delhi and NCR during April and May of 2022. Links to the survey were sent by email and several social media platforms, including WhatsApp. Before answering any questions on the questionnaire, participants were asked to read the study's information and provide their informed permission. Results: A total of 516 people did the survey and their responses were included in data analysis. 78 (15.12) agreed and 379 (73.455) said no access and 59(11.43%) said not always with a p-value<0.05. 464 (89.92%) agreed that they experienced anxiety and fear during COVID-19 related to their oral hygiene whereas 52 (10.08%) did not, with p-value<0.05. 406 (76.68%) agreed on receiving guidance and recommendations from a dental or a health professional to maintain or improve oral health during COVID-19 whereas 110 (21.32%) disagreed with p-value<0.05. Conclusion: Teledentistry was merely used; its use must be encouraged to provide online services to patients in such a pandemic situation. Yet people tried to change their oral hygiene habits and diet to improve their oral health. [ABSTRACT FROM AUTHOR]

Background: In India, the cosmetics industry has expanded significantly because of changing lifestyles and increased awareness. In terms of earning the most money from the personal care and cosmetics industry in 2021, India is ranked fourth globally. Many cosmetics sold in India include ingredients that cannot be used on humans. Objective: To assess knowledge, attitudes, and practice toward the uses of cosmetics and cosmetovigilance in India. Methods: A cross‑sectional study was conducted, from April to May 2022, among the general population living in the Delhi NCR region, India. Study questionnaires (printed and survey link) were distributed in public as well as at workplaces for the survey. Results: Around 268 (54.78%) females and 223 (45.21%) males participated in the survey. Amongst the total respondents ‑ 407 (83%) agreed that they are using cosmetic products on a daily basis, females 229 (85.44%), being the majority users compared to males 178 (80%), with a significant P value = 0.011. Most of the people reported side effects of shampoos ‑ 7.13% (hair fall, hair thinning, dryness of the scalp, itching), followed by allergic reactions to moisturizers ‑ 5.70%. Conclusion: Because of the right safety and effectiveness mentorship of cosmetics, regulatory agencies and stakeholders should adopt this broadly. Cosmetovigilance needs to be put into practice. [ABSTRACT FROM AUTHOR]

Quercetin is the major polyphenolic flavonoid that belongs to the class called flavanols. It is found in many foods, such as green tea, cranberry, apple, onions, asparagus, radish leaves, buckwheat, blueberry, broccoli, and coriander. It occurs in many different forms, but the most abundant quercetin derivatives are glycosides and ethers, namely, Quercetin 3-O-glycoside, Quercetin 3-sulfate, Quercetin 3-glucuronide, and Quercetin 3′-metylether. Quercetin has antioxidant, anti-inflammatory, cardioprotective, antiviral, and antibacterial effects. It is found to be beneficial against cardiovascular diseases, cancer, diabetes, neuro-degenerative diseases, allergy asthma, peptic ulcers, osteoporosis, arthritis, and eye disorders. In pre-clinical and clinical investigations, its impacts on various signaling pathways and molecular targets have demonstrated favorable benefits for the activities mentioned above, and some global clinical trials have been conducted to validate its therapeutic profile. It is also utilized as a nutraceutical due to its pharmacological properties. Although quercetin has several pharmacological benefits, its clinical use is restricted due to its poor water solubility, substantial first-pass metabolism, and consequent low bioavailability. To circumvent this limited bioavailability, a quercetin-based nanoformulation has been considered in recent times as it manifests increased quercetin uptake by the epithelial system and enhances the delivery of quercetin to the target site. This review mainly focuses on pharmacological action, clinical trials, patents, marketed products, and approaches to improving the bioavailability of quercetin with the use of a nanoformulation. [ABSTRACT FROM AUTHOR]

Studies on biofilm-related infections are gaining prominence owing to their involvement in most clinical infections and seriously threatening global public health. A biofilm is a natural form of bacterial growth ubiquitous in ecological niches, considered to be a generic survival mechanism adopted by both pathogenic and non-pathogenic microorganisms and entailing heterogeneous cell development within the matrix. In the ecological niche, quorum sensing is a communication channel that is crucial to developing biofilms. Biofilm formation leads to increased resistance to unfavourable ecological effects, comprising resistance to antibiotics and antimicrobial agents. Biofilms are frequently combated with modern conventional medicines such as antibiotics, but at present, they are considered inadequate for the treatment of multi-drug resistance; therefore, it is vital to discover some new antimicrobial agents that can prevent the production and growth of biofilm, in addition to minimizing the side effects of such therapies. In the search for some alternative and safe therapies, natural plant-derived phytomedicines are gaining popularity among the research community. Phytomedicines are natural agents derived from natural plants. These plant-derived agents may include flavonoids, terpenoids, lectins, alkaloids, polypeptides, polyacetylenes, phenolics, and essential oils. Since they are natural agents, they cause minimal side effects, so could be administered with dose flexibility. It is vital to discover some new antimicrobial agents that can control the production and growth of biofilms. This review summarizes and analyzes the efficacy characteristics and corresponding mechanisms of natural-product-based antibiofilm agents, i.e., phytochemicals, biosurfactants, antimicrobial peptides, and their sources, along with their mechanism, quorum sensing signalling pathways, disrupting extracellular matrix adhesion. The review also provides some other strategies to inhibit biofilm-related illness. The prepared list of newly discovered natural antibiofilm agents could help in devising novel strategies for biofilm-associated infections. [ABSTRACT FROM AUTHOR]

Black cohosh (Cimicifuga racemosa) (CR) is a popular herb and is medically lauded for ameliorating myriad symptoms associated with menopause. However, its pharmaceutical limitations and non-availability of a patient-compliant drug delivery approach have precluded its prevalent use. Henceforth, the current research premise is aimed at developing an ethosomal gel incorporating triterpene enriched fraction (TEF) obtained from CR and evaluating its effectiveness through the transdermal application. TEF-loaded ethosomes were formulated using solvent injection, optimized and characterised. The optimized ethosomes were then dispersed into a polymeric gel base to form ethosomal gel which was further compared with the conventional gel by in-vitro and ex-vivo experiments. Here, the quality by design (QbD) approach was exploited for the optimization and development of ethosomal gel. The elements of QbD comprising initial risk assessment, design of experimentation (DoE), and model validation for the development of formulation have all been described in detail. The optimized ethosomes (F03) showed a nanometric size range, negative zeta potential and good entrapment. The in vitro release profile of gel revealed a burst release pattern following the Korsmeyer Peppas model having Fickian diffusion. The transdermal flux of ethosomal gel was observed to be more than that of conventional gel. Texture analysis and rheological characterization of the gel, revealed good strength showing shear thinning and pseudoplastic behaviour. The confocal microscope investigation revealed the deeper skin permeation of ethosomal gel than conventional gel. This result was further strengthened by DSC, IR and histological assessment of the animal skin (Wistar rat), treated with the optimized formulation. Conclusively, the implementation of QbD in the formulation resulted in a better understanding of the process and the product. It aids in the reduction of product variability and defects, hence improving product development efficiencies. Additionally, the ethosomal gel was found to be a more effective and successful carrier for TEF than the conventional gel through the transdermal route. Moreover, this demands an appropriate animal study, which is underway, for a stronger outcome. [ABSTRACT FROM AUTHOR]

Psoriasis, due to its unique pathological manifestations and the limited success of existing therapeutic modalities, demands dedicated domain research. Our group has developed nanotherapeutics consisting of bioactives such as Thymoquinone (TQ) and Fulvic acid (FA), which have been successfully incorporated into a Nanoemulsion gel (NEG), taking kalonji oil as oil phase. The composition is aimed at ameliorating psoriasis with better therapeutic outcomes. TQ is a natural bio-active that has been linked to anti-psoriatic actions. FA has anti-inflammatory actions due to its free radical and oxidant-scavenging activity. Our previous publication reports the formulation development of the NEG, where we overcame the pharmaco-technical limitations of combining the above two natural bioactives. In vitro evaluation of the optimized NEG was carried out, which showed an enhanced dissolution rate and skin permeation of TQ. This work furthers the pharmaceutical progression of dual-targeted synergistic NEG to treat psoriasis. A suitable animal model, BALB/c mice, has been used to conduct the in vivo studies, which revealed the effective anti-psoriatic action of TQ. Molecular docking studies corroborated the results and revealed a good binding affinity for both the targets of TNF-α (Tumor necrosis factor) and IL-6 (Interlukin-6). Tissue uptake by Confocal laser scanning microscopy (CLSM), a skin interaction study of the gel formulation, and an antioxidant free radical scavenging assay (1-1 Diphenyl-2-picrylhydrazyl DPPH) were also carried out. It was concluded that the NEG may be effective in treating psoriasis with minimal side effects. [ABSTRACT FROM AUTHOR]

After the successful commercial exploitation of 3D printing technology, the advanced version of additive manufacturing, i.e., 4D printing, has been a new buzz in the technology-driven industries since 2013. It is a judicious combination of 3D printing technologies and smart materials (stimuli responsive), where time is the fourth dimension. Materials such as liquid crystal elastomer (LCE), shape memory polymers, alloys and composites exhibiting properties such as self–assembling and self-healing are used in the development/manufacturing of these products, which respond to external stimuli such as solvent, temperature, light, etc. The technologies being used are direct ink writing (DIW), fused filament fabrication (FFF), etc. It offers several advantages over 3D printing and has been exploited in different sectors such as healthcare, textiles, etc. Some remarkable applications of 4D printing technology in healthcare are self-adjusting stents, artificial muscle and drug delivery applications. Potential of applications call for further research into more responsive materials and technologies in this field. The given review is an attempt to collate all the information pertaining to techniques employed, raw materials, applications, clinical trials, recent patents and publications specific to healthcare products. The technology has also been evaluated in terms of regulatory perspectives. The data garnered is expected to make a strong contribution to the field of technology for human welfare and healthcare. [ABSTRACT FROM AUTHOR]

The present study was aimed to develop chitosan-coated enamel adhesive device of CAP-P 407 (Cellulose acetate phthalate-Poloxamer 407), loaded with MNC (Minocycline) for sustained release and site-specific drug delivery system for the carious lesion. The average tensile strength and in-vitro drug release of uncoated dental film were found to be 15.97 kg/mm2 and 98.11% in 24 h, respectively. The average in-vitro mucoadhesion time and tooth adhesion strength of the finished product was found to be 249 minutes and 268 g, respectively. In-vitro antimicrobial study showed the drug concentration is well above MIC even after 8 hours of drug release. [ABSTRACT FROM AUTHOR]

In the present investigation, a nanoemulgel of minocycline was formulated and optimized for an improved drug delivery and longer retention time in the targeted area. Combining eucalyptus oil, Tween 20, and Transcutol HP, different o/w nanoemulsions were formulated by the oil phase titration method and optimized by pseudo-ternary phase diagrams. The morphology, droplet size, viscosity, and refractive index of the thermodynamically stable nanoemulsion were determined. Furthermore, optimized nanoemulsion was suspended in 1.0% w/v of Carbopol 940 gel to formulate the nanoemulgel, and for this, pH, viscosity, and spreadability were determined and texture analysis was performed. To compare the extent of drug penetration between nanoemulsion and nanoemulgel, ex vivo skin permeation studies were conducted with Franz diffusion cell using rat skin as the permeation membrane, and the nanoemulgel exhibited sustained-release behavior. It can be concluded that the suggested minocycline-containing naoemulgel is expected to treat acne rosacea more effectively. [ABSTRACT FROM AUTHOR]

Obesity is a complex, multifactorial, lifestyle-related disorder which affects nearly one-third of the global population. In more than one way, obesity classifies as a potential indicator or contributing factor of various clinical conditions, subsequently leading to poor health outcomes and compromised quality of life (QoL). The high prevalence and reporting rate of obesity is irrespective of geographical difference, ethnicity and gender, however, they most often serve as predisposing risk factors for obesity. Additionally, environmental changes, availability & affordability of low nutrition, yet palatable food, hormonal disbalance and variation at the genetic level, prominently exacerbates the condition of obesity and its related effects. Clinically, obesity, may either lead to other pathophysiological conditions as well, such as liver dysfunction, polycystic ovarian syndrome, hypertension, coronary artery diseases and psychological impairment or vice-versa. Henceforth, to cope with the challenges of obesity and related conditions, a healthy lifestyle, personal care & social well-being is of prime importance. Additionally, a customized strategy to address the economic expenditure and newer therapeutic perspectives should be implemented to control the widespread damage of human population by this condition. The present review focuses on providing a brief knowledge about nutritional, biochemical, genetic and psychological aspects of obesity and its epidemiology. [ABSTRACT FROM AUTHOR]

