靶向小肠PepT1的碳酸钙纳米颗粒的制备与表征

doi:10.5246/jcps.2018.06.040

中国药学(英文版) ›› 2018, Vol. 27 ›› Issue (6): 397-407.DOI: 10.5246/jcps.2018.06.040

靶向小肠PepT1的碳酸钙纳米颗粒的制备与表征

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

收稿日期:2018-04-23 修回日期:2018-05-10 出版日期:2018-06-30 发布日期:2018-05-17
通讯作者: Tel.: +86-010-82801508, E-mail: yanliu@bjmu.edu.cn
基金资助:
The National Natural Science Foundation of China (Grant No. 81673366) and the National Key Science Research Program of China (973 Program, