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为了克服小肠上皮屏障,提高难溶性药物的小肠吸收,本研究制备了甘氨酰肌氨酸 (Gly-Sar) 修饰的靶向小肠寡肽转运体1 (Pep T1) 的碳酸钙纳米粒.首先成功合成了Gly-Sar与TPGS的偶联物,然后制备了载香豆素6 (C6) 的Gly-Sar修饰的碳酸钙纳米粒,其粒径约为193 nm,扫描电镜下可见其表面有丰富的裂纹,载药率为60.5％±5.9％.此外,经Gly-Sar修饰的碳酸钙纳米粒在跨膜转运过程中具有良好的载药稳定性,并能明显提高难溶性药物的小肠吸收.因此,靶向小肠Pep T1的碳酸钙纳米粒在难溶性药物的口服递送中具有潜在的优势.“,”To improve the oral absorption of poorly water-soluble drugs by overcoming the intestinal epithelium barrier, calcium carbonate nanoparticles targeting to intestine peptide transporter 1 (Pep T1) were fabricated by modification of the surface of calcium carbonate nanoparticles with Gly-Sar. Gly-Sar-conjugated TPGS was successfully synthesized and characterized, and coumarin 6-loaded Gly-Sar modified calcium carbonate nanoparticles were then prepared and characterized to have a nano-scaled size of about 193 nm in diameter, cracked surface morphology under a scanning electron microscope, and high drug loading efficiency (60.5±5.9) ％. Moreover, the Gly-Sar-modified calcium carbonate nanoparticles exhibited better drug loading stability during the process of their transcellular transport, and evidently enhanced intestinal absorption of poorly water-soluble agents. Therefore, the designed intestine Pep T1-targeted calcium carbonate nanoparticles might have a promising potential for oral delivery of poorly water-soluble drugs.