Resveratrol (RVT) is a well known phyto-chemical and is widely used in dietary supplements and botanical products. It shows a wide range of pharmacological/beneficial effects. Therefore, it can be a potential candidate to be developed as phyto-pharmaceutical. Multiple diseases are reported to be treated by the therapeutic effect of RVT since it has antioxidant, anti-cancer activity and anti-inflammatory activities. It also has a major role in diabetes, arthritis, cardiac disorder and platelet aggregation etc. The major requirements are establishments regarding safety, efficacy profile and physicochemical characterization. As it is already being consumed in variable maximum daily dose, there should not be a major safety concern but the dose needs to be established for different indications. Clinical trials are also being reported in different parts of the world. Physicochemical properties of the moiety are also well reported. Moreover, due to its beneficial effect on health it leads to the development of some intellectual property in the form of patents. [ABSTRACT FROM AUTHOR]

The bio-analytical method was developed and validated for simultaneous detection and quantification of paclitaxel (PAC) and erlotinib (ERL) in plasma samples. The sample preparation process was accomplished by liquid-liquid extraction technique. The dried and reconstituted samples were subjected to chromatography on Discovery -C18 (50 × 4.6 × 5µm) column and a mobile phase, composed of a mixture of 0.1% formic acid in water: acetonitrile (70:30, v/v), in isocratic mode at a flow rate of 0.6 mL/min. Liquid chromatography coupled to tandem mass spectrometry detection in positive ion mode was selected to provide optimal selectivity and sensitivity. The mass transitions of erlotinib, erlotinib13C6, Paclitaxel and docetaxel were m/z 394.5→278.4, m/z 400.4→284.5, m/z 876.6→308.4 and m/z 830.0→304.0 respectively. The linearity in the calibration curves was obtained in the concentration range of 3.6 − 1006.7 ng/ml (r ≥ 0.99) for erlotinib and 5.3 − 1500.0 ng/mL for paclitaxel with an LLOQ (lower limit of quantification) of 3.6 and 5.3 ng/ml respectively. The run time was achieved in 2.5 min only, for all the analytes. [ABSTRACT FROM AUTHOR]

Global burden of chronic wounds has increased drasticallyas they are vulnerable to bacterial infections that causes inflammation, thereby leads to a delay in the healing process. Furthermore, wound care and dressing industry is subjected to a global market of $30.4 billion by 2024. Our work entails fabrication of polymeric electrospun nanofibers loaded with different concentration of the amoxicillin (AMX) antibiotic. Biodegradable and biocompatible poly (vinyl) alcohol (PVA)/poly(meth)(methacrylate)(PMMA) polymerswere blended with different AMX concentration (100, 150, 200 and 250 mg) and fabricated by electrospinning technique. Morphology, structural properties and drug release from electrospun nanofibers depend on the different concentrations of drug incorporated in PVA:PMMA blend of polymer. Furthermore, these studies revealed drug-excipient compatibility and drug encapsulation within the nanofiber. In-vitro release study showed the AMX release time from PVA: PMMA: AMX was extended up to 7 days for AMX-250 with an initial burst release of 70% and further sustained drug release. Electrospun nanofibers of PVA:PMMA:AMX showed greater zone of inhibition of S. aureus as 2.1±0.4 cm for 100-AMX, 2.3±0.5 cm for 150-AMX, 2.4±0.1 for 200-AMX and 3.4±0.3 cm for 250-AMX. These results demonstrate that AMX retains the anti-bacterial activity and hence can be used as a potential wound dressing candidate. [ABSTRACT FROM AUTHOR]

Women's health is an imminent concern worldwide, but it remains an ignored segment of research in most developing countries, and is yet to take the center stage in even developed nations. Some exclusive female health concerns revolve around both pathological and physiological aspects. These gender-specific maladies include breast, cervical, and ovarian cancers, and physiological concerns such as menopause and osteoporosis, which are often coexistent. Recently, women's health issues, including postmenopausal syndrome, have attracted the attention of researchers and practitioners alike, opening newer pharmaceutical research and clinical avenues. Although not counted as a disease, postmenopausal syndrome (PMS) is a female health phenomenon underpinned by hormonal depletion. Enhanced life expectancy in women has added to their suffering, and pharmacological interventions are needed. Amongst the available treatment modalities, the use of numerous botanicals has emerged as an efficient health management tool for women. Cimicifuga racemosa (CR or Black Cohosh) is a plant/herb which has been traditionally exploited and extensively used by women. This review is an attempt to compile and provide a summary of the importance of CR in complementary and alternative therapies for the improvement of various disorders related to women, such as menopausal syndrome, mammary cancer, and osteoporosis. It aims to systematically highlight the bioactive constituents, pharmacology, pharmacokinetics, therapeutic potentials, quality control processes, chromatographic techniques, and possible mechanisms of action of clinically effective phytomedicine for women's health. Various clinical trials and patents relating to CR and women's health have been collated. Furthermore, the plant and its related products have been considered from a regulatory perspective to reveal its commercial feasibility. The present review summarizes the existing data on CR focusing on women's health, which can help to introduce this traditional phytomedicine to the world and provide some reference for future drug development. [ABSTRACT FROM AUTHOR]

Mass consumerization of three-dimensional (3D) printing innovation has revolutionised admittance of 3D-printing in an expansive scope of ventures. When utilised predominantly for industrial manufacturing, 3D-printing strategies have rapidly attained acquaintance in different parts of health care industry. 3D-printing is a moderately new technology that has discovered promising applications in the medication conveyance and clinical areas. This review intends to explore different parts of 3D- printing innovation concerning pharmaceutical and clinical applications. Review on pharmaceutical products like tablets, caplets, films, polypills, microdots, biodegradable patches, medical devices (uterine and subcutaneous), patient specific implants, cardiovascular stents, etc. and prosthetics/anatomical structures, surgical models, organs and tissues created utilising 3D-printing is being presented. In addition, the regulatory understanding and current IP and clinical trial status pertaining to 3D fabricated products/medical applications have also been funnelled, garnering information from different web portals of regulatory agencies and databases. It is additionally certain that for such new innovations, there would be difficulties and questions before these are acknowledged as protected and viable. The circumstance demands purposeful and wary endeavours to acquire regulations which would at last prompt the accomplishment of this progressive innovation, thus various regulatory challenges faced have been conscientiously discussed. [ABSTRACT FROM AUTHOR]

