Department of Pharmaceutics, Faculty of Pharmacy, Damanhour University, Damanhour, Egypt.
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Cairo University, Giza 11562, Egypt.
Colloids Surf B Biointerfaces. 2022 Mar;211:112299. doi: 10.1016/j.colsurfb.2021.112299. Epub 2021 Dec 18.
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.
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。