盐酸特比萘芬转移体、薄荷体和乙醇体纳米囊泡配方皮肤渗透及抗真菌效果的比较研究

A. Zaky
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引用次数: 7

摘要

本研究的目的是比较非闭塞条件下盐酸特比萘芬(TH)转移体、薄荷体和乙醇体制剂的皮肤渗透性和抗真菌效果。盐酸特比萘芬是一种治疗甲癣的抗真菌药物。其外用制剂渗透性差,导致疗效差。利用混合组分模型确定了不同浓度非离子表面活性剂制备TH转移体的最佳配方,并对Span和Tween (X1和X2)进行了研究。结果表明,X1和X2对药物的囊泡大小(Y1)和包封效率(EE) (Y2)均有显著影响。制备了囊泡,并对其形状、大小、zeta电位和包封效率进行了表征。体外研究采用Franz扩散细胞进行经皮吸收研究。转移体、薄荷体和醇质体最优配方的囊泡大小分别为78.7、122.8和67.8 nm, zeta电位分别为-8.28、8.77和11.30 mV,包封效率分别为92.67、93.86和95.75%。载药纳米囊泡的体外渗透率比药物悬浮液高2 ~ 3倍。可变形性验证了制备物的弹性。最后,TH纳米囊泡配方改善了药物传递,在皮肤渗透和抗真菌活性方面有更大的改善。我们所选择的配方显示出对黑曲霉治疗指甲或脚趾甲的有效抗真菌作用。关键字;盐酸特比萘芬,转移体,薄荷体,乙醇体,纳米囊泡
本文章由计算机程序翻译,如有差异,请以英文原文为准。
COMPARATIVE STUDY OF TERBINAFINE HYDROCHLORIDE TRANSFERSOME, MENTHOSOME AND ETHOSOME NANOVESICLE FORMULATIONS VIA SKIN PERMEATION AND ANTIFUNGAL EFFICACY
The purpose of the present research was to compare the skin permeation and study the antifungal efficacy of Terbinafine hydrochloride (TH) transfersome, menthosome and ethosome formulations under non-occlusive conditions. Terbinafine hydrochloride is an antifungal drug for onychomycosis. Poor permeability of its external preparation leads to poor curative effect. Preparation of TH transfersome utilized the mixture component model to determine the optimized desirable formula using different concentrations of nonionic surfactant, Span and Tween (X1 & X2 respectively) were investigated. The results revealed that both X1 and X2 had a pronounced effect on vesicle size (Y1) and entrapment efficiency (EE) of the drug (Y2). The vesicles were prepared and characterized for shape, size, zeta potential and entrapment efficiency. Ex vivo study via Franz diffusion cells was used for the percutaneous absorption studies. The optimum desirable formula of transfersome, menthosome and ethosome formulations were showed vesicle size (78.7, 122.8 and 67.8 nm), zeta potential (-8.28, 8.77 and 11.30 mV) and encapsulation efficiency (92.67, 93.86 and 95.75%), respectively. Ex vivo permeation of the drug-loaded nanovesicle showed more than two to three folds higher permeation rate compared with drug suspension. Deformability verified elasticity of the preparation. Finally, TH nanovesicle formulations improved drug delivery with greater improvement in skin permeation and antifungal activity. Our selected formulae showed potent antifungal effect against Aspergillus niger for the treatment of fingernails or toenails. Keywords; Terbinafine Hydrochloride, Transfersome, Menthosome, Ethosome, Nanovesicles
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