Bacterial infections have increased dramatically due to microbial biofilm formation resulting in chronic pathological conditions in human subjects. Microbial biofilm causes poor drug penetration and antibiotic resistance, which has made site‐specific sustained drug delivery the most appropriate option. Our work entails fabrication of ciprofloxacin hydrochloride (CPX) loaded nanofibers using polyvinyl alcohol (PVA) and poly(meth) methacrylate (PMMA) employing electrospinning method to form PVA:PMMA:CPX nanofibers mat. These nanofibers mat were optimized, characterized, and further subjected to anti‐biofilm activity. Microscopic images revealed average nanofibers diameter of 243 ± 80 nm with smooth surface morphology. Analytical graphs and thermal analysis confirmed drug encapsulation and drug‐polymer compatibility. In vitro studies demonstrated sustained release of CPX for 22 days displaying Hixon Crowell and two‐stage desorption kinetics. Anti‐biofilm activity showed zones of inhibition 3.0 ± 0.5 cm, 2.8 ± 0.1 cm, 2.9 ± 0.2 cm for Escherichia coli, Staphylococcus aureus, Enterococcus faecalis, respectively which was well above the minimum inhibitory concentration levels of the bacteria forming biofilm. Conclusively, these nanofibers mat have potential to be used as an anti‐biofilm product. [ABSTRACT FROM AUTHOR]

The objective of the present study was to prepare valencene (sesquiterpene) containing invasomes for itraconazole (ITZ) transungual delivery using central composite design. The phospholipid (X1) and valencene (X2) were selected as an independent variables, while vesicles size (Y1), entrapment efficiency (Y2) and in vitro drug release (Y3) were chosen as dependent variables. The antifungal activity of optimized formulation was screened against Trichophyton rubrum, a common causative onychomycosis pathogen, by cup plate method. The optimized ITZ-loaded invasomes formulation presented vesicles size of 176.8 ± 6.03 nm, entrapment efficiency of 83.21 ± 4.11% and in vitro drug release of 75.22 ± 5.03%. The ITZ-loaded invasomes gel formulation showed good homogeneity, pH 6.5 ± 0.23, viscosity 7.33 ± 0.67 Pa s and drug content 94.13 ± 1.13%. The spreadability and extrudability of developed ITZ-loaded invasomes gel were found to be 7.85 ± 0.24 gcm/s and 162 ± 2.74 g, respectively. The ITZ-loaded invasomes gel presented 71.11 ± 3.65% cumulative permeation of drug via goat hooves. The in vitro antifungal activity depicted that the ITZ-loaded invasomes gel and marketed preparation were presented zone of inhibition of 21.42 mm and 10.64 mm against T. rubrum respectively. Hence the prepared ITZ-loaded invasomes formulation could therefore be a promising topical dosage to mitigate the indications and hasten the cure for onychomycosis than conventional available therapies. [ABSTRACT FROM AUTHOR]

Onychomycosis is a difficult-to-treat fungal infection of the human nail plate or bed that primarily affects the natural anatomy of human toe and finger nails, leading to a hard, brittle, and uneven nail surface. The severe structural mutilation of nails restricts the application of conventional formulations and makes onychomycosis therapy a challenging clinical premise. Oral therapy with drugs such as terbinafine hydrochloride and itraconazole may lead to drug interactions and systemic adverse effects, whereas topical treatment with drugs such as ciclopirox olamine and amorolfine are often associated with poor drug permeation through the nail bed. Recent advances in laser/photodynamic therapies and their application in onychomycosis has emerged as a new therapeutic paradigm with global acceptance. The present article is an attempt to provide an insight into onychomycosis and its manifestations, and summarises the various therapeutic modalities, with a greater focus on laser/photodynamic therapy. [ABSTRACT FROM AUTHOR]

Objectives: In the current study, we have evaluated pharmacy undergraduate student's knowledge and perceptions towards this class of drug products. Methods: A random survey of 349 pharmacy students of six different pharmacy colleges from north India was carried out on an online-based questionnaire system to investigative knowledge and attitude towards biological/biosimilar. Chi-square test was used for the computation of p-value. Results: Out of 349 students, 80.22% of students have good knowledge about the same. 44.12% responded that the products are generally safe while 60.74% responded that these products don't produce any kind of adverse drug reaction. 62.18% students were not updated about ADR reporting system in India. But the students think that its knowledge is important but the educational training has been inadequate. Conclusion: Due to unawareness about biological products, there is a need to address the knowledge gap in graduating pharmacy students. Lack of knowledge could be overcome by upgrading the curriculum or through professional development courses. [ABSTRACT FROM AUTHOR]

Nanomedicine combination therapy, a strategy to delivery multiple drugs via a single nanosystem has opened new avenues to treat cancer and prevent side effects and overcome chemoresistance. The present work utilizes a chemotherapeutic agent topotecan hydrochlorideand a natural chemosensitizer (thymoquinone, TQ) incorporated into poly (lactic-co-glycolic acid) nanoparticles (PLGA NPs) to target tumor. The objective of the present work is to develop a reversed phase HPLC method for simultaneous estimation of TQ along with the pH dependent lactone and carboxylate forms of topotecan and validate its applicability. Chromatographic separation was obtained on Agilent 1200 Infinity series C18 analytical column using gradient elution with acetonitrile and 1% triethylamine acetate (TEAA) buffer (pH 5.5) as mobile phase and a flow rate of 0.8 mL/min. Analytical detection was done at 253 nm. Validation was performed as per ICH guidelines and characterization and stability of the optimized nanoparticles were evaluated. The retention time of 5.93, 8.73, and 19.76 min was obtained for lactone, carboxylate and TQ, respectively. Linearity response was established in the range of 5‒45 µg/mL. The limits of detection and quantification were found to be 15 and 50 ng/mL for lactone, 18 and 59 ng/mL for carboxylate, and 5 and 18 ng/mL for TQ, respectively. The method was validated in terms of robustness, precision, accuracy, specificity and percent loading, entrapment efficiency, and in vitro drug release. The stability of the nanoparticles was determined using the above validated method. The method was successfully validated and applied for routine analyses indicating its use as a suitable analytical tool to determine efficiency of the proposed therapy. [ABSTRACT FROM AUTHOR]

The major drawback of the eye drops is rapid elimination of drug from the precorneal region, thus ensuing poor bioavailability as well as therapeutic efficacy. To conquer these limitations, a pH triggered in situ gel was developed for sustained delivery of levofloxacin. Two polymers namely hydroxypropyl methylcellulose (HPMC) and sodium alginate along with the boric acid buffer were used to formulate the in situ gel. Based on the various physicochemical evaluation parameters like pH, clarity and gelling capacity placebo formulations were selected and further characterized for viscosity, in vitro release, ex vivo corneal permeation, and histopathological studies. The optimized in situ gel (F28) showed sustained release of 93 ± 4.23% for 24 h and cumulative drug permeation of 71.81 ± 4.7% for 72 h. Additionally, ocular irritation study and histopathology of the formulation treated cornea confirm the non-irritancy of the optimized formulation. Based on all the above performed studies, it can be concluded that the in situ gel would present a fruitful alternative for the ocular infections. [ABSTRACT FROM AUTHOR]

Despite the ongoing extensive research, cancer therapeutics still remains an area with unmet needs which is hampered by shortfall in the development of newer medicines. The present study discusses a nano-based combinational approach for treating solid tumor. Dual-loaded nanoparticles encapsulating gemcitabine HCl (GM) and simvastatin (SV) were fabricated by double emulsion solvent evaporation method and optimized. Optimized nanoparticles showed a particle size of 258 ± 2.4 nm, polydispersity index of 0.32 ± 0.052, and zeta potential of −12.5 mV. The size and the morphology of the particles wee further confirmed by transmission electron microscopy (TEM) and scanning electron microscopy, respectively of the particles. The entrapment efficiency of GM and SV in the nanoparticles was 38.5 ± 4.5% and 72.2 ± 5.6%, respectively. The in vitro release profile was studied for 60 h and showed Higuchi release pattern. The cell toxicity was done using MTT assay and lower IC50 was obtained with the nanoparticles as compared to the pure drug. The bioavailability of GM and SV in PLGA nanoparticles was enhanced by 1.4-fold and 1.3-fold respectively, compared to drug solution. The results revealed that co-delivery of GM and SV could be used for its oral delivery for the effective treatment of pancreatic cancer. [ABSTRACT FROM AUTHOR]

Background: Dual loaded liposomes have always been a hot topic of investigation because of their therapeutic advantages over single drug regimens. But simultaneous estimation of both the drugs during in vitro and in vivo analysis is most of the times a major obstacle for the researchers. This problem is even bigger when the two drugs are of opposite nature (hydrophilic and lipophilic). Methods: Here, we formulated anti-cancer liposomes loaded with Dacarbazine (hydrophilic) and Eugenol (lipophilic). Since both the drugs are of different nature, selecting a solvent system that dissolves both the drugs, as well as is a suitable media for determining in vitro release, was a challenge. After resolving this issue, we developed a simple and robust UV method based on the principle of solving simultaneous equations generated after Absorptivity measurements of the two drugs. Results: UV spectrophotometer is preferred over other analytical techniques because of its availability, broad area of applications, easy and fast handling, robust nature and simplicity. Thus, using the developed method for simultaneous determination, loading of the two drugs and their simultaneous release from the liposomes was determined. Conclusion: We could perform the in-vitro characterization of formulated anti-cancer liposomes using the developed UV Absorptivity method, which justifies the practical applicability of the developed method and proved that the method is specific and reproducible. [ABSTRACT FROM AUTHOR]

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 vitro release 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. [ABSTRACT FROM AUTHOR]

Purpose: Amikacin, a water-soluble aminoglycoside antibiotic used to treat gram-negative bacillary infections, is a Biopharmaceutics Classification System class III drug having poor permeability and short half-life. It is given parenterally, which limits its use in patients warranting "at-home care." An oral drug delivery of amikacin is, therefore, imminent. Aim: This work focused on establishing poly d, l-lactide-co-glycolide (PLGA)-based nanoparticles of amikacin with consolidated pharmaceutical attributes capable of circumventing gastrointestinal tract membrane barriers and promoting oral administration of the drug. The partied attributes are suggestive of enhanced uptake of the drug via Peyer's patches overlaying small intestine and support successful oral delivery. Materials and Methods: To have a robust delivery system, a statistical Box–Behnken experimental design was used and formulation parameters such as homogenization time, probe sonication time, and drug/polymer ratio of amikacin-loaded PLGA nanoparticles (A-NPs) for obtaining monodispersed nanoparticles of adequate size and high drug loading were optimized. Results: The model suggested to use the optimum homogenization time, probe sonication time, and drug/polymer ratio as 30s, 120s, and 1:10, respectively. Under these formulation conditions, the particle size was found to be 260.3nm and the drug loading was 3.645%. Conclusion: Biodegradable PLGA nanoparticulate systems with high payload, optimum size, and low polydispersity index will ensure successful uptake and ultimately leading to better bioavailability. Hence, under the aforementioned optimized conditions, the A-NPs prepared had particle size of 260.3nm, which is appreciable for its permeability across small intestine, and drug loading of 3.645%. [ABSTRACT FROM AUTHOR]

Introduction: Melanoma is the most serious form of skin cancer causing most of the skin cancer-related deaths. The incidence of melanoma has risen so dramatically over past few years that no other solid or blood malignancy comes close to it in terms of increased incidence. The main problem associated with the treatment of melanoma is low response rate to the existing treatment modalities, which in turn is due to the incomplete response by chemotherapeutic agents and inherent resistance of melanoma cells.Materials and Methods: Conventional therapeutic strategies, as well as, recent literature on melanoma have been thoroughly studied. This review summarizes the base of anti-melanoma treatment with conventional chemotherapeutic drugs, followed by an account of recent studies which explored the potential of nanotechnology and newer strategies and agents in melanoma treatment.Conclusion: Although melanoma is curable if detected in its early localized form, metastatic melanoma continues to be a therapeutic challenge. Metastatic melanoma has a very poor prognosis and conventional therapies have not improved the outcomes of the treatment so far. For this reason, newer combinations of anti-melanoma drugs and newer strategies utilizing nanotechnology have been constantly explored. [ABSTRACT FROM AUTHOR]

The present study was conducted for the optimization of transethosomes formulation for dermal fisetin delivery. The optimization of the formulation was carried out using "Box-Behnken design". The independent variables were Lipoid S 100, ethanol and sodium cholate. The prepared formulations were characterized for vesicle size, entrapment efficiency and in vitro skin penetration study. The vesicles-skin interaction, confocal laser scanning microscopy and dermatokinetic studies were performed with optimized formulation. Results of the present study demonstrated that the optimized formulation presented vesicle size of 74.21 ± 2.65 nm, zeta potential of −11.0 mV, entrapment efficiency of 68.31 ± 1.48% and flux of 4.13 ± 0.17 µg/cm2/h. The TEM image of optimized formulation exhibited sealed and spherical shape vesicles. Results of thermoanalytical techniques demonstrated that the prepared transethosomes vesicles formulation had fluidized the rigid membrane of rat's skin for smoother penetration of fisetin transethosomes. The confocal study results presented well distribution and penetration of Rhodamine B loaded transethosomes vesicles formulation up to deeper layers of the rat's skin as compared to the Rhodamine B-hydro alcoholic solution. Present study data revealed that the developed transethosomes vesicles formulation was found to be a potentially useful drug carrier for fisetin dermal delivery. [ABSTRACT FROM AUTHOR]

