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为克服小肠上皮这一药物口服吸收的主要屏障,进一步提高难溶药物的口服吸收,本研究设计并合成了偶联小肠上皮广泛分布的寡肽转运体PepT1的底物Gly-Sar的聚乙二醇-聚乳酸嵌段共聚物(Gly-Sar-PEG-b-PLA),制备并表征了靶向PepT1的聚合物胶束.用薄层色谱和核磁共振氢谱对其结构进行了确证和表征,用凝胶渗透色谱测定聚合物的分子量为5954 g/mol,多分散性指数为1.34.由Gly-Sar-PEG-b-PLA制备的载DiI的聚合物胶束的粒径为40.36 nm,多分散性指数为0.294,透射电镜观察胶束呈规则的球形,载药量为0.076％.此外,所制备的靶向PepT1的聚合物胶束增强了难溶药物的小肠吸收.因此,其在难溶药物的口服递送方面具有一定的潜力.“,”To overcome the main barrier of intestinal epithelium for the oral absorption of poorly water-soluble drugs and further improve their oral absorption,Gly-Sar,the substrate of the oligopeptide transporter PepT1 widely distributed in the small intestine,conjugated poly(ethylene glycol)-block-poly(D,L-lacfide) (Gly-Sar-PEG-b-PLA) was designed and synthesized,and PepTl-targeted polymeric micelles were prepared and characterized.The structure of the synthesized Gly-Sar-PEG-b-PLA was confirmed by use of TLC and 1H-NMR.The average molecular weight measured by GPC was 5954 g/mol with PDI of 1.34.The DiI-loaded polymeric micelles from Gly-Sar-PEG-b-PLA with drug loading content of 0.076％ were characterized to exhibit 40.36 nm in diameter with PDI of 0.294,and well-defined spherical shape observed by TEM.Furthermore,the PepT1-targeted polymeric micelles profoundly enhanced intestinal absorption of poorly water-soluble drug.Therefore,the designed PepTl-targeted polymeric micelles might have a promising potential for oral delivery of water-insoluble drugs.