Abstract
The application of lipid-based drug delivery systems on the industrial scale has successfully demonstrated their therapeutic and manufacturing advantages. Recently, various lipid-based formulations were successfully prepared for oral delivery of compounds that are difficult to administer. Nevertheless, an improved understanding of how these formulations affect drug absorption and metabolism is required to support the rapid and successful completion of drug development programs. In this review, we report the detailed mechanisms whereby lipids and lipid-based excipients affect drug absorption and metabolism, and summarize the capacity of lipids and lipid-based formulations to improve drug absorption by improving drug solubility, mucosa penetration, lymphatic transport, and hepatic metabolism. Finally, we discuss the progress made toward the use of novel lipid formulations to enhance oral absorption by surmounting specific absorption barriers.
Keywords: Absorption, lipid formulations, metabolism, poorly soluble drug, systemic exposure.
Current Drug Metabolism
Title:Lipid-Based Formulations for Oral Drug Delivery: Effects on Drug Absorption and Metabolism
Volume: 16 Issue: 3
Author(s): Quanlei Zhu, Xiuying Li, Dengning Xia, Hongzhen Yu, Dan Chen, Weiwei Fan and Yong Gan
Affiliation:
Keywords: Absorption, lipid formulations, metabolism, poorly soluble drug, systemic exposure.
Abstract: The application of lipid-based drug delivery systems on the industrial scale has successfully demonstrated their therapeutic and manufacturing advantages. Recently, various lipid-based formulations were successfully prepared for oral delivery of compounds that are difficult to administer. Nevertheless, an improved understanding of how these formulations affect drug absorption and metabolism is required to support the rapid and successful completion of drug development programs. In this review, we report the detailed mechanisms whereby lipids and lipid-based excipients affect drug absorption and metabolism, and summarize the capacity of lipids and lipid-based formulations to improve drug absorption by improving drug solubility, mucosa penetration, lymphatic transport, and hepatic metabolism. Finally, we discuss the progress made toward the use of novel lipid formulations to enhance oral absorption by surmounting specific absorption barriers.
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Cite this article as:
Zhu Quanlei, Li Xiuying, Xia Dengning, Yu Hongzhen, Chen Dan, Fan Weiwei and Gan Yong, Lipid-Based Formulations for Oral Drug Delivery: Effects on Drug Absorption and Metabolism, Current Drug Metabolism 2015; 16 (3) . https://dx.doi.org/10.2174/138920021603150812121453
DOI https://dx.doi.org/10.2174/138920021603150812121453 |
Print ISSN 1389-2002 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5453 |
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