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Development of a biodegradable nanoplatform poly(lactic-co-glycolic acid) (PLGA) for co-delivery of two drugs is hugely imperative and beneficial in anticancer therapeutics. In this study, co-deliv...

In last two decades, the lipid nanocarriers have been extensively investigated for their drug targeting efficiency towards the critical areas of the human body like CNS, cardiac region, tumor cells, etc. Owing to the flexibility and biocompatibility, the lipid-based nanocarriers, including nanoemulsion, liposomes, SLN, NLC etc. have gained much attention among various other nanocarrier systems for brain targeting of bioactives. Across different lipid nanocarriers, NLC remains to be the safest, stable, biocompatible and cost-effective drug carrier system with high encapsulation efficiency. Drug delivery to the brain always remains a challenging issue for scientists due to the complex structure and various barrier mechanisms surrounding the brain. The application of a suitable nanocarrier system and the use of any alternative route of drug administration like nose-to-brain drug delivery could overcome the hurdle and improves the therapeutic efficiency of CNS acting drugs thereof. NLC, a second-generation lipid nanocarrier, upsurges the drug permeation across the BBB due to its unique structural properties. The biocompatible lipid matrix and nano-size make it an ideal drug carrier for brain targeting. It offers many advantages over other drug carrier systems, including ease of manufacturing and scale-up to industrial level, higher drug targeting, high drug loading, control drug release, compatibility with a wide range of drug substances, non-toxic and non-irritant behavior. This review highlights recent progresses towards the development of NLC for brain targeting of bioactives with particular reference to its surface modifications, formulations aspects, pharmacokinetic behavior and efficacy towards the treatment of various neurological disorders like AD, PD, schizophrenia, epilepsy, brain cancer, CNS infection (viral and fungal), multiple sclerosis, cerebral ischemia, and cerebral malaria. This work describes in detail the role and application of NLC, along with its different fabrication techniques and associated limitations. Specific emphasis is given to compile a summary and graphical data on the area explored by scientists and researchers worldwide towards the treatment of neurological disorders with or without NLC. The article also highlights a brief insight into two prime approaches for brain targeting, including drug delivery across BBB and direct nose-to-brain drug delivery along with the current global status of specific neurological disorders.

The proposed study involves delivering drug/bioactive using a single nanoplatform based on poly lactic-co-glycolic acid (PLGA) for better efficacy, synergistic effect, and reduced toxicity. PLGA was conjugated to doxorubicin (D1), and this conjugate was used for encapsulation of naringenin (D2) to develop naringenin loaded PLGA-doxorubicin nanoparticles (PDNG). The PDNG NPs were 165.4 ± 4.27 nm in size, having 0.112 ± 0.035 PDI, with -10.1 ± 2.74 zeta potential. The surface morphology was confirmed through transmission electron microscopy (TEM) and atomic force microscopy (AFM). The in vitro studies revealed that PDNG NPs exhibited selective anticancer potential in breast cancer cells, and induced apoptosis with S-phase inhibition via an increase in intrinsic reactive oxygen species (ROS) and altering the mitochondrial potential. The results also signified the efficient uptake of nanoparticles encapsulated drugs by cells besides elevating the caspase level suggesting programmed cell death induction upon treatment. In vivo studies results revealed better half-life (27.35 ± 1.58 and 11.98 ± 1.21 h for doxorubicin and naringenin) with higher plasma drug concentration. In vivo biodistribution study was also in accordance with the in vitro studies and in line with the in vivo pharmacokinetic. In vivo tumor regression assay portrayed that the formulation PDNG halts the tumor growth and lessen the tumor volume with the stable bodyweight of the mice. Conclusively, the dual delivery approach was beneficial and highly effective against tumor-induced mice.

Anemia is the most common hematological abnormality of chemotherapy, which is responsible for poor clinical outcomes. To overcome this complication, the present study was aimed for developing a Eudragit/polylactic-co-glycolic acid (PLGA) based nanoparticulate system for a model drug paclitaxel (PTX). The study was planned using a simplex lattice mixture design. PTX nanoparticles (PTXNp) were evaluated in vitro for physicochemical properties, hemolytic effects and cytotoxic effects. Further, the nanoparticles were subjected to in vivo screening using rats for hemocompatibility, pharmacokinetic profile, and biodistribution to the vital organs. The PTXNps were 65.77–214.73 nm in size, showed more than 60% sustained drug release in 360 h and caused less than 8% hemolysis. The parameters like red blood cell count, activated partial thromboplastin time (aPTT), prothrombin time (PT) and C3 complement were similar to the negative control. Cytotoxicity results suggested that all the PTXNp demonstrated drug concentration-dependent cytotoxicity. The in vivo pharmacokinetic study concluded that PTXNp formulations had significantly higher blood AUC (93.194.55–163,071.15 h*ng/mL), longer half-lives (5.80–6.35 h) and extended mean residence times (6.05–8.54 h) in comparison to PTX solution (p

The unending outburst of COVID-19 has reinforced the necessity of SARS-CoV-2 identification approaches for the prevention of infection transmission and the proper care of severe and critical patients. As there is no cure, a prompt and reliable diagnosis of SARS-CoV2 is vital to counter the spread and to provide adequate care and treatment for the infection. Currently, RT-PCR is a gold standard detection method for the qualitative and quantitative detection of viral nucleic acids. Besides, enzyme-linked immunosorbent assay is also a primarily used method for qualitative estimation of viral load. However, almost all the detection methods have their pros and cons in terms of specificity, accuracy, sensitivity, cost, time consumption, the need for sophisticated laboratories, and the requirement of skilled technical experts to carry out the detection tests. Thus, it is suggested to integrate different techniques to enhance the detection efficiency and accurateness for SARS-CoV2. This review focuses on preliminary, pre-confirmatory, and confirmatory methods of detection such as imaging techniques (chest-X-ray and chest- computed tomography), nucleic acid detection methods, serological assay methods, and viral culture and identification methods that are currently being employed to detect the presence of SARS-CoV-2 infection along with recent detection method and applicability for COVID-19.

Lower generation PAMAM dendrimers have an immense potential for drug delivery with lower toxicity, but these dendrimers yet need certain basic ameliorations. In this study, the brain delivery potential of the synthesized PAMAM-Lf (lower generation PAMAM and lactoferrin conjugate) loaded with memantine (MEM) was explored and evaluated in vitro and in vivo in the disease-induced mouse model. The developed nanoscaffolds were characterized for size, zeta potential and in vitro release. Increase in the average size from 11.54 ± 0.91 to 131.72 ± 4.73 nm, respectively, was observed for drug-loaded PAMAM (i.e., PAMAM-MEM) and PAMAM-Lf (i.e., MEM-PAMAM-Lf). Release profile of MEM from MEM-PAMAM-Lf was slow and sustained up to 48 h. In vivo biodistribution in the Sprague-Dawley rat model revealed that the brain uptake of MEM-PAMAM-Lf was significantly higher than that of MEM alone. The behavioral response study in the healthy rats did not result in any significant changes. The in vivo study in an AlCl

Presently, nanotechnology appears as a powerful and innovative tool in the medical field. It has various advantages over the conventional drug therapy such as therapeutic specificity, has less side effects, reduces dose of drug, has more precise treatment and can access the inaccessible areas of the body like brain, tumor cells, etc. The human brain is the most complicated part of the body which is highly protected with the blood-brain barrier (BBB) and the other protective measures of the body. The available treatments for brain disorder are highly invasive (parenteral or surgical procedures) in nature or cause high peripheral toxicity (oral administration). Thus, a prominent strategy is needed which can easily approach the brain and offers a more specific treatment. Nanomedicines are effective tools used for the diagnosis and treatment of brain disorders. Key words: Brain, neurodegenerative disorders, nanotechnology, gold nanoparticle, quantum dots.

In the last few years, the stem cell therapy has gained much popularity among researchers and scientists of biomedical field. It became an effective and alternative approach for the treatment of various physiological conditions (like accidental injuries, burn damage, organ failure, bone marrow transfusion, etc.) and chronic disorders (diabetes, cancer, neurodegenerative disorders, periodontal diseases, etc.). Due to the unique ability of cellular differentiation and regeneration, stem cell therapy serves as the last hope for various incurable conditions and severe damages. The amalgamation of stem cell therapy with nanotechnology brings new prospects to the stem cell research, as it improves the specificity of the treatment and controls the stem cell proliferation and differentiation. In this review article, we have discussed various nanocarrier systems such as carbon nanotubes, quantum dots, nanofibers, nanoparticles, nanodiamonds, nanoparticle scaffold, etc. utilized for the delivery of stem cell inside the body.

Diabetes and its complications are a significant health concern throughout the globe. There are physiological differences in the mechanism of type-I and type-II diabetes and the conventional drug therapy as well as insulin administration seem to be insufficient to address the problem at large successfully. Hypoglycemic swings, frequent dose adjustments and resistance to the drug are major problems associated with drug therapy. Cellular approaches through stem cell based therapeutic interventions offer a promising solution to the problem. The need for pancreatic transplants in case of Type- I diabetes can also be by-passed/reduced due to the formation of insulin producing β cells via stem cells. Embryonic Stem Cells (ESCs) and induced Pluripotent Stem Cells (iPSCs), successfully used for generating insulin producing β cells. Although many experiments have shown promising results with stem cells in vitro, their clinical testing still needs more exploration. The review attempts to bring into light the clinical studies favoring the transplantation of stem cells in diabetic patients with an objective of improving insulin secretion and improving degeneration of different tissues in response to diabetes. It also focuses on the problems associated with successful implementation of the technique and possible directions for future research.

Tissue engineering is a multi-disciplinary field such as material science, life science, and bioengineering that are necessary to make artificial tissue or rejuvenate damaged tissue. Numerous tissue repair techniques and substitute now exist even though it has several shortcomings; these shortcomings give a good reason for the continuous research for more acceptable tissue-engineered substitutes. The search for and use of a suitable stem cell in tissue engineering is a promising concept. Stem cells have a distinctive capability to differentiate and self-renew that make more suitable for cell-based therapies in tissue repair and regeneration. This review article focuses on stem cell for tissue engineering and their methods of manufacture with their application in nerve, bone, skin, cartilage, bladder, cardiac, liver tissue repair and regeneration.

Bortezomib (BTZ) is a proteasome inhibitor as approved by US FDA for the treatment of multiple myeloma. It exhibits significant anti-cancer properties, against solid tumors; but lacks aqueous solubility, chemical stability which hinders its successful formulation development. The present study is an attempt to deliver BTZ using N-(2-hydroxypropyl) methacrylamide (HPMA) based copolymeric conjugates and biotinylated PNPs in an effective manner. Study describes a systematic synthetic pathway to synthesize functional polymeric conjugates such as HPMA-Biotin (HP-BT) HPMA-Polylactic acid (HPLA) and HPMA-PLA-Biotin (HPLA-BT) followed by exhaustive characterization both spectroscopically and microscopically. Our strategy yielded polymeric nanoparticles (PNPs) of narrow size range of 199.7 ± 1.32 nm. Release studies were performed at pH 7.4 and 5.6. PNPs were 2-folds less hemolytic (p < 0.0001) than pure drug. BTZ loaded PNPs of HPLA-BT demonstrated significant anti-cancer activity against MCF-7 cells. IC50 value of these PNPs was 56.06 ± 0.12 nM, which was approximately two folds less than BTZ (p < 0.0001). Cellular uptake study confirmed that higher uptake of formulations might be an outcome of biotin surface tethering characteristics that enhanced selectivity and targeting of formulations efficiently. In vivo pharmacokinetics evidenced increased bioavailability (AUC0 t-∞) of DL-HPLA-BT PNPs (drug loaded) than BTZ with an improved half-life. Overall the developed PNPs led to the improved and effective BTZ delivery.

Psoriasis is a consistently recurring, inflammatory, autoimmune disorder of the skin, affecting about 2-5% of the world population. Abundant therapeutic agents are accessible for the treatment of psoriasis. Nevertheless, none of them are entirely secure and effective to treat the disease without compromising patient compliance. Furthermore, already existing drugs are supposed to restrain the ailment and alleviate the sign and symptoms with no complete cure. However, they focus on restraining the disease and alleviating the symptoms without providing an absolute cure. Therefore there remains a vital challenge, to explore a new drug moiety or delivery system which could safely and effectively manage psoriasis without compromising patient compliance. Furthermore, conventional formulations offer reduced benefit/risk ratio of anti-psoriatic drugs, which limits the use of existing conventional formulations. Novel formulations based on nanocarriers are a promising prospect to overcome the limitation of conventional formulations by offering a reduction in dose, dosing frequency, dose-dependent, side effects with enhanced efficacy. Presently nano-formulations have gained widespread application for effective and safe treatment of psoriasis. The present review primarily focuses on conventional therapeutic strategy and recent advances in lipid-based, polymer-based and metallic nano-formulations of a variety of anti-psoriatic drugs. The practicability of various nanocarrier systems including liposomes, nanostructured lipid carriers, ethosomes, solid lipid nanoparticles, nanocapsules, micelles, dendrimers, gold nanoparticles and silver nanoparticles have been discussed in detail. The review also traces related patents to exemplify the role of various nanoparticles in psoriasis treatment. In a nutshell, nano-formulations remain established as a promising modality for treating psoriasis treatment as they propose better penetration, targeted delivery, enhanced safety, and efficacy.

Brain is supposed to be the most complicated part of the body which is very far from the reach of drug moieties. The drug entry in to the brain region depends upon various factors, and among those, the blood-brain-barrier remains the most prominent one. This barrier restricts the entry of almost all the drug and most of the essential biological components like proteins, peptides, etc. and hinders treatment of the CNS disorders. Alzheimer Disease (AD) is one such brain disorder, more specifically a neurodegenerative disorder which primarily affects the older adults.From solubility enhancement to targeted delivery, the nanoparticulate system became the answer for almost all the criticality related to drug delivery. Hence, nanoparticulate drug carrier system has been widely utilizing to remove the hurdles of brain drug delivery. Keeping this in mind, we have underlined the proficiencies of the nanocarrier systems which claim to improve the drug efficacy for the treatment of the AD.The nanotechnological approaches are highly exploited by the researchers to enhance the drug permeation across the BBB to improve its bioavailability and efficacy by protecting the drug from peripheral degradation. However, still in this area of drug targeting provides vast scope for discoveries towards the enhancement of drug efficacy through surface modifications, site specification, reduced toxicity of the nanocarrier system and so on.

Diabetes associated oxidative stress and impaired cholinergic neurotransmission causes cognitive deficits. Although phloridzin shows antioxidant- and insulin sensitizing-activities, its ameliorative potential in diabetes-induced memory dysfunction remains unexplored. In the present study, type 2 diabetes (T2D) was induced by streptozotocin (35 mg/kg, intraperitoneal) in rats on ad libitum high-fat diet. Diabetic animals were treated orally with phloridzin (10 and 20 mg/kg) for four weeks. Memory functions were evaluated by passive avoidance test (PAT) and novel object recognition (NOR) test. Brains of rats were subjected to biochemical analysis of glutathione (GSH), brain-derived neurotrophic factor (BDNF), malonaldehyde (MDA) and acetylcholinesterase (AChE). Role of cholinergic system in the effects of phloridzin was evaluated by scopolamine pre-treatment in behavioral studies. While diabetic rats showed a significant decrease in step through latency in PAT, and exploration time and discrimination index in NOR test; a substantial increase in all parameters was observed following phloridzin treatment. Phloridzin reversed abnormal levels of GSH, BDNF, MDA and AChE in the brain of diabetic animals. Moreover, in silico molecular docking study revealed that phloridzin acts as a potent agonist at M1 receptor as compared to acetylcholine. Viewed collectively, reversal of T2D-induced memory impairment by phloridzin might be attributed to upregulation of neurotrophic factors, reduced oxidative stress and increased cholinergic signaling in the brain. Therefore, phloridzin may be a promising molecule in the management of cognitive impairment comorbid with T2D.

In this modern era, with the help of various advanced technologies, medical science has overcome most of the health-related issues successfully. Though, some diseases still remain unresolved due to various physiological barriers. One such condition is Alzheimer; a neurodegenerative disorder characterized by progressive memory impairment, behavioral abnormalities, mood swing and disturbed routine activities of the person suffering from. It is well known to all that the brain is entirely covered by a protective layer commonly known as blood brain barrier (BBB) which is responsible to maintain the homeostasis of brain by restricting the entry of toxic substances, drug molecules, various proteins and peptides, small hydrophilic molecules, large lipophilic substances and so many other peripheral components to protect the brain from any harmful stimuli. This functionally essential structure creates a major hurdle for delivery of any drug into the brain. Still, there are some provisions on BBB which facilitate the entry of useful substances in the brain via specific mechanisms like passive diffusion, receptor-mediated transcytosis, carrier-mediated transcytosis etc. Another important factor for drug transport is the selection of a suitable drug delivery systems like, liposome, which is a novel drug carrier system offering a potential approach to resolving this problem. Its unique phospholipid bilayer structure (similar to physiological membrane) had made it more compatible with the lipoidal layer of BBB and helps the drug to enter the brain. The present review work focused on various surface modifications with functional ligand (like lactoferrin, transferrin etc.) and carrier molecules (such as glutathione, glucose etc.) on the liposomal structure to enhance its brain targeting ability towards the successful treatment of Alzheimer disease.

