Mengshuang Li1,2, Meng Xin1,3, Chuanlong Guo4, Guiming Lin1,2, Xianggen Wu1,2. 1. a Department of Pharmacy, College of Chemical Engineering , Qingdao University of Science and Technology , Qingdao , China. 2. b School of Medicine and Life Sciences , University of Jinan-Shandong Academy of Medical Sciences , Jinan , China. 3. c Department of Ophthalmology , Yantai Affiliated Hospital of Binzhou Medical University , Yantai , China. 4. d Institute of Oceanology , Chinese Academy of Sciences , Qingdao , China.
Abstract
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.
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.
Authors: Federica Franzone; Marcella Nebbioso; Tiziano Pergolizzi; Giuseppe Attanasio; Angela Musacchio; Antonio Greco; Paolo Giuseppe Limoli; Marco Artico; Demetrios A Spandidos; Samanta Taurone; Enzo Agostinelli Journal: Exp Ther Med Date: 2021-05-21 Impact factor: 2.447