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

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

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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.
Original languageEnglish
Article number801
Number of pages18
JournalPharmaceutics
Volume13
StatePublished - 27 May 2021

Scopus subject areas

  • Materials Science(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

Keywords

  • poly(ε-caprolactone)
  • poly(L-lactide)
  • polymeric nanoparticle
  • alternative methods to animal testing
  • biocompatibility
  • eye diseases
  • irritation
  • ocular drug delivery

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