Abstract

Poly(lactic-co-glycolic acid) (PLGA) based nanoparticles have gained increasing attention in delivery applications due to their capability for controlled drug release characteristics, biocompatibility, and tunable mechanical, as well as degradation, properties. However, thorough study is always required while evaluating potential toxicity of the particles from dose dumping, inconsistent release and drug-polymer interactions. In this research, we developed PLGA nanoparticles modified by chitosan (CS), a cationic and pH responsive polysaccharide that bears repetitive amine groups in its backbone. We used a model drug, diclofenac sodium (DS), a nonsteroidal anti-inflammatory drug (NSAID), to study the drug loading and release characteristics. PLGA nanoparticles were synthesized by double-emulsion solvent evaporation technique. The nanoparticles were evaluated based on their particle size, surface charge, entrapment efficacy, and effect of pH in drug release profile. About 390–420 nm of average diameters and uniform morphology of the particles were confirmed by scanning electron microscope (SEM) imaging and dynamic light scattering (DLS) measurement. Chitosan coating over PLGA surface was confirmed by FTIR and DLS. Drug entrapment efficacy was up to 52%. Chitosan coated PLGA showed a pH responsive drug release in in vitro. The release was about 45% more at pH 5.5 than at pH 7.4. The results of our study indicated the development of chitosan coating over PLGA nanoparticle for pH dependent controlled release DS drug for therapeutic applications.

Highlights

  • Drug delivery devices using biodegradable and biocompatible poly(lactic-co-glycolic acid) (PLGA) based nanoparticles have attracted a great deal of attention, as these systems can provide a sustained and controlled drug release and reduce side effects [1,2,3,4,5]

  • We investigated the ability of CS coated Poly(lactic-co-glycolic acid) (PLGA) based NPs to entrap and release, a model drug, nonsteroidal anti-inflammatory drug (NSAID) diclofenac, in a controlled manner

  • PLGA particles can be prepared by single- or double-emulsion techniques

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Summary

Introduction

Drug delivery devices using biodegradable and biocompatible poly(lactic-co-glycolic acid) (PLGA) based nanoparticles have attracted a great deal of attention, as these systems can provide a sustained and controlled drug release and reduce side effects [1,2,3,4,5]. They can protect drugs from degradation and enhance their stability. Biodegradable polymer based nanoparticle; PLGA/drug formulation strategies, can greatly enhance the therapeutic drug concentration in the blood stream for a long period of time and can subsequently reduce the multiple drug dose schedules. Cationic surface modifications of such systems has been accomplished by using cetyltrimethylammonium bromide, polyethyleneimine, poly(2-dimethylamino)ethyl methacrylate, didodecyldimethylammonium bromide, poly (ethylene glycol) and chitosan [4,15,16]

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