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将卵磷脂-胆盐纳米囊泡作为一种有前途的方法用于姜黄素的有效皮肤传递,以改善 Wistar 白化大鼠的 UV 诱导皮肤损伤。

Integrated lecithin-bile salt nanovesicles as a promising approach for effective skin delivery of luteolin to improve UV-induced skin damage in Wistar Albino rats.

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Damanhour University, Damanhour, Egypt.

Department of Pharmacology and Toxicology, Faculty of Pharmacy, Cairo University, Giza 11562, Egypt.

出版信息

Colloids Surf B Biointerfaces. 2022 Mar;211:112299. doi: 10.1016/j.colsurfb.2021.112299. Epub 2021 Dec 18.

Abstract

The present study improved the effectiveness of a poorly water-soluble drug, luteolin (LUT), by encapsulating it in lecithin-bile salt-integrated system called bilosomes (BLs). Such a delivery system offers the benefits of mimicking the skin's biological structure and being a prominent tool to circumvent skin delivery obstacles. The prepared BLs underwent complete in vitro assessment. The developed BLs showed enhanced characteristics compared to free luteolin suspension (P < 0.05). Optimized BLs attained good entrapment efficiency (78.60% ± 0.88%), small particle size (226.1 ± 2.45 nm), and sustained drug-release pattern. The study also showed that both blank and LUT-loaded BLs preparations were safe to the skin with a primary irritancy index of < 2 based on the Draize test. In vivo tests were conducted to study the effect of the bile salt-based nanovesicles compared with the free LUT suspension. The photoprotective effect was evaluated according to the visual examination and biochemical analyses of antioxidant, anti-inflammatory, and anti-wrinkling markers after ultraviolet B irradiation. Results of biochemical markers and histopathological examination demonstrated that the LUT-BLs effect was superior than the LUT suspension (P < 0.05). Consequently, the current study proves that novel LUT-loaded BLs is a promising nanoplatform that overcome LUT delivery obstacles and, hence, alleviate UV-induced skin damage.

摘要

本研究通过将疏水性较差的药物木樨草素(LUT)包封在称为双分子层囊泡(BLs)的卵磷脂-胆汁盐整合系统中,提高了其有效性。这种递药系统具有模拟皮肤生物结构的优点,是克服皮肤递药障碍的重要工具。所制备的 BLs 进行了全面的体外评估。与游离木樨草素混悬液相比,所开发的 BLs 表现出增强的特性(P<0.05)。优化的 BLs 达到了良好的包封效率(78.60%±0.88%)、较小的粒径(226.1±2.45nm)和持续的药物释放模式。研究还表明,空白和载 LUT 的 BLs 制剂对皮肤均安全,根据 Draize 试验,其初级刺激性指数<2。进行了体内试验以研究基于胆汁盐的纳米囊泡与游离 LUT 混悬液的比较效果。根据紫外线 B 照射后抗氧化、抗炎和抗皱标志物的视觉检查和生化分析来评估光保护效果。生化标志物和组织病理学检查的结果表明,LUT-BLs 的效果优于 LUT 混悬液(P<0.05)。因此,本研究证明了新型载 LUT 的 BLs 是一种有前途的纳米平台,可克服 LUT 递药障碍,从而减轻 UV 诱导的皮肤损伤。

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