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熊果酸醇质体的制备及其经皮扩散

[Preparation and transdermal diffusion of ursolic acid ethosomes].

作者信息

Chen Yan, Wiu Qingqing, Zhang Zhenhai, Zhou Lei, Liu Xuan, Du Meng, Jia Xiaobin

机构信息

Department of Pharmaceutics, Jiangsu University, Zhenjiang 212013, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2011 Apr;36(8):988-91.

PMID:21809568
Abstract

OBJECTIVE

To prepare ursolic acid ethosomes and investigate the penetration characteristics of ursolic ethosomes as a transdermal vehicle.

METHOD

Ursolic acid ethosomes were prepared by injection method, and the shape and particle size of the ethosomes were analyzed. Ursolic acid permeation tests in vitro through the skin of rats were performed in TP-3 diffusion cell. The accumulated permeation amounts of ursolic acid 10% isopropanol solution, ursolic acid liposomes, ursolic acid ethosomes were compared.

RESULT

The average encapsulation percentage, particle size, and Zeta potential of the ethosomes were (95.83 +/- 0.86)%, (87.5 +/- 7.5) nm and - (38.4 +/- 3.6) mV, respectively. The accumulated permeation amount of the ethosomes in 12 h was 146.49 microg x cm(-2), and its transdermal permeability in 12 h was 12.17 microg x cm(-2) x h(-1).

CONCLUSION

The encapsulation percentage of the ethosomes is good, and the stability of the ursolic acid ethosomes is fine. Ethosomes can significantly enhance the diffusion rate of ursolic acid through the skin of rats.

摘要

目的

制备熊果酸醇质体并考察其作为透皮给药载体的渗透特性。

方法

采用注入法制备熊果酸醇质体,分析醇质体的形态和粒径。在TP - 3扩散池中进行熊果酸体外透过大鼠皮肤的试验,比较熊果酸10%异丙醇溶液、熊果酸脂质体、熊果酸醇质体的累积渗透量。

结果

醇质体的平均包封率、粒径和Zeta电位分别为(95.83±0.86)%、(87.5±7.5)nm和 - (38.4±3.6)mV。醇质体12 h的累积渗透量为146.49μg·cm⁻²,其12 h的透皮速率为12.17μg·cm⁻²·h⁻¹。

结论

醇质体包封率良好,熊果酸醇质体稳定性较好。醇质体可显著提高熊果酸透过大鼠皮肤的扩散速率。

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