The effect of Ca2+ ion cross-linker on acryalamide grafted carboxymethyl xanthan gum (CMXG-g-PAAm) on the drug release was investigated. Previously, CMXG was synthesized from XG and further grafted to CMXG-g-PAAm to retard the drug release. Once the CaCl2 solution is added to CMXG-g-PAAm, Ca2+ considerably affected the drug release mechanism mainly by diffusion and erosion. In order to validate the grafted polymer, tablets were prepared using wet granulation and dry granulation methods It has been noticed that the tablets prepared by wet granulation successfully controls the release of the drug over an extended period of time. Moreover, the release profile was aligned to Korsmeyer-Peppas equation and exhibited the drug transport mechanism via diffusion and erosion.

Vincristine is a naturally occurring anticancer drug with a specific mechanism of action, given intravenously/bolus to treat various types of cancers, including breast cancer. The present studies explored the potential of thermosensitive injectable nanogel of vincristine loaded nanoparticles. In situ gel was chosen as the delivery system because it restricts the unwanted exposure in blood and other healthy tissues, thus eliminate hemolytic side effects of the drug and offer easy administration in vivo. Furthermore, non-biodegradable and cytocompatible polymeric Eudragit RSPO nanoparticles are proposed as ideal candidates for biomedical usage. The method of preparation includes two major steps—the first formation of vincristine nanoparticles with positively charged Eudragit RSPO. In the second step, these nanoparticles were suspended into a thermosensitive gel base to act as an in situ nanogel. Characterization parameters performed are size, surface charge, vincristine sulfate release behavior and mechanism, polymer-drug interaction, and encapsulation efficiency. In situ nanogel was also evaluated for gelling time, drug release, hemocompatibility and cytotoxic activity in breast cancer MCF-7 cell lines. The magnitude of size ( Furthermore, VS loaded in situ nanogels possessed less hemolytic activity than the pure drug. Hence, it can be concluded that thermo-receptive in situ nanogel of vincristine can be used to treat breast cancer cells with less hemolytic activity. Further in vivo studies are in progress to establish the effectiveness.

In the present work, an unreported graft copolymer of carboxymethyl xanthan gum and acrylamide has been synthesised by free radical polymerisation in a nitrogen atmosphere using ammonium persulphate as an initiator. The optimum reaction conditions adopted for affording maximum percentage of grafting including its grafting efficiency were obtained by varying the concentration of carboxymethyl xanthan gum from 4 to 24 g dm(-3); ammonium persulphate from 5×10(-4) to 30×10(-4)mol dm(-3); acrylamide from 0.4 to 1.2 mol dm(-3); reaction temperature from 55 to 75°C and reaction time from 30 to 90 min. The synthesised graft copolymer has been characterised by (1)H NMR, FTIR spectroscopy, X-ray diffraction measurement, thermal analysis, viscosity measurement and scanning electron microscopy. However, grafting of acrylamide onto carboxymethyl xanthan gum backbone enhanced its thermal stability. This graft copolymer might be well exploited globally as a potential carrier for drug delivery system.

Stem cells are the specialized cell population with unique self-renewal ability and act as the precursor of all the body cells. Broadly, stem cells are of two types one is embryonic stem cells while the other is adult or somatic stem cells. Embryonic stem cells are the cells of zygote of the blastocyst which give rise to all kind of body cells including embryonic cells, and it can reconstruct a complete organism. While the adult stem cells have limited differentiation ability in comparison with embryonic stem cells and it proliferates into some specific kind of cells. This unique ability of the stem cell makes it a compelling biomedical and therapeutic tool. Stem cells primarily serve as regenerative medicine for particular tissue regeneration or the whole organ regeneration in any physical injury or disease condition (like diabetes, cancer, periodontal disorder, etc.), tissue grafting and plastic surgery, etc. Along with this, it is also used in various preclinical and clinical investigations, biomedical engineering and as a potential diagnostic tool (such as the development of biomarkers) for non-invasive diagnosis of severe disorders. In this review article, we have summarized the application of stem cell as regenerative medicine and in the treatment of various chronic diseases.

To establish a platform for the possibility of effective and safe delivery of Temozolomide (TMZ) to brain via surface engineered (polyamidoamine) PAMAM dendrimer for the treatment of glioblastoma. The present study aims to investigate the efficacy of PAMAM-chitosan conjugate based TMZ nanoformulation (PCT) against gliomas in vitro as well as in vivo. The prepared nanoconjugated formulation was characterized by 1H NMR, FT-IR spectroscopy and for surface morphological parameters. The reported approach was also designed in such a way to ensure toxicity before in vivo delivery through conducting the hemolytic study. Surface morphology was found as per nanoformulation via size, pdi and zeta potential measurement. PCT was more efficacious in terms of IC50 values compared to pure TMZ against U-251 and T-98G glioma cell lines. The in vivo pharmacokinetic parameters proved sustained release fashion such as half-life (t1/2) of 22.74 h (PCT) rather than15.35 h (TMZ) only. Higher concentration was found in heart than brain in bio-distribution studies. This study exhibits the potential applicability of dendrimer and CS in improving the anticancer activity and delivery of TMZ to brain. The attractive ex vivo cytotoxicity against two glioma cell lines; U-251 and T-98G and phase solubility studies of TMZ revealed remarkable results. In vivo studies of prepared nanoformulation were significant and promising that explored the double concentration of TMZ in brain due to surface functionality of dendrimer. The reported work is novel and non- obvious as none of such approaches using chitosan anchored dendrimer for TMZ delivery has been reported earlier.

