Abstract

Millions of people are affected globally by alzheimer’s disease and it is regarded as a dangerous progressive medical and socio-economic burden. The drug delivery to brain is hindered due to the presence of blood brain barrier. Nanoparticle mediated drug delivery is a promising approach in this regard. Chitosan is a hydrophilic polysaccharide polymer of N-acetylglycosamine and glucosamine. Owing to its biodegradability, nontoxicity and biocompatibility it is regarded as a safe excipient. The aim of the study was to fabricate donepezil-loaded sustained release chitosan nanoparticles as a simple way to deliver nano-drugs to the brain. The nanoparticles were fabricated using ionic gelation method using different concentrations of Sodium tripolyphosphate (TPP) and chitosan. The fabricated nanoparticles were assessed for particle size, zeta potential, encapsulation efficiency and in vitro drug release. The effect of sonication time on the particle size of nanoparticles was also studied. The nanoparticles exhibited mean particle size (between 135-1487 nm) and zeta potential (between +3.9-+38mV) depending on chitosan and TPP concentration used. The rise in the sonication time from 25 to 125 sec exhibited a decrease in particle size. The encapsulation efficiency was found to be in the range of 39.1-74.4%. Sustained and slow release of donepezil at a constant rate was exhibited from nanoparticles. The nanoparticles show potential to deliver donepezil to brain with enhanced encapsulation efficiency.

Highlights

  • Neurodegenerative diseases comprise a range of disorders which progressively damages the cognition and memory of patient in the elderly people. 24.3 million Global population has been affected by Alzheimer’s and it is regarded as a harsh medical and socio-economic problem around the world [1]

  • We developed a nanoparticulate drug delivery system comprising of a natural hydrophilic polymer chitosan having numerous advantages such as easy fabrication of NP by minor agitation without the use of high temperature or organic solvents and obtaining a cationic charge on the surface of nanoparticles thereby enhancing the cell uptake and imparting muco-adhesive characteristic

  • The NPs were prepared by introducing gelation and monitoring its interaction with TPP which resulted in the reduction of CS’s aqueous solubility. This drug delivery system is based on intra- and inter-molecular bonds generated among positive charges of CS amino groups and TPP thereby resulting in successful nano-particulate formation

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Summary

Introduction

Neurodegenerative diseases comprise a range of disorders which progressively damages the cognition and memory of patient in the elderly people. 24.3 million Global population has been affected by Alzheimer’s and it is regarded as a harsh medical and socio-economic problem around the world [1]. Drug delivery system (DDS) shows promise in the treatment of CNS diseases because it displays numerous benefits such as drug delivery to a specific site, protection of drug from clearance by immune and circulatory systems, changing the physicochemical characteristics of drugs, reduction of doses and control of drug release [6,7,8]. They make DDS an attractive option for treating AD

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