Design and Evaluation of Long Acting Biodegradable PLGA Microspheres for Ocular Drug Delivery

Abstract

Background:: The research work involves the development of PLGA biodegradable microspheres loaded with dexamethasone for intraocular delivery. Objective:: The study aimed to design and evaluate long acting PLGA microspheres for ocular delivery of dexamethasone. Methods:: The present formulation involves the development of long-acting dexamethasone loaded microspheres composed of a biodegradable controlled release polymer, Poly(D,L-lactide-coglycolide) (PLGA), for the treatment of posterior segment eye disorders intravitreally. PLGA with a monomer ratio of 50:50 of lactic acid to glycolic acid was used to achieve a drug release for up to 45 days. Quality by Design approach was utilized for designing the experiments. Single emulsion solvent evaporation technique along with high-pressure homogenization was used to facilitate the formation of microspheres. Results:: Particle size evaluation, drug content and drug entrapment efficiency were determined for the microspheres. Particle size and morphology were observed using Field Emission Gun- Scanning Electron Microscopy (FEG-SEM) and microspheres were in the size range of 1-5 μm. Assessment of drug release was done using in vitro studies and trans retinal permeation was observed by ex vivo studies using goat retinal tissues. Conclusion:: Considering the dire need for prolonged therapeutic effect on diseases of the posterior eye, an intravitreal long-acting formulation was designed. The use of biodegradable polymer with biocompatible degradation products was a rational approach to achieve this aim. The outcome of the present research shows that developed microspheres would provide a long-acting drug profile and reduce the frequency of administration thereby improving patient compliance.