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湖北海棠(Pamp.)Rehd.提取物脂质体的优化、表征及评价

Optimization, characterization and evaluation of liposomes from Malus hupehensis (Pamp.) Rehd. extracts.

作者信息

Guo Dongyan, Liu Ji, Fan Yu, Cheng Jiangxue, Shi Yajun, Zou Junbo, Zhang Xiaofei

机构信息

Shaanxi Key Laboratory of New Drugs and Chinese Medicine Foundation Research, College of Pharmacy, Shaanxi University of Chinese Medicine, Xianyang, China.

College of Basic Medicine, Shaanxi University of Chinese Medicine, Xianyang, China.

出版信息

J Liposome Res. 2020 Dec;30(4):366-376. doi: 10.1080/08982104.2019.1651334. Epub 2019 Aug 23.

DOI:10.1080/08982104.2019.1651334
PMID:31387437
Abstract

The 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 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, extracts liposomes could be considered a promising vehicle for transdermal delivery.

摘要

这是一种传统药物和可食用植物。先前的研究发现,湖北海棠(Pamp.)Rehd.的提取物在体内和体外均具有良好的抗氧化活性。但其临床应用受到其溶解度差、代谢迅速和生物利用度低的限制。因此,本文旨在开发脂质体作为一种新型的经皮给药系统,以有效递送提取物。对制备的脂质体的包封率(EE%)、囊泡大小(VS)、多分散指数(PDI)、zeta电位(ZP)和载药量(DL)进行了表征。分别采用Box-Behnken设计响应面法和析因设计优化制剂和制备工艺。优化后的脂质体的EE为77.29±0.99%,VS为102.74±1.61nm,ZP为-21.79±1.43mV,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滞留能力。组织病理学研究确保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,提取物脂质体可被认为是一种有前途的经皮给药载体。

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