Cyclosporine-A incorporated cationic solid lipid nanoparticles for ocular delivery.
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 116 structured FD4 (0.1% CsA) formulation was chosen for in vivo studies. Sheep were used in in vivo studies and 200 microL 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.
Başaran
Ebru
E
Department of Pharmaceutical Technology, Anadolu University, Faculty of Pharmacy, Eskişehir, Turkey. ebcengiz@anadolu.edu.tr
Demirel
Müzeyyen
M
Sirmagül
Başar
B
Yazan
Yasemin
Y
D000818:Animals; D002152:Calorimetry, Differential Scanning; D002412:Cations / Q000737:chemistry; D016572:Cyclosporine / Q000008:administration & dosage*; D003692:Delayed-Action Preparations / Q000737:chemistry; D005123:Eye / Q000378:metabolism*; D007166:Immunosuppressive Agents / Q000008:administration & dosage*; D008055:Lipids / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D053758:Nanoparticles / Q000737:chemistry*; D009883:Ophthalmic Solutions / Q000737:chemistry*; D010316:Particle Size; D012756:Sheep; D017550:Spectroscopy, Fourier Transform Infrared; D014961:X-Ray Diffraction
D002412:Cations; D003692:Delayed-Action Preparations; D007166:Immunosuppressive Agents; D008055:Lipids; D009883:Ophthalmic Solutions; D016572:Cyclosporine