Nanomicelle formulation for topical delivery of cyclosporine A into the cornea: in vitro mechanism and in vivo permeation evaluation

• DOI: 10.1038/srep12968
• Publication Date: 2015-08-26T09:06:27Z
• Authors: Chuanlong Guo; Yan Zhang; Zhao Yang; Mengshuang Li; Fengjie Li; Fenghua Cui; Ting Liu; Weiyun Shi; Xianggen Wu
• Keywords: 04 agricultural and veterinary sciences; 0405 other agricultural sciences; Article; 3. Good health

Abstract A stable topical ophthalmic cyclosporine (CsA) formulation with good tolerance and high efficacy is still a desire in pharmaceutics clinics. This article describes the preparation of CsA containing nanomicelles using polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (PVCL-PVA-PEG) graft copolymer. Both polymer itself were evaluated for cytotoxicity ocular irritation. The vitro uptake intracellular fate characterized. In vivo cornea permeation test performed 0.5 mg/mL compared commercially available (10 mg/mL) oil-based solution. nanomicelle solution was simple to prepare remained storage stable. PVCL-PVA-PEG had no as its monomer micelle (IC 50 (48 h) = 14.02 mg/mL). also excellent rabbits. use significantly improved cellular uptake, apparently by an energy dependent endocytosis pathway that involved early endosomes, late lysosomes ER. showed delivered levels into cornea, when 10 These findings indicated could be promising delivery system administration CsA.