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Article

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

1
Institute of Chemistry, St. Petersburg State University, Universitetskii Pr. 26, Peterhoff, 198504 St. Petersburg, Russia
2
Chemistry Department, Faculty of Science, Beni-Suef University, Salah Salem Street, Beni Suef 62511, Egypt
3
Institute of Pharmacy (Pharmacology & Toxicology), Freie Universität Berlin, Königin-Luise-Str. 2+4, 14195 Berlin, Germany
4
Department of Veterinary Drugs, Federal Office of Consumer Protection and Food Safety, Mauerstr. 39-42, 10117 Berlin, Germany
*
Author to whom correspondence should be addressed.
Academic Editors: Carlos Alonso-Moreno, Iván Bravo Pérez and Daniel Hermida-Merino
Pharmaceutics 2021, 13(6), 801; https://doi.org/10.3390/pharmaceutics13060801
Received: 28 April 2021 / Revised: 23 May 2021 / Accepted: 25 May 2021 / Published: 27 May 2021
(This article belongs to the Special Issue Polymer Therapeutics: From Synthesis to Biomedical Applications)
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. View Full-Text
Keywords: poly(ε-caprolactone); poly(L-lactide); polymeric nanoparticle; alternative methods to animal testing; biocompatibility; eye diseases; irritation; ocular drug delivery poly(ε-caprolactone); poly(L-lactide); polymeric nanoparticle; alternative methods to animal testing; biocompatibility; eye diseases; irritation; ocular drug delivery
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MDPI and ACS Style

Mohamed, A.; Korzhikov-Vlakh, V.; Zhang, N.; Said, A.; Pilipenko, I.; Schäfer-Korting, M.; Zoschke, C.; Tennikova, T. Effect of Poly(L-lysine) and Heparin Coatings on the Surface of Polyester-Based Particles on Prednisolone Release and Biocompatibility. Pharmaceutics 2021, 13, 801. https://doi.org/10.3390/pharmaceutics13060801

AMA Style

Mohamed A, Korzhikov-Vlakh V, Zhang N, Said A, Pilipenko I, Schäfer-Korting M, Zoschke C, Tennikova T. Effect of Poly(L-lysine) and Heparin Coatings on the Surface of Polyester-Based Particles on Prednisolone Release and Biocompatibility. Pharmaceutics. 2021; 13(6):801. https://doi.org/10.3390/pharmaceutics13060801

Chicago/Turabian Style

Mohamed, Abdelrahman, Viktor Korzhikov-Vlakh, Nan Zhang, André Said, Iuliia Pilipenko, Monika Schäfer-Korting, Christian Zoschke, and Tatiana Tennikova. 2021. "Effect of Poly(L-lysine) and Heparin Coatings on the Surface of Polyester-Based Particles on Prednisolone Release and Biocompatibility" Pharmaceutics 13, no. 6: 801. https://doi.org/10.3390/pharmaceutics13060801

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