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用于柚皮苷局部应用的亚微米载体的制备与评价

Preparation and evaluation of submicron-carriers for naringenin topical application.

作者信息

Tsai Ming-Jun, Huang Yaw-Bin, Fang Jhih-Wun, Fu Yaw-Syan, Wu Pao-Chu

机构信息

Department of Neurology, China Medical University Hospital, Yuh-Der Road, Taichung City 404, Taiwan, ROC; School of Medicine, Medical College, China Medical University, Yuh-Der Road, Taichung City 404, Taiwan, ROC.

School of Pharmacy, Kaohsiung Medical University, 100 Shih-Chuan 1st Road, Kaohsiung City 807, Taiwan, ROC.

出版信息

Int J Pharm. 2015 Mar 15;481(1-2):84-90. doi: 10.1016/j.ijpharm.2015.01.034. Epub 2015 Jan 20.

DOI:10.1016/j.ijpharm.2015.01.034
PMID:25615985
Abstract

Submicron emulsion system is one kind of submicron-carrier that can ensure close contact and increase the amount of drug transport into the skin. In the present study, naringenin was loaded into a submicron emulsion system for topical applications. The enhancement effect of drug permeability through skin, stability, and skin irritation of naringenin-loaded submicron emulsions were evaluated. The results showed that the transdermal amount and deposition amount in skin of naringenin from submicron emulsion formulations were significantly increased when compared to the control group of saturated aqueous solution of naringenin. The drug-loaded submicron emulsions showed thermodynamic stability after centrifugation and cooling-heating cycle tests. The level of drug was more than 98% after 3 months of storage at 25°C and 40°C. In skin irritation test, the result also demonstrated that naringenin-loaded submicron emulsion had less skin irritation, indicating that the formulation can possibly be developed for topical application.

摘要

亚微乳剂系统是一种亚微米载体,可确保紧密接触并增加药物透皮转运量。在本研究中,将柚皮素载入亚微乳剂系统用于局部给药。评估了载柚皮素亚微乳剂的药物透皮增强效果、稳定性及皮肤刺激性。结果表明,与柚皮素饱和水溶液对照组相比,亚微乳剂制剂中柚皮素的透皮量和在皮肤中的沉积量显著增加。载药亚微乳剂经离心及冷热循环试验后显示出热力学稳定性。在25℃和40℃储存3个月后,药物含量超过98%。在皮肤刺激性试验中,结果还表明载柚皮素亚微乳剂的皮肤刺激性较小,表明该制剂有可能开发用于局部给药。

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