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新一代氟康唑:现有研究与技术综述

New Generation of Fluconazole: A Review on Existing Researches and Technologies.

作者信息

Behtash Afsaneh, Nafisi Shohreh, Maibach Howard I

机构信息

Department of Chemistry, Central Tehran Branch, IAU, Tehran, Iran.

出版信息

Curr Drug Deliv. 2017;14(1):2-15. doi: 10.2174/1567201813666160502125620.

Abstract

BACKGROUND

The frontline drug fluconazole (FLZ) has been used for treating skin fungal infections for over 35 years. FLZ has relatively large molecular size and hydrophobicity which improves its bioavailability via intravenous or oral routes but makes its use in a topical application problematic. In recent years, nano-based strategies have been examined to eliminate FLZ adverse effects and increase the drug efficiency. The present overview surveys nano-drug delivery systems used to improve FLZ efficiency; the strengths and weaknesses of the systems and the relevant achievements of pharmaceutical technology follow.

METHODS

A systematic literature search study was developed based on the significant concepts being used in the review. Key search terms and a matrix-based search strategy using Boolean logic strategy were defined. Nano-formulations affecting dermal permeation of nanomaterials and experimental setups for studying skin absorbance of FLZ-nanomaterials were analysed.

RESULTS

In recent years, nano-based strategies including solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs), liposomes, niosomes, ethosomes, microemulsions, nanoemulsions have been examined to increase FLZ antifungal efficiency and eliminate drug adverse effects. Significant differences was demonstrated in FLZ efficiency by different nanoparticles. Few data are available regarding a comparison of FLZ antifungal effects using various nanoparticles, but the present research suggests a positive impact on penetration.

CONCLUSION

Various nano-formulations have been applied to optimize fluconazole topical delivery. The present review indicated that the data related to improve fluconazole efficacy by nanoparticles are few and defining the appropriate nano-formulation is not currently possible. More research is needed to compare the capability of various nanoparticles on fluconazole skin permeation, and to translate these findings into clinical arena.

摘要

背景

一线药物氟康唑(FLZ)已用于治疗皮肤真菌感染超过35年。氟康唑分子尺寸相对较大且具有疏水性,这通过静脉内或口服途径提高了其生物利用度,但使其在局部应用中存在问题。近年来,已研究基于纳米的策略以消除氟康唑的不良反应并提高药物效率。本综述概述了用于提高氟康唑效率的纳米药物递送系统;这些系统的优缺点以及药物技术的相关成果如下。

方法

基于综述中使用的重要概念开展了一项系统的文献检索研究。定义了关键检索词和使用布尔逻辑策略的基于矩阵的检索策略。分析了影响纳米材料皮肤渗透的纳米制剂以及用于研究氟康唑-纳米材料皮肤吸收的实验设置。

结果

近年来,已研究了包括固体脂质纳米粒(SLNs)和纳米结构脂质载体(NLCs)、脂质体、非离子表面活性剂囊泡、醇质体、微乳、纳米乳在内的基于纳米的策略,以提高氟康唑的抗真菌效率并消除药物不良反应。不同纳米颗粒在氟康唑效率方面表现出显著差异。关于使用各种纳米颗粒比较氟康唑抗真菌效果的数据很少,但目前的研究表明对渗透有积极影响。

结论

已应用各种纳米制剂来优化氟康唑的局部递送。本综述表明,关于通过纳米颗粒提高氟康唑疗效的数据很少,目前无法确定合适的纳米制剂。需要更多研究来比较各种纳米颗粒对氟康唑皮肤渗透的能力,并将这些发现转化到临床领域。

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