FORMULATION AND EVALUATION OF ACARBOSE PELLETS BY EXTRUSION SPHERONIZATION TECHNIQUE

Objective: The objective of our work is to formulate and evaluate acarbose pellets for sustain drug delivery. The present study was aimed to develop sustain drug delivery system of acarbose pellets by extrusion spheronization technique using different polymers like Hydroxypropyl methyl cellulose, chitosan, ethylcellulose, microcrystalline cellulose. Pelletization of acarbose was done to achieve sustain drug release profile suitable for oral administration. Methods: The acarbose pellets were prepared by extrusion spheronization technique. The Fourier transform-infrared spectrum (FT-IR) and Differential scanning calorimetry thermogram of pure drug and drug-polymer blend showed the stable character of acarbose in the pellets. The prepared pellets were evaluated for different quality control parameters like particle size analysis, drug content, and Drug release characteristics. Results: The results obtained from different quality control parameters are within acceptable range and In vitro dissolution studies indicated that drug release from pellets follows zero-order kinetics with sustain release drug release up to 12 h with the use of ethyl cellulose as a sustain release polymer and mechanism of drug release is non-fickian. The formulated pellets were stable with respect to their physicochemical characters and drug content over a period of 60 d at accelerated stability condition. Conclusion: From present study, it was concluded that formulation of acarbose pellets by this will be a promising technique for the preparation of pellets to sustain drug release for the treatment of diabetes with better patient compliance

CHITOSAN NANOPARTICLES AS A NASAL DRUG DELIVERY FOR MEMANTINE HYDROCHLORIDE

Objective: The aim of the present study is to prepare crosslinked chitosan nanoparticles of memantine hydrochloride by using ionic gelation for nasal drug delivery system.Methods: The Memantine Hydrochloride loaded chitosan nanoparticles were prepared by ionic gelation of chitosan with tripolyphosphate anions (TPP). Various trials have been carried out to optimize the particle size, polydispersiblity index and zeta potential. The different concentration of chitosan to TPP of 2:1,3:1,4:1,5:1with varying the stirring time 2 hrs,4 hrs,6 hrs,8 hrs and stirring speed 500 rpm, 1000 rpm, 1500 rpm, 2000 rpm were used to prepare the memantine loaded chitosan nanoparticle was prepared.Results: The effects, including chitosan concentration, stirring speed and stirring time on the physicochemical properties of the nanoparticle, such as particle size, polydispersibility index was studiedConclusion: The formulation was optimized for the particle size and polydispersibility index and the particle size of nanoparticle was found to be 129 nm at 4 hrs of stirring times, 1000 rpm of stirring speed and 2:1concentration ratio of chitosan and TPP. Memantine loaded chitosan nanoparticle is a potential new delivery system for treatment of Alzheimer's disease, when transported via olfactory nasal pathway to the brain.Â

Preparation of Memantine-Loaded Chitosan Nanocrystals: In Vitro and Ex Vivo Toxicity Analysis

Alzheimer’s disease (AD) is a progressive neurodegenerative disorder with unmet medical need, and is the leading cause of age-related dementia affecting millions of people worldwide. This work aims at developing small, high-drug loading capacity (DL) and -entrapment efficiency (EE) memantine hydrochloride (MEM)/chitosan nanocrystals (CS-NCs) to treat moderate to severe dementia associated with AD. MEM-loaded chitosan nanocrystals (MEM/CS-NCs, further abbreviated as MEM-NCs) were prepared by the ionic gelation method. Different formulations were prepared by varying the concentrations of CS and sodium tripolyphosphate (STPP). The prepared MEM-NCs formulations (n = 8) were evaluated for their particle size (PS), polydispersibility index (PDI), zeta potential (ZP), DL, EE and characterized by scanning electron microscopy (SEM) and transmission electron microscopy (TEM). Furthermore, in vitro (i.e., release behavior, cytotoxicity) and ex vivo studies (i.e., histopathology) studies were carried out. The results show that the DL was over 92% and the EE was higher than 73%, while the particles were relatively small with nanometric PS (152.63 ± 12.95 to 310.23 ± 10.49 nm), uniform with acceptable PDI (0.336 ± 0.05 to 0.534 ± 0.02), and stable with positive ZP (23.8 ± 0.4 mV to 54.0 ± 0.5 mV). The optimal formulation (MEM-NC3) was selected mainly based on the PS (152.63 ± 12.95 nm), DL (98.44 ± 3.31%), and EE (78.7 ± 3.11%). Interestingly, it does not elicit any cytotoxic and tissue damage when examining at goat nasal mucosa. The selected formulation was subjected to surface morphological studies such as transmission electron microscopy (TEM), which revealed that the NCs were spherical in shape and small (100 nm). Interestingly, the selected formulation was able to sustain the drug release for up to 24 h with an initial burst release (86.51 %). We conclude that the prepared MEM-NCs represent a promising drug formulation for further in vivo studies (in animal models and in a clinical setting) to prevent and treat AD