TY - JOUR

T1 - Effect of Poly(L-lysine) and Heparin Coatings on the Surface of Polyester-Based Particles on Prednisolone Release and Biocompatibility

AU - Mohamed , Abdelrahman

AU - Korzhikov-Vlakh, Viktor

AU - Zhang, Nan

AU - Said, Andre

AU - Pilipenko, Iuliia

AU - Schäfer-Korting, Monika

AU - Zoschke, Christian

AU - Tennikova, Tatiana

N1 - Publisher Copyright: © 2021 by the authors. Licensee MDPI, Basel, Switzerland.

PY - 2021/6

Y1 - 2021/6

N2 - 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.

AB - 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.

KW - поли(капролактон), поли(лактид), полимернглаз,

KW - ые наночастицы, альтернативные методы для тестирования на животных, биосовместимость, заболевания

KW - poly(ε-caprolactone)

KW - poly(L-lactide)

KW - polymeric nanoparticle

KW - alternative methods to animal testing

KW - biocompatibility

KW - eye diseases

KW - irritation

KW - ocular drug delivery

KW - Polymeric nanoparticle

KW - Poly(L-lactide)

KW - Ocular drug delivery

KW - Alternative methods to animal testing

KW - Poly(ε-caprolactone)

KW - Biocompatibility

KW - Eye diseases

KW - Irritation

UR - https://pubmed.ncbi.nlm.nih.gov/34072016/

UR - https://www.mdpi.com/1999-4923/13/6/801

UR - http://www.scopus.com/inward/record.url?scp=85107760559&partnerID=8YFLogxK

U2 - 10.3390/pharmaceutics13060801

DO - 10.3390/pharmaceutics13060801

M3 - Article

VL - 13

JO - Pharmaceutics

JF - Pharmaceutics

SN - 1999-4923

IS - 6

M1 - 801

ER -