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新型羟苯甲酮负载纳米结构脂质载体(NLCs)的配方。

Formulation of a novel oxybenzone-loaded nanostructured lipid carriers (NLCs).

机构信息

Department of Pharmaceutics, National Organization of Drug Control and Research (NODCAR), Cairo, Egypt.

出版信息

AAPS PharmSciTech. 2010 Dec;11(4):1684-94. doi: 10.1208/s12249-010-9553-2. Epub 2010 Nov 24.

Abstract

The objective of the current study was to formulate oxybenzone into nanostructured lipid carriers (NLCs) to enhance its sunscreening efficacy and safety. NLCs of oxybenzone were prepared by the solvent diffusion method. A complete 2(3) factorial design was used for the evaluation of the prepared oxybenzone NLCs. The study design involves the investigation of the effect of three independent variables namely liquid lipid type (Miglyol 812 and oleic acid), liquid lipid concentration (15% and 30%), and oxybenzone concentration (5% and 10% with respect to total lipids) on the particle size (p.s.) , the entrapment efficiency (EE%) and the in vitro drug release after 8 h. The prepared NLCs were spherical in overall shape and were below 0.8 microm. Miglyol 812 and 30% liquid lipid were found to significantly decrease the p.s. and increase the EE% when compared to oleic acid and 15% liquid lipid. Increasing oxybenzone concentration increased significantly the p.s. but did not affect the EE%. NLCs prepared using Miglyol 812, 15% liquid lipid, and 10% oxybenzone showed slower drug release when compared to those prepared using oleic acid, 30% liquid lipid, and 5% oxybenzone, respectively. The candidate oxybenzone-loaded NLC dispersion was then formulated into gel. The incorporation of oxybenzone into NLCs greatly increased the in vitro sun protection factor and erythemal UVA protection factor of oxybenzone more than six- and eightfold, respectively, while providing the advantage of overcoming side effects of free oxybenzone as evidenced by very low irritation potential.

摘要

本研究的目的是将氧苯酮制成纳米结构脂质载体(NLC),以提高其防晒效果和安全性。通过溶剂扩散法制备氧苯酮 NLC。采用完全 2(3)析因设计评价所制备的氧苯酮 NLC。研究设计包括考察三种独立变量(液体脂质类型(Migl yol 812 和油酸)、液体脂质浓度(15%和 30%)和氧苯酮浓度(分别相对于总脂质为 5%和 10%)对粒径(p.s.)、包封效率(EE%)和 8 小时后体外药物释放的影响。所制备的 NLC 总体呈球形,粒径小于 0.8 微米。与油酸和 15%液体脂质相比,Migl yol 812 和 30%液体脂质显著降低了 p.s.,并提高了 EE%。增加氧苯酮浓度显著增加了 p.s.,但对 EE%没有影响。与分别使用油酸、30%液体脂质和 5%氧苯酮制备的 NLC 相比,使用 Migl yol 812、15%液体脂质和 10%氧苯酮制备的 NLC 显示出较慢的药物释放。然后将候选氧苯酮负载的 NLC 分散体制成凝胶。将氧苯酮掺入 NLC 中,使氧苯酮的体外防晒因子和红斑 UVA 保护因子分别增加了六倍和八倍以上,同时提供了克服游离氧苯酮副作用的优势,这从极低的刺激性潜力得到证明。

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