New nanomicelle curcumin formulation for ocular delivery: improved stability, solubility, and ocular anti-inflammatory treatment

作者：Li, Mengshuang; Xin, Meng; Guo, Chuanlong; Lin, Guiming; Wu, Xianggen^*

来源：Drug Development and Industrial Pharmacy, 2017, 43(11): 1846-1857.

DOI：10.1080/03639045.2017.1349787

• Curcumin
• stability
• polyvinyl caprolactam-polyvinyl acetatepolyethylene glycol graft copolymer (PVCL-PVA-PEG)
• nanomicelle
• ocular drug delivery

Context: A stable topical ophthalmic curcumin formulation with high solubility, stability, and efficacy is needed for pharmaceutical use in clinics. Objectives: The 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. @@@ Methods: Nanomicelle 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. @@@ Results: The 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. @@@ Conclusions: These findings indicate that nanomicelles could be promising topical delivery systems for the ocular administration of curcumin.

• 出版日期2017
• 单位济南大学; 中国科学院海洋研究所; 青岛科技大学; 滨州医学院; 山东省医学科学院