期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 579, 期 -, 页码 -出版社
ELSEVIER
DOI: 10.1016/j.ijpharm.2020.119136
关键词
Vitamin K-1 oxide; Nanoliposomes; Box-Behnken design; In vitro release; Ex vivo permeation
资金
- Department of chemistry, Science and Research Branch, Islamic Azad University
Due to the vitamin K-1 sensitizing potential, the oxidized-isoform of vitamin K-1 (vitamin K-1 oxide, VKO), has been recently used for treating laser-induced purpura and hyperpigmentation in cosmetics. The objective of this study was to formulate VKO in nanoliposomes by using Box-Behnken experimental design to obtain an optimized formula with higher efficiency. The ratio of phospholipid to cholesterol (PC/CHO ratio), VKO concentration and sonication time in low, medium, and high levels were independent variables, while the percent of VKO entrapment efficiency (EE%) and vesicle size were selected as dependent variables. Optimum desirability was identified and an optimized formulation was prepared, characterized, and selected for in vitro VKO release and ex vivo skin permeation. The PC/CHO ratio showed the greatest effect on both responses (P < 0.0001). This effect was positive on EE%, while a negative effect was shown on vesicle size. The optimized formulation showed controlled drug release of 79.2% through a silicon membrane, and achieved flux of 327.36 +/- 22.1 mu g/cm(2) through human skin after 24 h. So, nanoliposomes were proven as a suitable drug delivery system for topical delivery of VKO.
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