Primaquine phosphate (PQ) is mainly used as a radical cure therapy to eradicate relapse of malaria at the liver stage, which is particularly caused by P. falciparum and P. vivax. In the present study, PQ-loaded galactosylated gelatin nanoparticles (Gel–LA–PQ–NPs) were formulated using a one-step desolvation technique. The mean particle size of Gel–LA–PQ–NPs was found to be 93.48 ± 6.36 nm with a zeta potential of 4.80 ± 0.20 mV having 69.90 ± 1.53% encapsulation efficiency. Electron microscopy demonstrated that the NPs were spherical in shape and uniformly distributed without any cluster formation. The in vitro release of PQ from Gel–LA–PQ–NPs has been facilitated in sustained manner, and the release was three times slower than the naive drug. The prepared nanoparticles (Gel–LA–PQ–NPs) were significantly (p < 0.0001) less hemolytic than the pure drug PQ. The hematological ex vivo study further supported that the developed Gel–LA–PQ–NPs were safer than PQ. The in vitro antiplasmodium assay revealed that th...

The current review emphasizes on the herbal bioenhancers which themselves do not possess inherent pharmacological activity of their own but when co-administered with Active Pharmaceutical Ingredients (API), enhances their bioavailability and efficacy. Herbal bioenhancers play a crucial role in enhancing the bioavailability and bioefficacy of different classes of drugs, such as antihypertensives, anticancer, antiviral, antitubercular and antifungal drugs at low doses. This paper highlights various natural compounds that can be utilized as an efficient bioenhancer. Several herbal compounds including piperine, quercetin, genistein, naringin, sinomenine, curcumin, and glycyrrhizin have demonstrated capability to improve the pharmacokinetic parameters of several potent API. This article also focuses on various United States patents on herbal bioenhancers, which has proved to be beneficial in improving oral absorption of nutraceuticals like vitamins, minerals, amino acids and certain herbal compounds. The present paper also describes proposed mechanism of action, which mainly includes absorption process, drug metabolism, and action on drug target. The herbal bioenhancers are easily available, safe, free from side effects, minimizes drug toxicity, shortens the duration of treatment, lowers the drug resistance problems and minimizes the cost of treatment. Inspite of the fact that herbal bioenhancers provide an innovative concept for enhancing the bioavailability of several potent drugs, there are numerous bioenhancers of herbal origin that are yet to be explored in several vital areas. These bioenhancers must also be implied to enhance the bioavailability and bioefficacy through routes other than the oral route of drug delivery. There is a vast array of unexploited plants which can be investigated for their drug bioenhancing potency. The toxicity profiles of these herbal bioenhancers must not be overlooked. Researches must be carried out to solve these issues and to deliver a safe and effective dose of drugs to attain desired pharmacological response.

Objectives In this study, we have used melphalan (ML) as a model drug, used extensively for the treatment of breast cancer. Due to its remarkable haemolytic activity, clinical application of this drug is limited. Methods We incorporated the two synthesized PEGylated melphalan conjugates, viz. MLPEG 2000 and MLPEG 5000, separately into the medium molecular weight chitosan (CS)-based smart thermoreversible in-situ forming injectable hydrogel. Prepared hydrogels were evaluated for gelation time, rheological behaviour, drug release and stability. Key findings Although PEGylated melphalan shows significant increase in aqueous solubility and decrease in haemolytic activity, it was loaded to hydrogel to improve dose frequency and local effect. Hydrogel comprising CS (3.22%, w/v) and glycerophosphate disodium salt (GP) (16%, w/v) showed consistent gelation time and retard the release of drug without compromising its stability. To underline the role of GP, conjugates were loaded into CS solution with and without the GP. Remarkably, absence of GP results in rapid initial burst with nearly complete drug release within 50 h, while addition of GP exhibited drug release up to 100 h. Conclusions Thus, this study highlighted the role of CS/GP thermoreversible injectable hydrogel for successful loading of PEGylated melphalan.

Emulgel is an emerging topical drug delivery system to which if more effort is paid towards its formulation & development with more number of topically effective drugs it will prove a boon for derma care & cosmetology. Emulgels are either emulsion of oil in water or water in oil type, which is gelled by mixing it with gelling agent. Incorporation of emulsion into gel increases its stability & makes it a dual control release system. Due to lack of excess oily bases & insoluble excipients, it shows better drug release as compared to other topical drug delivery system. Presence of gel phase makes it a non greasy & favors good patient compliance. These reviews give knowledge about Emulgel including its properties, advantages, formulation considerations, and its recent advances in research field. All factors such as selection of gelling agent, oil agent, emulsifiers influencing the stability and efficacy of Emulgel are discussed. All justifications are described in accordance with the research work carried out by various scientists. These brief reviews on formulation method have been included. Current research works that carried out on Emulgel are also discussed and highlighted the wide utility of Emulgel in topical drug delivery system. After the vast study, it can be concluded that the Emulgels appear better & effective drug delivery system as compared to other topical drug delivery system. The comprehensive analysis of rheological and release properties will provide an insight into the potential usage of Emulgel formulation as drug delivery system.

Application of pharmaceutical nanotechnology (nanomedicines) for plant actives and extracts, is gaining a tremendous growth and interest among the scientists. This emerging herbal revolution has headed towards the development of another approaches for the delivery of poorly soluble herbal bioactives and plant extracts for enhancing their bioavailability and efficacy. In the same context, a majority of pharmaceutical nanotechnologies and targeting strategies including phytosomes, nanoparticles, hydrogels, microspheres, transferosomes and ethosomes, self nano emulsifying drug delivery systems (SNEDDS), self micro emulsifying drug delivery systems (SMEDDS) has been applied for the delivery of bioactives and plant extracts and were identified and explored. These pharmaceutical nanotechnologies have been proven to be the most efficient and reliable delivery systems, as these enhance the solubility, absorption, pharmacokinetics, bioavailability and provide protection from toxicity. Considering these aspects, the present review highlights the present scenario related to the expansion of novel herbal formulations utilizing the nanotechnologies and compilation of their delivery types and mechanism, methodology, loaded drug, drug size, entrapment efficiency of drug, in vivo activity and its application. Moreover, this review article provides an understanding of therapeutic efficacy of the herbal medicines to be loaded into the novel drug delivery system for various biomedical applications.

