Comparative evaluation of cyclosporine A/HPβCD-incorporated PLGA nanoparticles for development of effective ocular preparations

Aksungur P., Demirbilek M., DENKBAŞ E. B. , Ünlü N.

Journal of Microencapsulation, vol.29, no.6, pp.605-613, 2012 (SCI-Expanded) identifier identifier

  • Publication Type: Article / Article
  • Volume: 29 Issue: 6
  • Publication Date: 2012
  • Doi Number: 10.3109/02652048.2012.668961
  • Journal Name: Journal of Microencapsulation
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.605-613
  • Keywords: CsA, Dry eye disease, HPβCD, Nanoparticles, PLGA
  • Ankara Haci Bayram Veli University Affiliated: No


To improve poor water solubility of cyclosporine A (CsA), hydroxypropyl-beta-cyclodextrin (HPβCD) was incorporated into the nanoparticle formulation. Solid complexes of CsA with HPβCD in different ratios were prepared by the kneading method. CsA containing alone or in combination with HPβCD in poly-lactide-co-glycolide (P-CsA or P-CsA-HPβCD) nanoparticles were prepared by the emulsification solvent evaporation method. The mean size of CsA-loaded NPs was found to be approximately 220nm. The solubility of CsA was significantly improved and the phase solubility diagram of CsAHPβCD systems showed an AL type phase. Nanoparticles showed high CsA encapsulation efficiency (88) and production yield (89). Release rate was increased by the presence of HPβCD and total cumulative release ranged from 75 to 96 in 24h. In vitro cytotoxicity study assay resulted in a low toxicity for all types of nanoparticles. After 6h incubation period, the cellular uptake was found at 33 and 32 for PCsA and PHPβCDCsA nanoparticles, respectively. © 2012 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted.