Effect of Poly(L-lysine) and Heparin Coatings on the Surface of Polyester-Based Particles on Prednisolone Release and Biocompatibility.

Abdelrahman Mohamed,Monika Schäfer-Korting,Tatiana Tennikova,Viktor Korzhikov-Vlakh,André Said,Nan Zhang,Christian Zoschke,Iuliia Pilipenko

doi:10.3390/pharmaceutics13060801

Abstract

A plethora of micro- and nanoparticle types are currently investigated for advanced ocular treatment due to improved drug retention times, higher bioavailability and better biocompatibility. Yet, comparative studies of both physicochemical and toxicological performance of these novel drug delivery systems are still rare. Herein, poly(L-lactic acid)- and poly(ε-caprolactone)-based micro- and nanoparticles were loaded with prednisolone as a model drug. The physicochemical properties of the particles were varied with respect to their hydrophilicity and size as well as their charge and the effect on prednisolone release was evaluated. The particle biocompatibility was assessed by a two-tier testing strategy, combining the EpiOcularTM eye irritation test and bovine corneal opacity and permeability assay. The biodegradable polyelectrolyte corona on the particles’ surface determined the surface charge and the release rate, enabling prednisolone release for at least 30 days. Thereby, the prednisolone release process was mainly governed by molecular diffusion. Finally, the developed particle formulations were found to be nontoxic in the tested range of concentrations.

Highlights

We have shown that release of the drug could be severely affected by the coating of the particles with polyelectrolyte layers
The objective of this study was to elucidate the effect of surface properties of polyestersbased micro- and nanoparticles with different hydrophobicities on the release kinetics of the encapsulated model drug prednisolone
The formulated particles were modified ized as carriers for the prednisolone model drug

Summary

Introduction

NPs as compared layers of polyelectrolytes, (PLys-Hep) , show even a release profile, without an initial could be explained by the greater specific surface area of NPs, which allows the “burst”. This could be referred to the action of two factors, namely, a decrease in the drug rapid drug release from. Leakage of theMoreover, drug duringfast modification and formation of the hydrophilic thickness, through which the diffusion of the drug occurs, and greater drug layer on the particle surface This layer could serve as an additional barrier for drugconcentr diffusion, which helps to prolong thesee drug release in the particles (drug loading, Table 1). This layer could serve as an additional barrier for drugconcentr diffusion, which helps to prolong thesee drug release in the particles (drug loading, Table 1). (Figure 4).

Objectives

Methods

Results

Conclusion