Transdermal drug delivery system (TDDS) utilizes the skin as executable route for drug administration but the foremost barrier against drug permeability is the stratum corneum and therefore, it limits therapeutic bioavailability of the bioactive. This review focuses on the recent advancements in the TDDS which include iontophoresis, sonophoresis, electroporation, microneedles, magnetophoresis, photomechanical waves and electron beam irradiation. These advancements are exhaustively discussed with techniques involved with their beneficial claims for different categories of bioactive. However, a lot of research has been carried out in TDDS, still the system has many pros and cons such as inconsistent drug release, prevention of burst release formulation and problems related to toxicity. In addition to that, to exploit the TDDS more efficiently scientists have worked on some combinational approaches for manufacturing TDDS viz., chemical-iontophoresis, chemical-electroporation, chemical-ultrasound, iontophoresis-ultrasound, electroporation-iontophoresis electroporation-ultrasound and pressure waves-chemicals and reported the synergistic effect of the same for safe, effective and practical use of TDDS. The present article covers all the above-mentioned aspects in detail and hence the article will assuredly serve as an enlightening tool for the visionaries working in the concerned area.

Traditional medicines that formed the basis of health care throughout the world since the earliest days of mankind are still widely used and have considerable importance in international trade. Recognition of their clinical, pharmaceutical, and economic value is still growing, although this varies widely between countries and therefore regulation of exploitation and exportation is essential, together with international cooperation and coordination for their conservation so as to ensure their availability for the future. World Health Organization and European Union issued the guidelines defined the basic criteria for the evaluation of quality, safety, and efficacy of herbal medicines with the goal of assisting national regulatory authorities, scientific organizations, and manufacturers in assessing documentation, submissions, and dossiers in respect of such products. Legislative controls in respect of medicinal plants have not evolved around a structured control model. There are different ways in which countries define medicinal plants or herbs or products derived from them. The present review highlights the status of different countries adopted various approaches to licensing, dispensing, manufacturing, and trading to ensure their safety, quality, and efficacy.

The oral route is most preferred one as there is ease of administration and it is a painless approach. This favored route is restricted to those drug molecules that are absorbent over gastric mucosa. One of the promising techniques is SMEDDS. Self-micro emulsifying drug delivery system has gained more attention due to enhanced oral bioavailability enabling a reduction in dose, more consistent temporal profiles of drug absorption, selective targeting of drug towards specific absorption window in GIT, and protection of drugs from the unreceptive environment in the gut. SMEDDS provide the dissolved drugs form, and also its small size of droplets imparts substantial interfacial area for the absorption of drugs. It can simply get penetrated into the GIT which is the major advantages over another emulsion. The present study is performed for the motivation of the graduates towards publication and research. Hence, we have encouraged the graduates to prepare an informative article on the present subject

Targeting of drug to the colon oral route the drug release is controlled by the gastrointestinal pH, transit times and intestinal flora. Metronidazole is only used antibiotics, which can be used, in colonic disease. Matrix formulations containing various proportions of Xanthan gum and HPMC E5LV were prepared by wet granulation technique using 10% starch paste. Six Matrix tablet formulation (1 to 6) of Metronidazole were prepared different mixture of Xanthan gum and HPMC-E5LV. All the formulations were evaluated for in-process quality control tests. The in-vitro drug release study first in 0.1N HCl followed by in pH 7.4 phosphate buffer, the formulation F3 show good drug release in control manner. Hence, synthetic polymer such as HPMCE5LV is most cheap and suitable for colonic drug delivery.

The transdermal drug delivery systems (TDDS) are drug delivery system that gives rapid, the immediate therapeutic effect of the drug across the patient's skin and its different layers. They are also called as patches. More than 75% of the drugs, now a day's, are taken orally and are not very much effective. To overcome these problems, the transdermal drug delivery system has been evolved. The advantage of transdermal patches is that they deliver the drugs for better systemic effects at a controlled and a predetermined rate. This drug delivery system also endorses the controlled release of drug medicament into the skin of the patients. The chief aim of this drug delivery system is to deliver the drug contents into the systemic circulation through the permeation of skin at a predetermined rate. This article is an overview of different types of transdermal patches, their various method of preparation as well as their various physicochemical evaluation methods. The present study is performed for the motivation of the graduates towards publication and research. Hence, we have encouraged the graduates to prepare an informative article on the present subject.

Alzheimer's disease, is a somatic disease that affects the brain. It is a progressive disease that destroys memory and other important mental functions. During this disease, accumulation of cerebral extracellular amyloid, which is mostly composed of accumulated amyloid-β (Ab) peptide as well as the accumulation of intracellular neurofibrillary tangles, appears to start up. This results in the loss of connection between nerve cell, and lead to the degeneration of neurons and finally death of brain tissue. Also due to the deficiency of some important chemical messenger in the brain, the signal transmission gets ultimately, affected in the body. The main objective of this study was to prepare the optimized formula of a VCO based emulsion containing Tween 20 as the surfactant for treatment of Alzheimer's disease which may help to increase the cholesterol level in the brain and to destroy the β amyloid plaque as a result of which the level of chemical messenger will increase in the brain. This study is further aimed to analyze, concentration of drug reaching into the brain and to study its effect in destroying β amyloid plaque.

The main objective of the present investigation was to formulate Risperidone immediate release tablet. Risperidone, an antipsychotic drug mainly act as a D2 and 5HT2A receptor antagonist. Superdisintegrants agents like kollidon and citric acid were used and compressed into tablet by direct compression method. Risperidone is mainly used to treat schizophrenia bipolar disorder. The six formulations having different concentration of superdisintegrants were prepared and formulation blend was examined for angle of repose, bulk density tapped density and compressibility. The tablet were evaluated for various parameters like hardness, thickness, friability, weight variation, disintegration time and invitro dissolution time, all the parameter were found within limits.

