A New Mode of Thinfilm and Nanofiber for Burst Release of the Drug for Alzheimer Disease; A Complete Scenario from Dispersible Polymer to Formulation Methodology.

Alzheimer's Disease (AD) is usually caused by intellectual deterioration which occurs due to the degeneration of cholinergic neurons. Donepezil is employed for cholinesterase enzyme Inhibition (ChEI) to treat AD in a wider population. Over the years, researchers finding difficulties prompted through traditional dosage forms particularly in geriatric patience. To avoid swallowing difficulties brought about with the aid of the AD population, researchers majorly focused on Oral Thin-Film technology (OTF). This technology strongly eliminates issues caused by solid oral dosage forms. It is one of the quality strategies to alternate a drug that is used in the first-pass metabolism or pre systematic metabolism. The solubility of the drug is a bigger problem and it can expand by way of lowering particle size. Nanofibers are need of the day to minimize the drug particles at the submicron stage which can increase the drug release rate drastically. It can be prepared by Electrospinning technology by incorporating polymeric material into poorly soluble drugs. Mostly natural and biodegradable polymers prefer in all pharmaceutical preparations. Polymers employed for oral delivery should be stable, possess mucoadhesive properties, and should release the drug by diffusion, degradation, and swelling mechanism. The objective of the present review explains various thin-film and nanofiber formulations used for faster drug release in the treatment of Alzheimer's disease.

Micro and nanocrystalline cellulose based oral dispersible film; preparation and evaluation of in vitro/in vivo rapid release studies for donepezil

Oral fast-dispersible film was prepared by utlizing donepezil hydrochloride (drug) and various cellulose derivatives such as hydroxypropyl methyl cellulose (hypermellose) (HPMC), microcrystalline cellulose (MCC) and nanocrystalline cellulose (NCC) to treat Alzheimer's disease. NCC was synthesized by ultra-sonication method using MCC and this was converted to thinfilm formulation (NCC-F) using solvent casting technique. The interaction between the polymer and the drug was investigated by spectral analysis such as UV, FTIR, and 1H- NMR. FTIR confirmed that the compatibility of drug and polymer in ODF formulation. NCC-F has shown an average surface roughness of 77.04 nm from AFM and the average particle size of 300 nm from SEM analysis. Nano sized particle of NCC-F leads faster in vitro dissolution rate (94.53%) when compared with MCC-F and F3 formulation. Animal model (in vivo) studies of NCC-F formulation has reached peak plasma concentration (Cmax) up to 19.018 ng/mL in the span of (tmax) 4 h with greater relative bioavailability of 143.1%. These results suggested that high surface roughness with nanosized NCC-F formulation attained extended drug availability up to (t1/2) 70 h.

Nanomedicines as Drug Delivery Carriers of Anti-Tubercular Drugs: From Pathogenesis to Infection Control.

In spite of advances in tuberculosis (TB) chemotherapy, TB is still airborne deadly disorder as a major issue of health concern worldwide today. Extensive researches have been focused to develop novel drug delivery systems to shorten the lengthy therapy approaches, prevention of relapses, reducing dose-related toxicities and to rectify technologically related drawbacks of anti-tubercular drugs. Moreover, the rapid emergence of drug resistance, poor patient compliance due to negative therapeutic outcomes and intracellular survival of Mycobacterium highlighted to develop carrier with optimum effectiveness of the anti-tubercular drugs. This could be achieved by targeting and concentrating the drug on the infection reservoir of Mycobacterium. In this article, we briefly compiled the general aspects of Mycobacterium pathogenesis, disease treatment along with progressive updates in novel drug delivery carrier system to enhance therapeutic effects of drug and the high level of patient compliance. Recently developed several vaccines might be shortly available as reported by WHO.

Hyperbranched cellulose polyester of oral thin film and nanofiber for rapid release of donepezil; preparation and in vivo evaluation.

Cellulose blended hyperbranched polyester (CHP) and hyperbranched cellulose polyester (HPC) were synthesized by melt condensation method using 2,2-bis (methylol) propionic acid and p-TSA. Obtained polymers were utilized for the preparation of various donepezil loaded thinfilm (CHPF, HPCF) and nanofibers (CHPN, HPCN) using solvent casting and electrospinning technique respectively. Formulated thinfilms and nanofibers were subjected to thermal analysis and microscopic evaluations. Compared with thinfilm formulations, hyperbranched nanofiber has shown lower particle size about 50-100 nm. This might be helped in releasing 98% of drug in the span of 10 min in in vitro studies for HPCN 4 formulation. Further investigation of in vivo bioavailability studies, peak plasma concentration was observed at 3 to 3.5 h for HPCN formulation. Hyperbranched cellulose formulations (HPCN 4) have significantly higher absorption (AUC 0-∞) (1294.1 ±â€¯5.4 ng/mL) than cellulose blended hyperbranched polymer formulations (876.1 ±â€¯6.1 ng/mL). These studies revealed that the hyperbranched nanofiber formulations possess high mechanical strength and good drug release properties. Current study concludes prepared Hyperbranched cellulose nanofiber will be good alternative for commercially available dosage forms for the treatment of Alzheimer's diseases.

Chitosan nanofilm and electrospun nanofiber for quick drug release in the treatment of Alzheimer's disease: In vitro and in vivo evaluation.

Chitosan micro sized ODF (CBF), chitosan nano sized ODF (CNF) and chitosan nanofiber (CNfib) were prepared to release the donepezil drug quickly for Alzheimer's disease. CNF and CNfib were prepared from ionic gelation technique and electro-spinning process which were further examined under in vitro and in vivo animal model studies. Good thermal stability of CNfib (450°C) when compared to CBF (325°C) and CNF (305°C). The particle size was below 150nm in diameter for CNfib and 250nm in diameter for CNF4 from TEM technique. In vitro antimicrobial activities for ODF and nanofibers were conducted by well diffusion method against Gram +ve and Gram -ve bacteria after 24h of incubation. From the in vitro release profile, the CNfib was competently showed rapid release of drug up to 97% than the thin film of CBF2 and CNF4 respectively in the initial period of 10min. In vivo animal model studies demonstrated that the drug reached the maximum concentration within 3.5h for chitosan nanofiber and nanofilm (CNF4). The chitosan nanofiber has given significantly faster absorption rate [1860.5ng/ml of AUC(0-∞)] and the mean total area under curve was 161.71% on contrasted with chitosan nanofilm (CNF4).