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载姜黄素阴道乳膏的制剂研究、稳定性考察及其在大鼠阴道假丝酵母菌病模型中的初步药效评价。

Formulation, stability study and preclinical evaluation of a vaginal cream containing curcumin in a rat model of vulvovaginal candidiasis.

机构信息

Department of Drugs and Pharmaceutics, Faculty of Pharmaceutical Sciences, São Paulo State University - UNESP, Araraquara, SP, Brazil.

Laboratory of Pharmacology, Federal University of São João Del-Rei, Campus Centro Oeste Dona Lindu, Divinópolis, Minas Gerais, Brazil.

出版信息

Mycoses. 2018 Oct;61(10):723-730. doi: 10.1111/myc.12762. Epub 2018 Jul 31.

DOI:10.1111/myc.12762
PMID:29517833
Abstract

Owing to the growing resistance among isolates of Candida species to usual antifungal agents and the well-known therapeutic potential of curcumin, the purpose of this study was to develop and validate a vaginal formulation containing this substance and to evaluating its effectiveness in the treatment of experimental vulvovaginal candidiasis. Curcumin was incorporated in a vaginal cream in three concentrations (0.01%, 0.1% and 1.0%). The different concentrations of the cream and its controls were intravaginally administered in an immunosuppressed rat model to evaluate the efficacy in the treatment of experimental vulvovaginal candidiasis. Samples of the cream were also subjected to centrifugation and physical stability tests and an analytical method for quantification of curcumin was validated based on HPLC. The formulation was stable and the HPLC method could be considered suitable for the quantitative determination of curcumin in the cream. After 6 days of preclinical study, the number of infected animals was 1/6 in all groups treated with curcumin vaginal cream and the fungal burden showed a progressive reduction. Reduction in the inflammatory infiltrate was observed in the group treated with 1.0% cream. Vaginal cream containing curcumin could be considered a promising effective antifungal medicine in the treatment of vulvovaginal candidiasis.

摘要

由于念珠菌属真菌的抗药性日益增强,以及姜黄素的显著治疗潜力,本研究旨在开发和验证一种含有该物质的阴道制剂,并评估其在治疗实验性外阴阴道念珠菌病中的疗效。姜黄素以三种浓度(0.01%、0.1%和 1.0%)被掺入阴道乳膏中。乳膏的不同浓度及其对照品被阴道内给药于免疫抑制大鼠模型,以评估在治疗实验性外阴阴道念珠菌病中的疗效。乳膏的样品还进行了离心和物理稳定性测试,并基于 HPLC 验证了一种姜黄素定量分析方法。该制剂稳定,HPLC 方法可被认为适合于乳膏中姜黄素的定量测定。经过 6 天的临床前研究,所有接受姜黄素阴道乳膏治疗的动物中,感染动物的数量均为 1/6,真菌负荷呈逐渐减少的趋势。在 1.0%乳膏治疗组中观察到炎症浸润的减少。含有姜黄素的阴道乳膏可被认为是治疗外阴阴道念珠菌病的一种有前途的有效抗真菌药物。

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