Cyclosporine-A incorporated cationic solid lipid nanoparticles for ocular delivery


BAŞARAN E., Demirel M., SIRMAGÜL B., Yazan Y.

JOURNAL OF MICROENCAPSULATION, vol.27, no.1, pp.37-47, 2010 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 27 Issue: 1
  • Publication Date: 2010
  • Doi Number: 10.3109/02652040902846883
  • Journal Name: JOURNAL OF MICROENCAPSULATION
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.37-47
  • Keywords: Cyclosporine A, cationic solid lipid nanoparticles, ocular application, BINARY-MIXTURES, DRUG-DELIVERY, LIQUID, SLN, STABILITY, EYE
  • Anadolu University Affiliated: Yes

Abstract

In the present study, Cyclosporine A (CsA) was successfully incorporated into cationic solid lipid nanoparticles (SLN) for ocular application. Physicochemical characterizations of SLNs were analysed in detail during the storage period of 6 months. Due to the better characteristics like smaller particle size (248.00 +/- 0.33 nm) with narrow size distribution (PI = 0.25 +/- 0.00), high zeta potential (50.30 +/- 0.78 mV) and more stable lipid structure, Dynasan (R) 116 structured FD4 (0.1% CsA) formulation was chosen for in vivo studies. Sheep were used in in vivo studies and 200 mu L of formulation was applied to sheep' eyes (n = 6) under veterinarian supervision. Samples were collected at pre-determined time intervals and were analysed by enzyme immune assay (EIA). CsA could be detected in both aqueous and vitreous humour samples for 48 h showing the ocular penetration of formulation. Release profiles were not decreased during 48 h indicating controlled and prolonged release of active agent from positively charged SLN formulations due to increased residence time in eyes. Similarities in CsA concentration data showed that inter-individual variance did not influence the ocular penetration of CsA when formulated as SLN.