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苦参总生物碱纳米乳的理化性质及体外透皮性能

[Physicochemical properties and skin penetration in vitro of total alkaloids of Sophora flavescens nanoemulsion].

作者信息

Feng Ai-Ling, Wang Ying-Zi, Zhang Sheng-Hai, Sun Xiu-Yu, Duan Fei-Peng, Li Cai-Xia

机构信息

School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2013 Aug;38(16):2628-32.

PMID:24228577
Abstract

The research aimed at investigating the physicochemical properties, stability and skin penetration in vitro of total alkaloids of Sophora flavescens nanoemulsion. Prepare total alkaloids of S. flavescens nanoemulsion and detect the determination of matrine and oxymatrine in the nanoemulsion using HPLC method. Transmission electron microscopy and laser particle size analyzer were utilized to detect the shape and size of the nanoemulsion respectively. And also the stability of nanoemulsion was studied under the conditions of low temperature (4 degrees C), normal temperature (25 degrees C) and high temperature (60 degrees C). Franz diffusion cell was used to research the transdermal absorption of nanoemulsion in vitro. The results found that the nanoemulsion we prepared presented appearance of rounded, uniform; its average diameter was (15.55 +/- 2.24) nm, and particle size distribution value was 0. 161; the appearance, diameter and percentage determination of total alkaloids of S. flavescens had no variations after 15 d under 4, 25, 60 degrees C respectively. The steady-state permeation rate was 4.564 1 microg x cm(-2) x h(-1), 24 h cumulative amount of penetration was 110.7 microg x cm(-2), which was 1.86 fold of 24 h cumulative amount of aqueous solution (59.41 microg x cm(-2)). All the results demonstrated total alkaloids of S. flavescens nanoemulsion had good permeability, and could provide a new preparation for its clinical application.

摘要

本研究旨在考察苦参总生物碱纳米乳的理化性质、稳定性及体外皮肤渗透情况。制备苦参总生物碱纳米乳,并采用高效液相色谱法测定纳米乳中苦参碱和氧化苦参碱的含量。分别利用透射电子显微镜和激光粒度分析仪检测纳米乳的形态和粒径。同时考察纳米乳在低温(4℃)、常温(25℃)和高温(60℃)条件下的稳定性。采用Franz扩散池研究纳米乳的体外透皮吸收情况。结果发现,所制备的纳米乳呈圆形、均匀外观;平均粒径为(15.55±2.24)nm,粒度分布值为0.161;苦参总生物碱纳米乳在4℃、25℃、60℃条件下放置15 d后,外观、粒径及总生物碱含量测定均无变化。稳态渗透速率为4.564 1μg·cm-2·h-1,24 h累积渗透量为110.7μg·cm-2,是水溶液24 h累积渗透量(59.41μg·cm-2)的1.86倍。所有结果表明,苦参总生物碱纳米乳具有良好的渗透性,可为其临床应用提供一种新的制剂。

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