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微乳液体系:从设计和结构到建立多途径药物传递的新给药系统。

Microemulsion systems: from the design and architecture to the building of a new delivery system for multiple-route drug delivery.

机构信息

Federal University of Rio Grande Do Norte (UFRN), Department of Pharmacy, Dispersed Systems Laboratory (LaSiD), Natal, RN, Brazil.

São Paulo State University (UNESP), School of Pharmaceutical Sciences, Araraquara, SP, Brazil.

出版信息

Drug Deliv Transl Res. 2021 Oct;11(5):2108-2133. doi: 10.1007/s13346-020-00872-8. Epub 2020 Nov 8.

Abstract

Poorly soluble active pharmaceutical ingredients (APIs) create major problems in drug dosage form formulation resulting in significant delays in drug pharmaceutical screening, impairing the drug dosage form production. Aiming to minimize the use of excipients for increasing drug apparent solubility and, as a result, its bioavailability, exploration of innovative approaches is an earnest need. Microemulsion is an alternative drug delivery system that emerged as a valuable tool to achieve safe formulations for insoluble compounds and to improve their biopharmaceutical properties and pharmacokinetics. This review aims to present the state of the art of microemulsion systems, bringing an overview about their origin and how they can be properly produced and thoroughly characterized by different approaches. Furthermore, comments on regulatory issues regarding stability assessment and toxicity evaluation are discussed. The review concludes with a current opinion on microemulsion systems. The overall objective of this work was to describe all the potentialities of microemulsion systems as a drug carrier for therapeutic purposes, highlighting the unique features of this nanotechnological platform. Display Image.

摘要

难溶性药物活性成分(APIs)在药物剂型配方中会产生重大问题,导致药物筛选显著延迟,影响药物剂型生产。为了尽量减少赋形剂的使用以提高药物表观溶解度,并提高其生物利用度,探索创新方法是当务之急。微乳液是一种替代药物传递系统,它作为一种有价值的工具出现,可用于为不溶性化合物制备安全的配方,并改善其生物制药特性和药代动力学。本文旨在介绍微乳液系统的最新技术,概述其起源以及如何通过不同方法进行适当的生产和彻底的特性描述。此外,还讨论了关于稳定性评估和毒性评估的监管问题。本文最后对微乳液系统提出了当前的看法。这项工作的总体目标是描述微乳液系统作为治疗用途的药物载体的所有潜力,突出该纳米技术平台的独特特征。显示图片。

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