ANTIEPILEPTIC RECTAL HYDROGEL LOADED WITH CARBAMAZEPINE – RICE BRAN WAX MICROSPHERES

ABSTRACTObjectives: The objective behind the study is to develop a mucoadhesive rectal hydrogel from carbamazepine (CBZ) – rice bran wax (RBW)microspheres for the purpose of controlled release for the treatment of epilepsy.Methods: The study was conducted to formulate controlled release rectal hydrogel loaded with CBZ – RBW microspheres in two different natural polymers,RBW and collagen which are prepared by modified cooling induced solidification method and gel preparation along with their evaluation studies.Results: A thorough analysis of the optimized gel revealed that all the evaluation parameters evaluated are within the acceptable limits. Further, theoptimized microsphere formulation (M5) was used to formulate it as rectal hydrogel using polymer collagen and was characterized. The mucoadhesiontime of 25% w/w collagen hydrogel (H4) was 565 minutes, allowing the loaded microspheres to be attached on rectal mucosa. In vitro drug releasefrom the mucoadhesive hydrogel formulations showed controlled drug release pattern with a maximum drug release of 96.45±0.35% for optimizedH4 formulation after 12 hr, followed zero order release pattern with diffusion mediated Higuchi model. Ex vivo permeation studies using bovine rectalmucosa revealed that H4 formulation showed greater permeability compared to control. Histopathological findings revealed that H4 formulation issafer for rectal administration without any signs of rectal irritancy. The stability studies of optimized formulation (H4) proved that hydrogel remainedstable over a wide range of temperature condition.Conclusion: Hence, the developed rectal hydrogel formulation seems to be a viable alternative to conventional drug delivery system for the effectivemanagement of epilepsy.Keywords: Carbamazepine, Rice bran wax, Rectal hydrogel, Sustainability

ENZYMOSOMES: A RISING EFFECTUAL TOOL FOR TARGETED DRUG DELIVERY SYSTEM

The study aims to develop enzymosomes as an emerging novel drug delivery system for site-specific action. Enzymosomes utilises the specific nature of an enzyme, which is binding to a specific substrate at a controlled rate and catalysing product production step. An enzyme is encapsulated by coupling covalently to the surface of liposomes/lipid vesicles to form enzymosomes. Enzymes links through acylation, direct conjugation, physical adsorption, encapsulation methods to prepare enzymosomes with targeted action. Such novel drug delivery systems prove effective drug release and concomitantly reduces undesirable side effects of conventional treatment methods and hence showcase improvement in the long-term therapy of the disease. They are a promising substitute to conventional treatment therapies of gout, antiplatelet activities etc. Enzymosomes are newly designed supramolecular vesicular delivery systems to be useful as a tool in pharmaceutics for the raising of drug targeting and physicochemical properties and hence bioavailability. It shows beneficial effects of drugs with a narrow precision because targeting of these drugs to their site of action improves the drugs overall pharmacodynamics and pharmacokinetic profile. It also minimizes alterations in the normal enzymatic activity, thus enhancing half-life and achieve enzyme activity on targeted sites such as cancerous cells

PREPARATION AND EVALUATION OF CHITOSAN SODIUM ALGINATE CARBAMAZEPINE MICROSPHERES

ABSTRACTObjective: The objective behind our study is that a mucoadhesive rectal hydrogel chitosan sodium alginate carbamazepine (CBZ) microspheres forthe purpose of controlled release for the treatment of epilepsy to avoid the possible side effects.Methods: The study was conducted to formulate controlled release chitosan sodium alginate CBZ microspheres with the dispersion of CBZ into thenatural polymers chitosan and sodium alginate forming microspheres conducting along with their evaluation studies.Results: The formulated microspheres were subjected to various evaluation parameters, and all the physical parameters examined are within theacceptable limits. Further, the optimized microsphere formulation (CM5) was characterized. Hence, the developed optimized microsphere formulation(CM5) seems to be a viable substitute to conventional drug delivery system for the effective management of epilepsy.Conclusion: The prepared formulation also provides a desired CBZ loaded sodium alginate microspheres with the controlled release drug delivery.Keywords: Carbamazepine, Sodium alginate microspheres, Particle size

