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微乳剂在制药领域的应用:对多药物递送的影响。

Microemulsion utility in pharmaceuticals: Implications for multi-drug delivery.

作者信息

Callender Shannon P, Mathews Jessica A, Kobernyk Katherine, Wettig Shawn D

机构信息

School of Pharmacy, University of Waterloo, 200 University Ave. W., Waterloo, Ontario N2L3G1, Canada.

School of Pharmacy, University of Waterloo, 200 University Ave. W., Waterloo, Ontario N2L3G1, Canada; Waterloo Institute for Nanotechnology, University of Waterloo, 200 University Ave. W., Waterloo, Ontario N2L3G1, Canada.

出版信息

Int J Pharm. 2017 Jun 30;526(1-2):425-442. doi: 10.1016/j.ijpharm.2017.05.005. Epub 2017 May 7.

Abstract

Emulsion technology has been utilized extensively in the pharmaceutical industry. This article presents a comprehensive review of the literature on an important subcategory of emulsions, microemulsions. Microemulsions are optically transparent, thermodynamically stable colloidal systems, 10-100nm diameter, that form spontaneously upon mixing of oil, water and emulsifier. This review is the first to address advantages and disadvantages, as well as considerations and challenges in multi-drug delivery. For the period 1 January 2011-30 April 2016, 431 publications related to microemulsion drug delivery were identified and screened according to microemulsion, drug classification, and surfactant types. Results indicate the use of microemulsions predominantly in lipophilic drug delivery (79.4%) via oil-in-water microemulsions and non-ionic surfactants (90%) for oral or topical administration. Cancer is the disease state most targeted followed by inflammatory diseases, microbial infections and cardiovascular disease. Key generalizations from this analysis include: 1) microemulsion formulation is largely based on trial-and-error despite over 1200 publications related to microemulsion drug delivery since their discovery in 1943; 2) characterization using methods including interfacial tension, droplet size, electrical conductivity, turbidity and viscosity may provide additional information for greater predictability; 3) microemulsion drug delivery publications arise primarily from China (27%) and India (21%) suggesting additional research opportunities elsewhere.

摘要

乳液技术已在制药行业中得到广泛应用。本文对乳液的一个重要子类别——微乳液的文献进行了全面综述。微乳液是光学透明、热力学稳定的胶体系统,直径为10 - 100纳米,在油、水和乳化剂混合时自发形成。本综述首次探讨了多药物递送中的优缺点以及注意事项和挑战。在2011年1月1日至2016年4月30日期间,共识别出431篇与微乳液药物递送相关的出版物,并根据微乳液、药物分类和表面活性剂类型进行了筛选。结果表明,微乳液主要用于亲脂性药物递送(79.4%),通过水包油型微乳液和非离子表面活性剂(90%)进行口服或局部给药。癌症是最主要的靶向疾病状态,其次是炎症性疾病、微生物感染和心血管疾病。该分析的主要概括包括:1)尽管自1943年发现微乳液药物递送以来已有超过1200篇相关出版物,但微乳液配方在很大程度上仍基于反复试验;2)使用包括界面张力、液滴大小、电导率、浊度和粘度等方法进行表征可能会提供更多信息,以提高预测性;3)微乳液药物递送的出版物主要来自中国(27%)和印度(21%),这表明其他地方还有更多的研究机会。

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