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Targeting Receptors, Transporters and Site of Absorption to Improve Oral Drug Delivery

机译：靶向受体，转运蛋白和吸收部位，以改善口服药物的递送

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Although the oral route of drug administration is the most acceptable way of self-medication with a high degree of patient compliance, the intestinal absorption of many drugs is severely hampered by different biological barriers. These barriers comprise of biochemical and physical components. The biochemical barrier includes enzymatic degradation in the gastrointestinal lumen, brush border and in the cytoplasm of the epithelial cells as well as efflux transporters that pump drug molecules from inside the epithelial cell back to the gastrointestinal lumen. The physical barrier consists of the epithelial cell membranes, tight junctions and mucus layer. Different strategies have been applied to improve the absorption of drugs after oral administration, which range from chemical modification of drug molecules and formulation technologies to the targeting of receptors, transporters and specialized cells such as the gut-associated lymphoid tissues. This review focuses specifically on the targeting of receptor-mediated endocytosis, transporters and the absorption-site as methods of optimizing intestinal drug absorption. Intestinal epithelial cells express several nutrient transporters that can be targeted by modifying the drug molecule in such a way that it is recognized as a substrate. Receptor-mediated endocytosis is a transport mechanism that can be targeted for instance by linking a receptor substrate to the drug molecule of interest. Many formulation strategies exist for enhancing drug absorption of which one is to deliver drugs at a specific site in the gastrointestinal tract where optimum drug absorption takes place.
机译：尽管口服药物途径是最可接受的自我药物治疗方式，并具有高度的患者依从性，但许多药物的肠道吸收受到不同生物屏障的严重阻碍。这些障碍包括生化和物理成分。生化屏障包括在胃肠腔，刷状边界和上皮细胞的细胞质中的酶促降解，以及将药物分子从上皮细胞内部泵回到胃肠腔的外向转运蛋白。物理屏障由上皮细胞膜，紧密连接和粘液层组成。口服给药后，已采用了不同的策略来改善药物的吸收，其范围从药物分子的化学修饰和配制技术到靶向受体，转运蛋白和专门细胞（例如与肠道相关的淋巴组织）。这篇综述专门针对受体介导的内吞作用，转运蛋白和吸收位点作为优化肠道药物吸收的方法。肠上皮细胞表达几种营养转运蛋白，这些转运蛋白可以通过修饰药物分子以使其被识别为底物的方式来靶向。受体介导的内吞作用是一种转运机制，例如可以通过将受体底物与目标药物分子连接来靶向。存在许多用于增强药物吸收的配制策略，其中一种策略是在发生最佳药物吸收的胃肠道的特定部位递送药物。

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