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用于外阴阴道念珠菌病局部治疗的含卡泊芬净的新制剂

New Formulations Loading Caspofungin for Topical Therapy of Vulvovaginal Candidiasis.

作者信息

Pérez-González Noelia, Bozal-de Febrer Nuria, Calpena-Campmany Ana C, Nardi-Ricart Anna, Rodríguez-Lagunas María J, Morales-Molina José A, Soriano-Ruiz José L, Fernández-Campos Francisco, Clares-Naveros Beatriz

机构信息

Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, Campus of Cartuja, University of Granada, 18071 Granada, Spain.

Department of Biology, Healthcare and the Environment, Faculty of Pharmacy and Food Sciences, University of Barcelona, 27-31 Joan XXIII Ave., 08028 Barcelona, Spain.

出版信息

Gels. 2021 Dec 12;7(4):259. doi: 10.3390/gels7040259.

Abstract

Vulvovaginal candidiasis (VVC) poses a significant problem worldwide affecting women from all strata of society. It is manifested as changes in vaginal discharge, irritation, itching and stinging sensation. Although most patients respond to topical treatment, there is still a need for increase the therapeutic arsenal due to resistances to anti-infective agents. The present study was designed to develop and characterize three hydrogels of chitosan (CTS), Poloxamer 407 (P407) and a combination of both containing 2% caspofungin (CSP) for the vaginal treatment of VVC. CTS was used by its mucoadhesive properties and P407 was used to exploit potential advantages related to increasing drug concentration in order to provide a local effect. The formulations were physically, mechanically and morphologically characterized. Drug release profile and ex vivo vaginal permeation studies were performed. Antifungal efficacy against different strains of spp. was also evaluated. In addition, tolerance of formulations was studied by histological analysis. Results confirmed that CSP hydrogels could be proposed as promising candidates for the treatment of VVC.

摘要

外阴阴道念珠菌病(VVC)在全球范围内都是一个重大问题,影响着社会各阶层的女性。其表现为白带异常、阴道刺激、瘙痒和刺痛感。尽管大多数患者对局部治疗有反应,但由于对抗感染药物产生耐药性,仍需要增加治疗手段。本研究旨在开发并表征三种水凝胶,分别为壳聚糖(CTS)、泊洛沙姆407(P407)以及二者与2%卡泊芬净(CSP)的组合,用于VVC的阴道治疗。使用CTS是因其具有粘膜粘附特性,使用P407是为了利用与提高药物浓度相关的潜在优势,以产生局部效应。对这些制剂进行了物理、机械和形态学表征。进行了药物释放曲线和离体阴道渗透研究。还评估了对不同 菌株的抗真菌疗效。此外,通过组织学分析研究了制剂的耐受性。结果证实,CSP水凝胶有望成为治疗VVC的候选药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6d26/8701247/076a87cf2458/gels-07-00259-g001.jpg

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