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基于脂质的系统作为提高难溶性药物生物利用度的一种有前景的方法。

Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs.

作者信息

Cerpnjak Katja, Zvonar Alenka, Gašperlin Mirjana, Vrečer Franc

出版信息

Acta Pharm. 2013 Dec;63(4):427-45. doi: 10.2478/acph-2013-0040.

Abstract

Low oral bioavailability as a consequence of low water solubility of drugs is a growing challenge to the development of new pharmaceutical products. One of the most popular approaches of oral bioavailability and solubility enhancement is the utilization of lipid-based drug delivery systems. Their use in product development is growing due to the versatility of pharmaceutical lipid excipients and drug formulations, and their compatibility with liquid, semi-solid, and solid dosage forms. Lipid formulations, such as self-emulsifying (SEDDS), self-microemulsifying SMEDDS) and self- -nanoemulsifying drug delivery systems (SNEDDS) were explored in many studies as an efficient approach for improving the bioavailability and dissolution rate of poorly water-soluble drugs. One of the greatest advantages of incorporating poorly soluble drugs into such formulations is their spontaneous emulsification and formation of an emulsion, microemulsion or nanoemulsion in aqueous media. This review article focuses on the following topics. First, it presents a classification overview of lipid-based drug delivery systems and mechanisms involved in improving the solubility and bioavailability of poorly water-soluble drugs. Second, the article reviews components of lipid-based drug delivery systems for oral use with their characteristics. Third, it brings a detailed description of SEDDS, SMEDDS and SNEDDS, which are very often misused in literature, with special emphasis on the comparison between microemulsions and nanoemulsions.

摘要

药物低水溶性导致的低口服生物利用度是新型药品开发中日益严峻的挑战。提高口服生物利用度和溶解度最常用的方法之一是利用脂质体药物递送系统。由于药用脂质辅料和药物制剂的多功能性以及它们与液体、半固体和固体剂型的兼容性,它们在产品开发中的应用正在增加。脂质制剂,如自乳化药物递送系统(SEDDS)、自微乳化药物递送系统(SMEDDS)和自纳米乳化药物递送系统(SNEDDS),在许多研究中被探索作为提高难溶性药物生物利用度和溶出速率的有效方法。将难溶性药物纳入此类制剂的最大优点之一是它们在水性介质中能自发乳化并形成乳液、微乳液或纳米乳液。这篇综述文章聚焦于以下主题。首先,它介绍了脂质体药物递送系统的分类概述以及提高难溶性药物溶解度和生物利用度所涉及的机制。其次,文章综述了口服脂质体药物递送系统的成分及其特性。第三,它详细描述了SEDDS、SMEDDS和SNEDDS,这些在文献中经常被误用,特别强调了微乳液和纳米乳液之间的比较。

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