Tabriz University of Medical Sciences, Liver and Gastrointestinal Diseases Research Center and Faculty of Pharmacy , Tabriz , Iran.
Expert Opin Drug Metab Toxicol. 2014 Jun;10(6):859-71. doi: 10.1517/17425255.2014.905543. Epub 2014 Apr 7.
There are many factors that can affect the absorption process of orally administered drugs. Intestinal transporters play an important role in drug absorption. These transporters are divided into two major classes: the solute carriers and the ATP-binding cassette (ABC) transporters. P-glycoprotein (P-gp), belonging to the ABC transporter superfamily, flushes out the substrate drugs from a cell, thus regulating the intestinal absorption of drugs.
This review gives a brief overview of uptake and efflux transporters localized in the intestine. However, because P-gp has been identified as an important underlying mechanism of drug interactions in humans, the review is strongly focused on summarizing the currently available data on the impact of P-gp for absorption of drugs.
The concomitant use of P-gp substrates and inhibitors (preferably in a single nanocarrier formulation) could be an effective and safe way to improve the bioavailability of drugs. It seems the study of P-gp and modulating its activity may be an interesting therapeutic goal to be considered in future research.
有许多因素会影响口服药物的吸收过程。肠道转运体在药物吸收中发挥着重要作用。这些转运体分为两大类：溶质载体和 ATP 结合盒（ABC）转运体。P 糖蛋白（P-gp）属于 ABC 转运体超家族，可将底物药物从细胞中冲洗出来，从而调节药物的肠道吸收。
本文综述了定位于肠道的摄取和外排转运体。然而，由于 P-gp 已被确定为人类药物相互作用的重要潜在机制，因此该综述重点总结了目前关于 P-gp 对药物吸收影响的可用数据。
同时使用 P-gp 底物和抑制剂（最好在单一纳米载体配方中）可能是提高药物生物利用度的有效且安全的方法。似乎研究 P-gp 并调节其活性可能是未来研究中值得考虑的一个有趣的治疗目标。