Controlled release drug delivery system has achieved greater importance in the field of pharmaceutical sciences to provide therapeutic advantages over the conventional drug delivery system. Nowadays, the gastrointestinal controlled drug delivery systemis more prominent than the controlled release system because these can govern the release rate of therapeutically active drug for a sustained period. A Gastro retentive dosage form improves the therapy by prolonging the gastric residence time of the drugs. Prolonged gastric retention improvesbioavailability, reduces drug waste and improves solubility for drugs that are less soluble in a high pH environment. In this review, we have discussed various systems associated with gastro retentive drug delivery with their effective mode of action. Also, the approaches and factors to increase the gastric retention time have also been discussed. This drug delivery system has potential to overcome the limitations of the conventional system. The present study is performed for the motivation of the graduates towards publication and research. Hence, we have encouraged the graduates to prepare an informative article on the present subject.

Inspite of several dosage forms available in the market for effective localized action, the lozenges finds a special importance, as they are the best dosage forms for formulating large dose medicaments. The anatomy of mouth and cheek favors easy absorption of drug, reducing the systemic absorption thus ensuring a better patient compliance especially for pediatrics and geriatrics. Ascorbic acid mechanism of action suites this type of formulation and easily absorbed in oral cavity. Preformulation studies are primarily done to investigate the physicochemical properties of drug and to establish its compatibility with other excipients. Ascorbic acid was mixed with all excipients, used in the formulation in different. The formulated lozenges were evaluated for physical parameters and the results complied with the pharmacopoeiallimits.ascorbic acid hard candy lozenges were prepared by heat fusion method using sugar as a base. The usage of corn syrup in the formulation made the lozenges transparent and smooth, which helped in improving the elegancy of formulation. The controlled release of medicament from Lozenges was achieved by using polymers like methyl cellulose, locust bean gum, HPMC, K4M and xanthan gum. The prepared lozenges were subjected to physico-chemical as well as in vitro drug release study. Among all the formulations of hard candy lozenges FL1 showed good stability.

Mouth dissolving oral films are useful in patients such as paediatric, geriatric, bedridden or developmentally disabled who face difficulty in swallowing conventional tablets or capsules and liquid orals or syrups leading to ineffective therapy. Mouthdissolving films have been played an important role in the current pharmaceutical research. They have convenience and ease of use over other dosage forms such as orally disintegrating tablets and immediate release tablets. Mouth dissolving films are oral solid dosage form that disintegrate and dissolve within a minute when placed in mouth without taking water or chewing. Risperidone is effective for treating the positive and negative symptoms of schizophrenia compared to first generation antipsychotics. But oral administration of Risperidone has drawbacks such as hepatic first pass metabolism which is overcome by means of mouth dissolving film. In the present research, mouthdissolving films of riseperidone were developed using low viscosity grades of HPMC K15 and sorbitol polymers and propylene glycol as plasticizer and purified water as solvent followed by solvent casting method. All films prepared were smooth and elegant in appearance and showed no visible cracks; were uniform in thickness, weight and drug content.

The aim of present research was to report the buccoadhesive tablet of itraconazole to provide localized delivery of drug for the treatment of oral thrush and maintain the drug concentration in the mouth for prolonged period of time thereby improving the oral bioavailability of drug. Buccoadhesive tablet is a sustained release of itraconazole for easy permeation across buccal mucosa and provide a local delivery concentration that may or may not be sufficient to maintain MIC to kill the microorganism. Solid dispersion of itraconazole was prepared by solvent evaporation technique using silica gel act as adsorbent and drug was soluble in chloroform to obtain a slurry or uniform mixture. The buccoadhesive tablet was prepared by direct compression method using different polymers such as Carbopol(C934P), HPMC K4M, Eudragit E100. Five formulations of different concentrations were prepared. Itraconazole strength were kept constant at 30mg and target was fixed at 120mg. After examine the moisture content, bulk density, tapped density, Angle of repose of powder blend get the result were found to be prescribed limit and indicated good flow property. Then the tablets were evaluated for hardness, thickness, weight variation, drug content, friability, swelling index, In-vitro drug release.

Monteleukast sodium is most commonly used in treatment of Asthma. It mainly prevents leukotriene mediated effect associated with asthama. Dispersible tablet are film coated or uncoated tablet that can be dispersed in liquid medium before administration, giving a homogenous dispersion. Dispersible tablet were prepared by using a direct compression method employing super disintegrating agentsuch as cross povidone, cross carmellose sodium and sodium starch glycolate, the tablet were preparedusing various diluents like MCC and lactose. Magnesium stearate and talc is used as a lubricant and glidant. Pre-compression parameter such as angle of repose, bulk density, tapped density, carrs index, hausner ratio carried out to study the flow properties of powder to achieve uniformity of tablet. The prepared tablet were evaluated for hardness, thickness, weight variation friablitity, % drug content, disintegration time and other parameter such as wetting time were also evaluated.

The candesartan cilexetil floating matrix drug delivery system was design to prolong the gastric residence time and improve its bioavailability. The candesartan cilexetil floating matrix tablet was prepared by using direct compression technique. Various natural polymer such as xanthan gum, guar gum as well as synthetic polymer such as hydroxypropyl methyl cellulose used in combination along with other standard excipients. Here, sodium bicarbonate acts as gas-generating agent. The granules undergoes through pre and post compression studies. The tablet evaluated by using various evaluating parameter viz, hardness, friability, weight variation, content uniformity, floating capacity and in vitro drug release studies.

