Yang Yan, Ou Rujing, Guan Shixia, Ye Xiaoling, Hu Bo, Zhang Yi, Lu Shufan, Zhou Yubin, Yuan Zhongwen, Zhang Jun, Li Qing-Guo
a College of Traditional Chinese Medicine , Guang Zhou University of Chinese Medicine , Guang Zhou , China .
b School of Material Science and Engineering , Nanyang Technological University , Singapore , and.
Drug Deliv. 2015 Dec;22(8):1086-1093. doi: 10.3109/10717544.2013.878856. Epub 2014 Jan 22.
Terbinafine hydrochloride is an antifungal drug for onychomycosis. Poor permeability of its external preparation leads to poor curative effect. Transfersomes, also known as flexible liposome, could improve transmission of drug for local external use. Terbinafine hydrochloride-loaded liposome is expected to become a breakthrough on the treatment of onychomycosis.
This study is aimed to prepare high skin penetration terbinafine hydrochloride transfersomes with high encapsulation efficiency, appropriate drug loading and good stability.
Taking entrapment efficiency as the main indicator, the formulations and the processes of preparation were investigated. Transfersomes with different surfactants were prepared in the optimization processes, and the formulations were optimized through the transdermal test in vitro. As a result, a gel contained transfersomes was obtained with a brief evaluation. Its pharmacokinetic properties of going through the skin were studied by using the micro dialysis technology and liquid chromatography-mass spectrometry to assay the penetration behavior of terbinafine.
Mean particle size of the terbinafine hydrochloride transfersomes was 69.6 ± 1.23 nm, and the entrapment efficiency was 95.4% ± 0.51. The content of the gel was 4.45 ± 0.15 mg/g. The accumulated permeation of the transfersomes gel in 12 h was 88.52 ± 4.06 µg cm and the intracutaneous drug detention was 94.38 ± 5.26 µg cm. The results of pharmacokinetic studies showed the C and area under the curve (AUC) were apparently higher than the commercial cream.
The terbinafine hydrochloride transfersomes was highly absorbed by the skin. The absorption rate was significantly higher than that of the commercial cream either in the transdermal test in vitro or in the pharmacokinetic studies in vivo.
盐酸特比萘芬是一种用于治疗甲癣的抗真菌药物。其外用制剂渗透性差，导致治疗效果不佳。传递体，也称为柔性脂质体，可改善局部外用药物的传递。载有盐酸特比萘芬的脂质体有望成为甲癣治疗的突破。
本研究旨在制备具有高包封率、合适载药量和良好稳定性的高皮肤渗透性盐酸特比萘芬传递体。
以包封率为主要指标，研究制剂和制备工艺。在优化过程中制备了含有不同表面活性剂的传递体，并通过体外透皮试验对制剂进行优化。结果，通过简要评估获得了含传递体的凝胶。利用微透析技术和液相色谱-质谱联用技术研究其经皮药代动力学性质，以测定特比萘芬的渗透行为。
盐酸特比萘芬传递体的平均粒径为69.6±1.23nm，包封率为95.4%±0.51。凝胶含量为4.45±0.15mg/g。传递体凝胶在12小时内的累积渗透量为88.52±4.06μg/cm，皮内药物滞留量为94.38±5.26μg/cm。药代动力学研究结果表明，其血药浓度（C）和曲线下面积（AUC）明显高于市售乳膏。
盐酸特比萘芬传递体被皮肤高度吸收。在体外透皮试验和体内药代动力学研究中，其吸收速率均显著高于市售乳膏。
