Abstract The Malus hupehensis (Pamp.) Rehd. is a traditional medicine and edible plant. The previous study found that the extracts of M. hupehensis (Pamp.) Rehd. had a good antioxidant activity in vivo and in vitro. But its clinical application was limited by its poor solubility, rapidly metabolized and poor bioavailability. Hence, this article aimed at developing liposomes as a novel transdermal system for delivering M. hupehensis extracts efficiently. The prepared liposomes were characterized regarding their entrapment efficiency percentage (EE%), vesicle size (VS), polydispersity index (PDI), zeta potential (ZP) and drug loading (DL). Box-Behnken design response surface methodology and factorial design were used to optimize formulation and preparation process, respectively. The optimized liposomes had an EE of 77.29 ± 0.99%, VS of 102.74 ± 1.61 nm, ZP of −21.79 ± 1.43 mV, PDI of 0.291 ± 0.005 and DL was 6.68 ± 0.49%. Transmission electron microscopy showed liposomes had a regular spherical surface. In addition, liposomes exhibited superior skin permeation potential and retention capacity compared with solution. Histopathological study ensured the safety of liposome application. Meanwhile, the optimized liposome has a good stability. Hence, M. hupehensis extracts liposomes could be considered a promising vehicle for transdermal delivery.

中文翻译：

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Malus hupehensis (Pamp.) Rehd 提取物脂质体的优化、表征和评价

摘要 Malus hupehensis (Pamp.) Rehd。是一种传统药食植物。先前的研究发现 M. hupehensis (Pamp.) Rehd. 的提取物。在体内外均具有良好的抗氧化活性。但其溶解性差、代谢快、生物利用度差等限制了其临床应用。因此，本文旨在将脂质体开发为一种新的透皮系统，用于有效递送 M. hupehensis 提取物。制备的脂质体通过包封率 (EE%)、囊泡大小 (VS)、多分散指数 (PDI)、zeta 电位 (ZP) 和载药量 (DL) 进行表征。Box-Behnken 设计响应面方法和因子设计分别用于优化配方和制备过程。优化后的脂质体的 EE 为 77.29 ± 0.99%，VS 为 102.74 ± 1。61 nm，ZP 为 -21.79 ± 1.43 mV，PDI 为 0.291 ± 0.005，DL 为 6.68 ± 0.49%。透射电子显微镜显示脂质体具有规则的球形表面。此外，与溶液相比，脂质体表现出优异的皮肤渗透潜力和保留能力。组织病理学研究保证了脂质体应用的安全性。同时，优化后的脂质体具有良好的稳定性。因此，湖北分枝杆菌提取物脂质体可被认为是一种有前途的透皮给药载体。优化后的脂质体稳定性好。因此，湖北分枝杆菌提取物脂质体可被认为是一种有前途的透皮给药载体。优化后的脂质体稳定性好。因此，湖北分枝杆菌提取物脂质体可被认为是一种有前途的透皮给药载体。