ANTI-EPILEPTIC DRUG LOADED NIOSOMAL TRANSDERMAL PATCH FOR ENHANCED SKIN PERMEATION

Objective: To formulate and characterize midazolam loaded niosomal transdermal patches for overcoming the frequent dosing and lower bioavailability complications associated with conventional therapy. Methods: The loaded niosomal transdermal patches were prepared by thin film hydration method. The preliminary evaluation and characterization studies was conducted to find the optimised formulation. The in vitro release and ex-vivo permeation studies were investigated. The histopathological studies and stability studies were also assessed. Results: The midazolam loaded niosomal transdermal patches of vesicle size and zeta potential 116.1±84.46 d. nm and 8.56±1.2 mV respectively was formulated. The characterizations of both niosome and niosomal transdermal patches were found to be within the acceptable limits. The in vitro drug release showed an initial burst release followed by sustained release for both optimised niosomal formulation N5 and optimised niosomal transdermal patch formulation NT5with a maximum activity at 97.3±0.35% and 98.9±0.20% respectively. The ex vivo permeation studies of niosomal transdermal patch NT5 was performed which showed a higher permeability than control solution with a flux value of 0.151. The histopathological studies of the optimised formulation showed no detectable lesions upon skin surface and irritations. The stability studies showed that patches were stable over 90 d in different atmospheric conditions. Conclusion: The midazolam loaded niosomal transdermal patch was found to be a promising nano drug delivery alternative which showed better entrapment, release with permeation profile for the daily management of epilepsy with decreased dosing frequency

NANODISCS: A NEW EPOCH IN THE STUDY OF MEMBRANE PROTEINS AND AS AN EMERGING DRUG DELIVERY SYSTEM

Nano discs recently evolved as a novel tool for studying the membrane associated proteins and serve as an effective drug delivery system. Nano discs constitute disc shaped nano particles and can be defined as a membrane system which is synthetic in nature and aids in the study of membrane proteins. It is mainly made of phospholipid bilayer and the water repelling edge is isolated by amphipathic proteins called membrane scaffolding proteins [MSP]. Micelles present in the nano disc mimics the property of the biological membrane proteins. It is a powerful technology that competently delivers the drug components in to the right cells in the right tissues. Membrane scaffold proteins are primarily expressed, purified and characterized and self-assembled to form Nano discs by the process of dialysis using biobeads. Nano discs are proven to be effective in the study of membrane proteins because they can fluidize and counterbalance and also help in reclusion, refinement, biophysical and biochemical studies of them. It also presents a more genuine environment than liposomes, bicelles, amphipols and detergent micelles. Major technological advantages of nano discs include the higher stability and carrier capacity and also the increased feasibility of incorporating both hydrophilic and hydrophobic substances of drug carrier. Thus nano discs serves as an excellent system in its ability to precisely control its composition and provide a nano scale membrane surface for investigating molecular recognition events. This article reviews the emphasis of nanodiscs in studying membrane proteins as well as its effectivity in transforming into a major drug delivery system. An overview of published literatures between 1996 and 2017 was conducted to write the review

DISCOSOMES: A FUTURISTIC UPHEAVAL IN VESICULAR DRUG DELIVERY

The formulation system employed to convey pharmaceutical drugs compound in the body to attain the desired therapeutic effect at a predetermined rate depending on pharmacological aspects, drug profile, and physiological conditions can be referred to as a novel drug delivery system (NDDS). Due to the intricately sensitive anatomy and physiology of the eye pharmacologist find the ocular delivery system to be more involuted than other routes. Pre-corneal, static and dynamic is the 3 types of ophthalmic barriers, which along with the inflow and outflow of lacrimal fluids, nasolacrimal drainage, are some of the germane factors that affect bioavailability. Unlike conventional dosage forms, where the distribution of drugs in non-targeted body fluids and tissues transcends the quantity of required drug in targeted tissues and causes repercussions, these modified drug delivery systems surpass the ocular barriers and adverse reactions, emphasizing on less invasive, prolonged action. It also promotes sustained release formulation that subjugates the drug loss or degradation to treat many ocular diseases effectively. The current review recapitulates the fundamentals of discosomes, a type of vesicular drug delivery system that acts as a vehicle for the drug delivery of both hydrophilic and lipophilic drugs. Discosomes are giant, disc-shaped structures modified from niosomes by arresting the vesicles at the discosome phase. Due to their idiosyncratic size, it provides all due benefits compared to other ocular drug delivery systems. From the review, it can be culminated that discosomes are a potential subject of opposition and opportunities in the arena of safe and effective ocular drug delivery

