Preparation and characterization of intestine PepT1-targeted calcium carbonate nanoparticles  

靶向小肠PepT1的碳酸钙纳米颗粒的制备与表征（英文）

作　　者：Yunqiang Deng Yao Jin Chuyu He Yang Zou Yuanhang Zhou Shidi Han Chuhang Zhou Qi Liu Xinru Li Yanxia Zhou Yan Liu 邓运强;靳尧;何楚瑜;邹洋;周远航;韩诗迪;周楚航;刘琦;李馨儒;周艳霞;刘艳(北京大学医学部药学院分子药剂学与新释药系统北京市重点实验室,北京100191)

机构地区：Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems,School of Pharmaceutical Sciences,Peking University Health Science Center,Beij ing 100191,China

出　　处：《Journal of Chinese Pharmaceutical Sciences》2018年第6期397-407,共11页中国药学（英文版）

基　　金：The National Natural Science Foundation of China(Grant No.81673366);the National Key Science Research Program of China(973 Program,Grant No.2015CB932100)

摘　　要：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.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。

关 键 词：Calcium carbonate nanoparticles Oligopeptide transporter Gly-Sar In vitro release Intestinal absorption 

分 类 号：R944[医药卫生—药剂学]