New micelle myricetin formulation for ocular delivery: improved stability, solubility, and ocular anti-inflammatory treatment

doi:10.1080/10717544.2019.1622608

	New micelle myricetin formulation for ocular delivery: improved stability, solubility, and ocular anti-inflammatory treatment
	Sun, Fengyuan 1; Zheng, Zhou 2; Lan, Jie 3; Li, Xuefei 1; Li, Mengshuang 1,4; Song, Kaichao 1; Wu, Xianggen 1,5
刊名	DRUG DELIVERY
	2019
卷号	26 期号:1 页码:575-585
关键词	Myricetin micelle ocular drug delivery polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer stability
ISSN号	1071-7544
DOI	10.1080/10717544.2019.1622608
英文摘要	Myricetin (Myr) is a naturally occurring flavonoid exhibiting diverse biological and pharmacological properties, but its characteristics such as water insolubility, poor aqueous stability, and poor bioavailability limit its clinical application, including in ophthalmology. To increase its clinical application in ophthalmology, Myr was designed to be encapsulated in a polyvinyl caprolactam-polyvinyl acetatepolyethylene glycol graft copolymer (PVCL-PVA-PEG) polymeric micelles to increases its aqueous solubility, stability, and corneal permeability to promote its efficacy in eye disease treatments. Thus, the Myr micelle ophthalmic solution was prepared and characterized encapsulation efficiency (EE), micelle size, and zeta potential. The chemical stability of Myr and the short-term storage stability of the Myr micelle ophthalmic solution were evaluated, followed by in vitro cytotoxicity and in vivo ocular irritation; in vitro cellular uptake and in vivo corneal permeation; and in vitro antioxidant activity and in vivo anti-inflammatory efficacy were also further evaluated. Myr could be incorporated into micelles with high EE. PVCL-PVA-PEG micelles significantly enhanced Myr's aqueous solubility and chemical stability. The Myr micelle ophthalmic solution also showed high storage stability. In rabbits, the Myr micelle ophthalmic solution displayed good in vitro cellular tolerance. Remarkable improvements in in vitro cellular uptake and in vivo corneal permeation were also observed in the Myr micelle ophthalmic solution, and significant improvements in the in vitro antioxidant activity and in vivo anti-inflammatory efficacy were also obtained. Overall, these results supported that the Myr micelle ophthalmic solution could be a promising nanomedicine for ocular tissues.
资助项目	Science and Technology Foundation of Shinan District, Qingdao, Shandong Province, China[2018-4-029-YY]
WOS关键词	IN-VITRO MECHANISM ; POLYMERIC MICELLES ; ORAL BIOAVAILABILITY ; ANTIOXIDANT ACTIVITY ; 15 HYDROXYSTEARATE ; CYCLOSPORINE-A ; DRUG-DELIVERY ; VIVO ; CURCUMIN ; NANOMICELLE
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	TAYLOR & FRANCIS LTD
WOS记录号	WOS:000473788500001
内容类型	期刊论文
源URL	[http://ir.fio.com.cn:8080/handle/2SI8HI0U/24571]
专题	自然资源部第一海洋研究所
通讯作者	Wu, Xianggen
作者单位	1.Qingdao Univ Sci & Technol, Coll Chem Engn, Dept Pharm, Qingdao 266042, Shandong, Peoples R China 2.State Ocean Adm, Key Lab Marine Bioact Subst, Inst Oceanog 1, Qingdao, Shandong, Peoples R China 3.Shandong Acad Med Sci, Qingdao Eye Hosp, Shandong Eye Inst, Qingdao, Shandong, Peoples R China 4.Qingdao Women & Childrens Hosp, Pharm Intravenous Admixture Serv, Qingdao, Shandong, Peoples R China 5.Qingdao Univ Sci & Technol, Key Lab Pharmaceut Res Metab Dis, Qingdao, Shandong, Peoples R China
推荐引用方式 GB/T 7714	Sun, Fengyuan,Zheng, Zhou,Lan, Jie,et al. New micelle myricetin formulation for ocular delivery: improved stability, solubility, and ocular anti-inflammatory treatment[J]. DRUG DELIVERY,2019,26(1):575-585.
APA	Sun, Fengyuan.,Zheng, Zhou.,Lan, Jie.,Li, Xuefei.,Li, Mengshuang.,...&Wu, Xianggen.(2019).New micelle myricetin formulation for ocular delivery: improved stability, solubility, and ocular anti-inflammatory treatment.DRUG DELIVERY,26(1),575-585.
MLA	Sun, Fengyuan,et al."New micelle myricetin formulation for ocular delivery: improved stability, solubility, and ocular anti-inflammatory treatment".DRUG DELIVERY 26.1(2019):575-585.