The study reports a rapid and short analytical technique for separation, characterization, and quantitation along with comparative pharmacological effect of curcuminoids in cerebral ischemia. Flash chromatography, using silica and diol columns along with gradient mobile phase, was utilized to separate three curcuminoids, i.e., curcumin (Cur), demethoxycurcumin (DMC), and bisdemethoxycurcumin (BDMC) for the first time. The separated peaks were monitored at 200–360 nm, whereas the purity of compounds (96.2–97.6%) was determined through qualitative analysis such as infrared and 1H and 13C-nuclear magnetic resonance spectroscopy, mass spectrometry (MS), and differential scanning calorimetry. Furthermore, chitosan nanoparticles (CS-NPs) for curcuminoids were prepared and characterized through zeta sizer, zeta potential, scanning electron microscopy, and transmission electron microscopy. The developed ultra performance of liquid chromatography-electrospray ionization-quadrupole-time of flight-mass spectrometry/mass spectrometry (UPLC-ESI-Q-TOF-MS/MS) method showed simplified automation and shorter run time for Combi flash over conventional separation techniques. The CS-NPs for all the three curcuminoids and combined-curcuminoids (CCr) (combined and administered together for a synergistic effect), following intranasal administration in middle cerebral artery–occluded rats were evaluated for grip strength, locomotor activity, and histopathological examination where the anti-ischemic activity was observed, in terms of potency, for all three CS-NPs and CCr as CCr>Cur>DMC>>BDMC. Cur-CS-NPs exhibited more potency among Cur, DMC, and BDMC, whereas CCr was the more potent anti-ischemic drug compared to Cur, DMC, and BDMC. For Cur the characteristic activity is proposed because of the presence of methoxy group on the phenyl ring whereas for CCr it is synergistic effect of curcuminoids. [ABSTRACT FROM AUTHOR]

Efficient drug delivery at vaginal cavity is often a challenge owing to its peculiar physiological variations including vast differences in pH. Keeping in view this attribute of the target site, the current work was aimed at developing formulation strategies which could overcome this and successfully deliver molecules like itraconazole through SLNs. Optimized SLNs with the given composition was selected for further development into mucoadhesive and thermosensitive gel. Stearic acid and Compritol 888 (1:1, w/w ratio) as lipid, a mixture of 3% Poloxomer 188 and 0.5% sodium taurocholate as surfactant and organic to aqueous ratio of 10:50 was taken. Carbopol 934 and Pluronic F 127 were taken for the development of gel. Optimized gel exhibited a desired gelling temperature (35 °C); viscosity (0.920 PaS) and appreciablein vitrodrug release (62.2% in 20 h). MTT assay did not show any cytotoxic effect of the gel. When evaluatedin vivo,it did not exhibit any irritation potential despite appreciable bioadhesion. A remarkable decrease in CFUs was also observed in comparison with control and marketed formulation when evaluated in rat infection model. Thus, the proposed study defines the challenges for developing a suitable formulation system overcoming the delivery barriers of the vaginal site. [ABSTRACT FROM PUBLISHER]

Topotecan (TPT) is indicated against a variety of solid tumors, but has restricted clinical use owing to associated pharmaceutical caveats. This study is focused at formulating a successful TPT PLGA nanosystem which ameliorates the rapid conversion of active lactone form of drug to its inactive carboxylate form and consequently improvises its efficacy. TPT PLGA nanoparticles were formulated by a double emulsion-solvent evaporation technique with sequential optimization to obtain desired particle size, PDI, zeta potential, and entrapment efficiency. Stability of TPT was ensured by maintaining an acidic pH in the drug-containing phase and the system was evaluated forin vitro–in vivoperformance including cytotoxic potency. The optimized nanosystem had a particle size of 187.33 ± 7.50 nm, a PDI of 0.179 ± 0.05, and an entrapment efficiency of 56 ± 1.2%. Low pH in the interior of nanoparticles stabilized the drug to remain in its active lactone form and revealed a biphasic release pattern till 15 d. Additionally, anin vitrocytotoxicity testing as well asin vivoantitumor efficacy demonstrated a significant potential of higher proliferation inhibition as compared with neat drug (TPT). Thus, the investigation summarized an innovative simple tool for developing stable TPT NPs for effective delivery for treating solid tumors. [ABSTRACT FROM PUBLISHER]

Objective: The present work aims to develop and validate stability indicating a novel liquid chromatography method with applicability i.e. to study the pharmacokinetics factor as well as estimate Tamoxifen (TMX) in bio-analytes, using Ultra High Pressure Liquid Chromatography/ Mass Spectrometry (UPLC-ESI-Q-TOF-MS/MS) in plasma. Methods: A bioanalytical method based on UPLC-ESI-Q-TOF-MS/MS has been developed and validated for the quantitative determination of TMX in female mice plasma using Clomiphine as an Internal Standard (IS). After Liquid-liquid extraction (LLE), analyte and IS, chromatographic separation was achieved on ACQUITY UPLC BEH C18 Waters column with dimensions; 100 mm x 2.1 mm; 1.7 µm, isocratic mobile phase (Acetonitrile:2 mM ammonium formate: 90:10; v/v), and a flow rate of 0.25 mL min-1. Results: The transitions occurred at m/z 372.1→178.1 and m/z 407.1 → 100.1 for TMX and IS, respectively. Liquidliquid extraction technique (LLE) using ethyl acetate was applied in order to optimize the recovery of analytes in mice plasma. The run and retention time of TMX were 6.0 and 2.63 minutes, respectively while the linear dynamic range established was 1.002-4001.07 ng/ml (r²>0.998 ± 0.0003). Intra-assay and inter-assay accuracy (% RSD) was found in the range; 2.43- 3.49. Conclusion: The proposed LC--MS/MS assay method is simple, rapid and sensitive for the determination of TMX in mice plasma for pharmacokinetic studies. Analytes were stable under various conditions i.e. autosampler, freeze--thaw, at room temperature, and under deep freeze conditions. [ABSTRACT FROM AUTHOR]