Azithromycin is used for the treatment of bacterial infection, mainly used in middle ear infection, typhoid, sinusitis, bronchitis in urinary tract infection and venereal disease. The present study aimed to develop dry or oral reconstitutable suspension to minimize the solubility problem of the drug. It shows the adequate chemical stability of the drug during the shelf life and it avoids the problem of physical stability and solubility of drug. The study was carried out by preparing the dry powder or granules for oral reconstitutable suspension by using suspending agent sodium CMC and acacia on release profile of the drug. The prepared best formulation (F6) was selected depending on its physiochemical properties. The prepared oral reconstitutable suspension was evaluated for the rheological, viscosity, re-suspendibility and sedimentation volume. The formulation of acacia showed excellent sedimentation volume and good re-dispersibility as compared to other formulation. The study was found that the dry physical mixture method showed good stability of the drug.

Mucoadhesion is commonly defined as the adhesion between two materials, at least one of which is a mucosal surface. Over the past few decades, mucosal drug delivery has received a great deal of attention. Mucoadhesive dosage forms may be designed to enable prolonged retention at the site of application, providing a controlled rate of drug release for the improved therapeutic outcome. Application of dosage forms to mucosal surfaces may be of benefit to drug molecules not amenable to the oral route, such as those that undergo acid degradation or extensive first-pass metabolism. The mucoadhesive ability of a dosage form is dependent upon a variety of factors, including the nature of the mucosal tissue and the physicochemical properties of the polymeric formulation. The present study is performed for the motivation of the graduates towards publication and research. Hence, we have encouraged the graduates to prepare an informative article on the present subject.

The aim of this research was to prepare and evaluate sustain release mucoadhesive tablet ofitraconazole, in order to overcome its poor biopharmaceutical property and therapeutical efficacy. Itraconazole have low aqueous solubility and high permeability, hence in order to improve its solubility in both HCl and water it is formulated as solid dispersion by using solvent evaporation method. Solid dispersion was formulated using with itraconazole PEG 6000 in the ratio of 1: 2. Solid dispersion was then formulated in matrix of hydrophilic mucoadhesive polymers Carbopol 934P (CP) and HPMC E5LV into mucoadhesive sustained release tablet. Further, formulation were optimized for various amounts of CP and HPMC. Various amount of HPMC and Carbapol were taken as formulation variables for optimizing response variables i.e. dissolution parameters. Solid dispersion leads to enhancement in solubility of itraconazole in water up to 5.95% and in HCl it was 6.43%. In addition to enhancement of solubility in HCl and water they also lead to the slow release of drug up to 1.44% in 1 hour. Optimum combination of mucoadhesive polymers Carbopol 934P (CP) and HPMC E5LV provided adequate fairly regulated release profile. The experimental and predicted results for optimum formulations were found to be in close agreement. The formulation showed percentage drug release upto 86% for 9hour.

Lamotrigine is an anticonvulsant drug used in the treatment of epilepsy and bipolar disorders. Its acts primarily by obstructing voltage dependent sodium channel hence a decreased level of excitatory neurotransmitter. Solid dispersion is a newer technique of enhancing the solubility of poorly soluble drugs using suitable polymer. Moreover, for obtaining better drug absorption, faster onset of action and safety regarding its administration fast dissolving tablets are becoming standards. These upon administration into mouth gets rapidly dissolve due to presence of saliva without any need of water. Lamotrigine solid dispersion was prepared using PEG 6000 as polymer in the ratio (1: 1). Fast dissolving tablet of lamotrigine was formulated using 3 different superdisintegrants (crosscarmellose, kollidon, sodium starch glycolate (SSG)) in different ratios. The formulated tablets were then evaluated for its different parameters. The result of invitro dissolution study showed that formulation F5 is most successful as it dissolved in a very short period containing combination of kollidon and SSG in the ratio (1: 3). An increased disintegration time was noted with combination of crosscarmellose and SSG (1: 1) ratio.

Drug induced hemolysis is a frequent complication associated with chemotherapy. It results from interaction of drug with erythrocyte membrane and leads to cell lysis. In recent past, various approaches were made to reduce drug-induced hemolysis, which includes drug polymer conjugation, drug delivery via colloidal carriers and hydrogels, co-administration of botanical agents and modification in molecular chemistry of drug molecules. The basic concept behind these strategies is to protect the red blood cells from membrane damaging effects of drugs. There are several examples of drug polymer conjugate that either are approved by Food and Drug Administration or are under clinical trial for delivering drugs with reduced toxicities. Likewise, colloidal carriers are also used successfully nowadays for the delivery of various chemotherapeutic agents like gemcitabine and amphotericin B with remarkable decrease in their hemolytic activity. Similarly, co-administration of botanical agents with drugs works as secondary system proving protection and strength to erythrocyte membranes. In addition to the above statement, interaction hindrance between RBC and drug molecule by molecular modification plays an important role in reducing hemolysis. This review predominantly describes the above recent approaches explored to achieve the reduced hemolytic activity of drugs especially chemotherapeutic agents.

The current article has been focused on the Mucoadhesive drug delivery system may be designed to enable prolonged retention at the site of application, providing a controlled rate of drug release for improved therapeutic outcome. Mucoadhesion is commonly defined as the adhesion between two materials, at least one of which is a mucosal surface. Application of dosage forms to mucosal surfaces may be of benefit to drug molecules not amenable to the oral route, such as those that undergo acid degradation or extensive first-pass metabolism. The Mucoadhesive ability of a dosage form is dependent upon a variety of factors, including the nature of the mucosal tissue and the physicochemical properties of the polymeric formulation. This review article aims to provide an overview of the various aspects of mucoadhesion, Mucoadhesive materials, factors affecting mucoadhesion, evaluating methods, and finally various Mucoadhesive drug delivery systems (buccal, nasal, ocular, gastro, vaginal, and rectal) based on literatures were reported so far. In this review article, the various aspects of pharmaceutical microemulsion were compiled together and the target audiences are specifically the M. Pharm and B. Pharm students so that their knowledge towards the subject concern can be enhanced and also at the same time can be motivated towards the publication.