STATE-OF-THE-ART NANOTECHNOLOGY BASED DRUG DELIVERY STRATEGIES TO COMBAT COVID-19

The emerging Coronavirus Disease-19 (COVID-19) pandemic has had a global impact on all important aspects of our society. As it is known, SARS-Cov-2 can withstand up to 72 h in adverse environmental conditions, which can aid its rapid spread. Woefully, an efficacious and approbated vaccine for the SARS-CoV-2 virus remains unavailable, which makes the problem more frightening and presently more complicated bestowing forlorn medical care. Nevertheless, global clinical research is studying several over-the-counter (OTC) drugs approved for other indications to confront coronavirus. Over the past decade, therapeutic nanoparticles have been regarded as a felicitous tool for the efficient and persnickety delivery of therapeutic groups (i.e., drugs, vaccines, siRNAs, and peptides) to the site of infection. They can adequately convey the drug encapsulated nanoparticle to a designated locus without instigating unsought effects. Besides, they acquiesce the use of non-invasive imaging methods to monitor the surface of the infection and the response to treatment. The formulated nanoparticle is apposite for intranasal drug delivery which is a meritorious method to deliver therapeutic moiety for viral diseases affecting the lungs. Applying nanoparticles via intranasal route surmounted several demerits of mucosal administration like circumventing enzymatic degradation of the therapeutic moiety, upgrading and prolonging the action of the drug, etc., and can thus corroborate as an exceptional strategy to encounter respiratory viruses like coronavirus. In this article, we illuminate the promising role of nanoparticles as effective carriers of therapeutic or immunomodulatory agents to help combat COVID-19. The search criteria used were Pubmed, Medscape, Google scholar, etc and the keywords are coronavirus, nanoformulations, nanoparticles, drug delivery, intranasal delivery, etc. The articles range from 2012 to 2020

FAST DISSOLVING SUBLINGUAL PATCH OF PHENOBARBITAL SODIUM: FORMULATION AND IN VITRO EVALUATION

Objective: To formulate and characterize. Phenobarbital sodium loaded sublingual patch using biodegradable, mucoadhesive, fast-dissolving natural polymer pullulan for immediate management of epileptic seizures. Methods: Phenobarbital sodium loaded sublingual patches were prepared by the solvent casting method and were subjected to various physicochemical evaluation parameters to find the optimized sublingual patch. The in vitro drug release study and kinetic model of the optimized formulation was also carried out. The stability study of the optimized Phenobarbital sodium loaded sublingual patch was also done. Results: From in vitro drug release study, it was found that Phenobarbital sodium loaded sublingual patch (S4) exhibited a maximum drug release of 96.24±1.27% at the end of 60 min compared to other formulations indicating a faster drug release from the formulation with release kinetics as Higuchi diffusion model. In fact, a notable release data was obtained between 0.5 to 8 min by all formulations, specifically S4 formulation (20.84±1.97% and 77.22±2.41% drug release at the end of 0.5 min and 8 min respectively) showed a better percentage release profile in comparison with other formulations. Such a trend is vital to deliver the drug at a faster rate to promote immediate effect for managing the fatal and complicated seizure. Considering the physicochemical property and in vitro drug release data, S4 formulation was regarded as an optimized one. The stability study also confirmed that S4 formulation is stable at refrigeration conditions. Conclusion: The formulated Phenobarbital sodium loaded sublingual patch is an effective drug delivery carrier which enables faster drug release to manage epileptic seizure

FORMULATION AND EVALUATION OF NIOSOMAL SUSPENSION OF CEFIXIME

Objectives : The present study was aimed to overcome the problems associated with the drug such as bioavailability, to reduce the dosage regimen, half life and to determine the appropriateness of niosomal formulation as a drug carrier.Methods: The niosomal suspension was prepared by thin film technique, by varying ratios of span 60 and cholesterol and varying the concentration of span 60. The prepared four formulations were evaluated for various parameters.Results: The optimized formulation had a vesicular size of 250-400nm .Varying the concentration of span 60 ,the entrapment efficiency demonstrated that it had a considerable task.The highest entrapment efficiency was  95.3%. The kinetics study confirmed that the liberation of drug from the niosomal suspension is in a restricted manner. The statistical optimization showed that NS2 is the optimized formulation. The gastrointestinal enzymes showed no significant change in the release of drug from the formulation. The Zone of Inhibition showed that Optimized formulation has better activity than the marketed formulation. The MIC was found to be 0.05mg , hence can be used as a efficient carrier for delivery of Cefixime.Conclusion: The present study concludes that the prepared Niosomal suspension is a convenient and efficiency carrier for the delivery of antibacterial drug. Besides this, it provided controlled delivery of drug.    Â

NOVASOME: A PIONEERING ADVANCEMENTIN VESICULAR DRUG DELIVERY

Pharmaceutical research has developed various new types of innovative forms of drug delivery. Advancement in current drug delivery methods has led to the development of numerous new revolutionary technologies that support safe and efficient formulations over existing ones. Novasome technology is one of the latest liposome developments that have overcome many of the liposomal drug delivery system-related problems. This provides a seven bilayer membrane which is capable of absorbing water-soluble as well as insoluble drugs. The improved efficiency of entrapping drugs with good encapsulation features enables better frequency of dosing, which can be accomplished through the high shear system. These find their applications in diverse fields such as cosmetics, chemicals, personal care, food, pharmacy, and agrochemicals. Several products have already been launched into the market using this technology with an additional launch plan. Due to its depth of penetration, novasomes have been one of the most popular derma cosmetics. It is being studied continuously to obtain improved release characteristics. The prospect of drug delivery and targeting using novasomes is an important area of research and development. This review pinpoints the various aspect of the novasome and will be a milestone for the researchers in the area of drug delivery