Stroke is a one of the leading causes of disease and deaths worldwide, which causes irreversible deterioration of the central nervous system. Curcuminoids are reported to have a potential role in the amelioration of cerebral ischemia but they exhibit low serum and tissue levels due to low solubility and poor absorption. Curcumin (CUR), demethoxycurcumin (DMC) and bisdemethoxycurcumin (BDMC)-loaded PNIPAM nanoparticles (NPs) were prepared by free radical polymerization and characterized for particles size, entrapment efficiency, zeta potential,in vitrorelease andex vivopermeation study. Optimized CUR, DMC and BDMC-loaded NPs had the mean size of 92.46 ± 2.8, 91.23 ± 4.2 and 94.28 ± 1.91 nm; zeta potential of −16.2 ± 1.42, −15.6 ± 1.33 and −16.6 ± 1.21 mV; loading capacity of 39.31 ± 3.7, 38.91 ± 3.6 and 40.61 ± 3.6% and entrapment efficiency of 84.63 ± 4.2, 84.71 ± 3.99 and 85.73 ± 4.31%, respectively. Ultra-performance liquid chromatography/electrospray ionization quadrupole time-of-flight mass spectroscopy based bioanalytical method was developed and validated for pharmacokinetics, biodistribution, brain-targeting efficiency and brain drug-targeting potential studies post-intranasal (i.n.) administration which showed enhanced bioavailability of curcuminoids in brain as compared to intravenous administration. Improved neurobehavioural activity (locomotor and grip strength) and reduced cytokines levels (TNF-α and IL-1β) was observed in middle cerebral artery occlusion induced cerebral ischemic rats after i.n. administration of curcuminoids NPs. Finally, the toxicity study was performed which revealed safe nature of developed NPs. [ABSTRACT FROM AUTHOR]

The current investigation aims to present a novel solid lipid-based nanoparticulate system of resveratrol (RV) for the effective treatment of liver cirrhosis. A simplified solvent injection method was employed and the Box–Behnken experimental design was applied for optimization to get a window particle size of 150–200 nm having maximum entrapment efficiency as well as % release. Optimized resveratrol solid lipid nanoparticles (RV-SLNs) (SR-1) of appropriate characteristics (particle size = 191.1 ± 10.44 nm; zeta potential= −13.56 ± 4.14 mV; entrapment efficiency = 75.23 ± 3.85%; maximum % release = 80.53 ± 3.99%) were produced. Differential scanning calorimetry and X-ray diffraction studies were carried out which collectively proved the reduced crystallinity and stability enhancing the effect of the SLNs. Improved drug stability was further established by the appreciable shelf-life of the formulation from International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use (ICH)-recommended accelerated stability studies.In vivostudies revealed nearly five-fold increase in the bioavailability of SR-1 (AUC0→∞=3411 ± 170.34 µg/ml/h) as compared to RV suspension (AUC0→∞=653.5 ± 30.10 µg/ml/h). Pharmacodynamic data exhibited a significant decrease in the serum biomarker enzymes (serum glutamic oxalo-acetic transaminase (SGOT), serum glutamic pyruvic transaminase (SGPT) and alkaline phosphatase) after oral administration of RV-SLNs as compared to control and marketed (SILYBON®) formulations against paracetamol-induced liver cirrhosis. The effect of the treatment was confirmed by the histopathology of the liver microtome sections. Finally, reverse transcriptase-polymerase chain reaction studies were conducted on isolated liver mRNA from SR-1 treated animals and significant down-regulation of tissue inhibitor of metalloproteinases-1 and nuclear factor-kB was witnessed. [ABSTRACT FROM PUBLISHER]

A receptor level interaction of etoposide with P-glycoprotein (P-gp) and subsequent intestinal efflux has an adverse effect on its oral absorption. The present work is aimed to enhance the bioavailability of etoposide by co-administering it with quercetin (a P-gp inhibitor) in dual-loaded polymeric nanoparticle formulation. Poly-lactic-co-glycolic acid (PLGA) nanoparticles were optimized for various parameters like o/w phase volume ratio, poly-vinyl alcohol concentration, PLGA concentration and sonication time. The cytotoxicity studies (MTT assay) revealed a 9- and 11-fold decrease in the IC 50 values for etoposide-loaded nanoparticles (ENP) and etoposide + quercetin dual-loaded nanoparticles (EQNP) when compared to that of free etoposide, respectively, and the results were further supported by florescent-activated cell sorter studies. The confocal imaging of the intestinal sections treated with ENP and EQNP containing fluorescent probe (rhodamine) showed the superiority of the EQNP to permeate deeper. Furthermore, pharmacokinetic studies on rats revealed that EQNP exhibited a 2.4-fold increase in bioavailability of etoposide than ENP with no quercetin. The developed loaded nanoparticles have the high potential to enhance the bioavailability of the etoposide and sensitize the resistant cells. [ABSTRACT FROM AUTHOR]

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 4e6 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. [ABSTRACT FROM AUTHOR]

The present work is aimed to develop a simple, sensitive, robust and reliable HPLC method for the estimation of irinotecan in the physiological media in order to assess the permeability profile of irinotecan, using the everted gut sac, in the presence of various P-gp modulators. Separation was achieved using, C18 column with mobile phase consisting of acetonitrile and 0.045 µM sodium dihydrogen phosphate dihydrate buffer containing ion pair agent heptane sulphonic acid sodium salt (0.0054 µM), pH 3. The fow rate was maintained at 1 ml/min and analysis was performed at 254.9 nm using PDA detector. Calibration data showed an excellent linear relationship between peak-area verses drug concentration (r², 0.9999). Linearity was found to be in the range of 0.060-10.0 µg/ml. Limits of detection and quantifcation were found to ~0.020 µg/ml and ~0.060 µg/ml, respectively. The developed method was found to be precise (RSD <1.5%, for repeatability and <2.55% for intermediate precision, acceptable ranges of precision), accurate (The recovered content of irinotecan in the presence of various P-gp modulators varied from 96.11-101.51%, within acceptable range, 80-120%), specifc and robust (% RSD <2). Developed method has been applied successfully for the evaluation of eleven P-gp modulators from diverse chemical class. [ABSTRACT FROM AUTHOR]

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 F254 plates (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-1 and 40-800 ng spot-1 for 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-1 and ≈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 vitro drug release profile and stability assessment of dual drug loaded PLGA nanoparticles (NPs). [ABSTRACT FROM AUTHOR]

An ultra high performance liquid chromatography-electrospray ionization-synapt mass spectrometric method (UHPLC/ESI-QTOF-MS/MS) for the analysis of curcumin (Cur), demethoxycurcumin (DMC), bisdemethoxycurcumin (BDMC) in Wistar rat brain homogenate was developed and validated. The chromatographic separation was achieved on a Waters ACQUITY UPLC™ BEH C18 (2.1mm × 100 mm; 1.7μm) column using isocratic mobile phase, consisting of acetonitrile: 10mM ammonium formate: formic acid (90:10:0.05 v/v/v), at a flow rate of 0.2 ml min-1. The transitions occurred at m/z 367.0694/217.0598, 337.0717/173.0910, 307.0760/187.0844 for Cur, DMC, BDMC and m/z 307.0344/229.0677 for the IS (Nimesulide) respectively. The recovery of the analytes from Wistar rat brain homogenate was optimized using liquid-liquid extraction technique (LLE) in (ethyl acetate: chloform) mixture. The total run time was 3.0 min and the elution of Cur, DMC, BDMC occurred at 1.6, 1.75, 1.70 min, and for the IS 1.87 min, respectively. The linear dynamic range was established over the concentration range of 1.00 ng mL-1 to 1000.0 ng mL-1(r2; 0.9909 ± 0.0011, 0.9911 ± 0.003, and 0.9919 ± 0.0013) for Cur, DMC, and BDMC, respectively. The intra and inter-assay accuracy in terms of % CV for Cur, DMC, and BDMC was in the range 0.47-2.20, 0.47-1.65, and0.44-2.70, respectively. The lower limit of detection (LOD) and quantitation (LOQ) for Cur, DMC, and BDMC were 0.46, 0.05, 0.16 ng mL-1 and 0.153, 0.015, 0.052 ng mL-1, respectively. Analytes were stable and the method proved to be accurate (recovery, >85%), specific and was applied to evaluate the Cur, DMC, BDMC loaded PNIPAM NPs as vehicles for nose to brain drug delivery. Copyright © 2013 John Wiley & Sons, Ltd. [ABSTRACT FROM AUTHOR]

Oxidative stress and inflammatory damage play an important role in cerebral ischemic pathogenesis and may represent a target for treatment. The development of new strategies for enhancing drug delivery to the brain is of great importance in diagnostics and therapeutics of central nervous diseases. The present study examined the hypothesis that intranasal delivery of nanoformulation of curcuminoids would reduce oxidative stress-associated brain injury after middle cerebral artery occlusion (MCAO). The rats were subjected to 2 h of MCAO followed by 22 h reperfusion, after which the grip strength, locomotor activity was performed. The effects of treatment in the rats were assessed by grip strength, locomotor activity and biochemical studies (glutathione peroxidase, glutathione reductase, lipid peroxidation, superoxide dismutase, and catalase) in the brain. Pretreatment with polymeric N-isopropyl acryl amide (PNIPAM) nanoparticles formulation of all three curcuminoids (curcumin (Cur), demethoxycurcumin (DMC), and bisdemethoxycurcumin (BDMC)) at doses (100 μg/kg body weight) given intranasally was effective in bringing significant changes on all the parameters. While nanoformulation of curcumin at a dose of 100 μg/kg body weight was most active in the treatment of cerebral ischemia as compared to others nanoformulation of curcuminoids. The potency of antioxidant activity significantly decreased in the order of PNIPAM nanoformulation of Cur > DMC >> BDMC, thus suggesting the critical role of methoxy groups on the phenyl ring. [ABSTRACT FROM AUTHOR]

A sensitive, selective, precise, and stability-indicating, high-performance, thin-layer chromatographic (HPTLC) method for analysis of sertraline, both as a bulk drug and in house formulation, was developed and validated. The method employed thin-layer chromatographic (TLC) aluminium plates precoated with silica gel 60F-254 as the stationary phase. The solvent system consisted of Toulene/Ethyl acetate/Ammonia (1:5:0.1, v/v) as a mobile phase. The densitometric analysis were carried out at 273 nm using Camag TLC scanner which generated compact spots for SRT (Rf = 0.70 ± 0.02). The linear regression data for the calibration plots showed good linear relationship with r2 = 0.998 in the concentration range of 25–2000 ng spot−1. Sertraline was subjected to acid and alkali hydrolysis, oxidation, photodegradation, and dry heat treatment. Also, the degraded products were well separated from the pure drug. The method was validated for precision, accuracy, ruggedness, and recovery. As the method could effectively separate the drug from its degradation products, it can be employed as a stability indicating one. Moreover, the proposed HPTLC method was utilized to investigate the kinetics of acid and base degradation process. [ABSTRACT FROM AUTHOR]

The oral delivery of hydrophobic drug presents a major challenge because of the low aqueous solubility of such compounds. Self-emulsifying/microemulsifying drug delivery system (SEDDS/SMEDDS), which are isotropic mixtures of oils, surfactants, solvents and co-solvents/surfactants, can be used for the design of formulations in order to improve the oral absorption of highly lipophilic drug compounds. The efficiency of oral absorption of said drug from such type of formulation depends on many formulation-related parameters, such as surfactant concentration, oil/surfactant ratio, polarity of the emulsion, droplet size and charge, all of which in essence determine the self-emulsification ability. Thus, only very specific pharmaceutical excipient combinations will lead to efficient self-emulsifying systems. With the growing interest in this field, there is an increasing need for guidelines in excipient selection to obtain effective delivery system with improved bioavailability. The aim of this review is to present the recent approaches in selecting the most appropriate lipid system(s); methods for its characterization and role of various excipients for improved delivery of dosage form. [ABSTRACT FROM AUTHOR]

A rapid, simple, sensitive, selective, precise and robust thin-layer chromatography densitometric method for the determination of free sterols in leech was developed and validated on silica gel layer using carbon tetrachloride–methanol–formic acid (9.5:1.5:0.55, v/v/v). Spectrodensitometric scanning was carried using a Camag TLC scanner III at 366 nm after spraying 2% methanolic sulphuric acid, which gave compact spots for cholesterol (RF = 0.35 ± 0.02). The regression analysis data for calibration plot implied a good linear relationship (r2 = 0.99958) between response and concentration over the range 100–600 ng per spot with respect to peak area. The limits of detection and quantification were found to be 13.8 ± 0.51 and 45.01 ± 1.29 ng per spot, respectively. Validation was in accordance to the International Conference on Harmonization guidelines. Cholesterol was subjected to forced stress conditions of oxidation, hydrolysis and heat. Degradation products resulting from the forced stress did not interfere with detection because the degradant peaks were well separated from the cholesterol peak. The densitometric method can be regarded as stability-indicating and can be used for quality control assay of cholesterol in leech extract. [ABSTRACT FROM PUBLISHER]

CD44 or hyaluronan receptor is a transmembrane receptor associated with aggressive tumour growth, proliferation, and metastasis. In normal physiology, this receptor has a crucial role in cell adhesion, inflammation, and repair processes. However, many tumour cells over-express this receptor and abuse it to become progressive and perpetual units. The article comments from common functioning of the CD44 receptor, to its diabolic multi-dimensional effects in promotion of malignant cells. It also illuminates the relations of CD44 endorsed processes with other biomolecular events in cancer progression. In an end, the review focuses comprehensively at ongoing researches to exploit the CD44 over-expression as a probable target in treatment, management, and diagnosis of malignancy. [ABSTRACT FROM AUTHOR]