• Mengshuang Li, Meng Xin, Chuanlong Guo, Guiming Lin, and Xianggen Wu.
• a Department of Pharmacy, College of Chemical Engineering , Qingdao University of Science and Technology , Qingdao , China.
• Drug Dev Ind Pharm. 2017 Nov 1; 43 (11): 1846-1857.

ContextA stable topical ophthalmic curcumin formulation with high solubility, stability, and efficacy is needed for pharmaceutical use in clinics.ObjectivesThe objective of this article was to describe a novel curcumin containing a nanomicelle formulation using a polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (PVCL-PVA-PEG) graft copolymer.MethodsNanomicelle curcumin was formulated and optimized and then further evaluated for in vitro cytotoxicity/in vivo ocular irritation, in vitro cellular uptake/in vivo corneal permeation, and in vitro antioxidant activity/in vivo anti-inflammatory efficacy.ResultsThe solubility, chemical stability, and antioxidant activity were greatly improved after the encapsulation of the PVCL-PVA-PEG nanomicelles. The nanomicelle curcumin ophthalmic solution was simple to prepare and the nanomicelles are stable to the storage conditions, and it had good cellular tolerance. Nanomicelle curcumin also had excellent ocular tolerance in rabbits. The use of nanomicelles significantly improved in vitro cellular uptake and in vivo corneal permeation as well as improved anti-inflammatory efficacy when compared with a free curcumin solution.ConclusionsThese findings indicate that nanomicelles could be promising topical delivery systems for the ocular administration of curcumin.

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