Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, New Delhi 110062, India.
Colloids Surf B Biointerfaces. 2013 Mar 1;103:275-82. doi: 10.1016/j.colsurfb.2012.10.038. Epub 2012 Oct 30.
The singular aim of the proposed work is the development of a synergistic thermosensitive gel for vaginal application in subjects prone to recurrent vaginal candidiasis and other microbial infections. The dual loading of Itraconazole and tea tree oil in a single formulation seems promising as it would elaborate the microbial coverage. Despite being low solubility of Itraconazole in tea tree oil, a homogeneous, transparent and stable solution of both was created by co-solvency using chloroform. Complete removal of chloroform was authenticated by GC-MS and the oil solution was used in the development of nanoemulsion which was further translated into a gel bearing thermosensitive properties. In vitro analyses (MTT assay, viscosity measurement, mucoadhesion, ex vivo permeation, etc.) and in vivo studies (bioadhesion, irritation potential and fungal clearance kinetics in rat model) of final formulation were carried out to establish its potential for further clinical evaluation.
本研究旨在开发一种协同热敏凝胶，用于阴道给药，适用于易患复发性阴道念珠菌病和其他微生物感染的患者。伊曲康唑和茶树油的双重负载似乎很有前景，因为它可以扩大微生物的覆盖范围。尽管伊曲康唑在茶树油中的溶解度较低，但通过共溶剂法使用氯仿可以制备出两者均为均相、透明且稳定的溶液。GC-MS 验证了氯仿的完全去除，油溶液用于制备纳米乳，进一步转化为具有热敏特性的凝胶。对最终制剂进行了体外分析（MTT 测定、粘度测定、黏膜黏附性、体外渗透等）和体内研究（大鼠模型中的生物黏附性、刺激性潜力和真菌清除动力学），以确定其进一步临床评估的潜力。
