Zhu Quanlei, Li Xiuying, Xia Dengning, Yu Hongzhen, Chen Dan, Fan Weiwei, Gan Yong
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, NO. 501 Haike Road, Shanghai 201203, China.
Curr Drug Metab. 2015;16(3):200-10. doi: 10.2174/138920021603150812121453.
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.
基于脂质的药物递送系统在工业规模上的应用已成功证明了其治疗和制造优势。最近，已成功制备了各种基于脂质的制剂用于口服递送难以给药的化合物。然而，需要更好地了解这些制剂如何影响药物吸收和代谢，以支持药物开发项目的快速和成功完成。在本综述中，我们报告了脂质和基于脂质的辅料影响药物吸收和代谢的详细机制，并总结了脂质和基于脂质的制剂通过改善药物溶解度、粘膜渗透、淋巴转运和肝脏代谢来提高药物吸收的能力。最后，我们讨论了在使用新型脂质制剂克服特定吸收障碍以增强口服吸收方面取得的进展。
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