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New micelle myricetin formulation for ocular delivery: improved stability, solubility, and ocular anti-inflammatory treatment.
Sun, Fengyuan; Zheng, Zhou; Lan, Jie; Li, Xuefei; Li, Mengshuang; Song, Kaichao; Wu, Xianggen.
Afiliação
  • Sun F; a Department of Pharmacy, College of Chemical Engineering , Qingdao University of Science and Technology , Qingdao , China.
  • Zheng Z; b Key Laboratory of Marine Bioactive Substances , First Institute of Oceanography, State Oceanic Administration , Qingdao , China.
  • Lan J; c Qingdao Eye Hospital, Shandong Eye Institute , Shandong Academy of Medical Sciences , Qingdao , China.
  • Li X; a Department of Pharmacy, College of Chemical Engineering , Qingdao University of Science and Technology , Qingdao , China.
  • Li M; a Department of Pharmacy, College of Chemical Engineering , Qingdao University of Science and Technology , Qingdao , China.
  • Song K; d Pharmacy Intravenous Admixture Services , Qingdao Women and Children's Hospital , Qingdao , China.
  • Wu X; a Department of Pharmacy, College of Chemical Engineering , Qingdao University of Science and Technology , Qingdao , China.
Drug Deliv ; 26(1): 575-585, 2019 Dec.
Article em En | MEDLINE | ID: mdl-31172843
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 acetate-polyethylene 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.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Soluções Oftálmicas / Solubilidade / Flavonoides / Anti-Inflamatórios Idioma: En Ano de publicação: 2019 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Soluções Oftálmicas / Solubilidade / Flavonoides / Anti-Inflamatórios Idioma: En Ano de publicação: 2019 Tipo de documento: Article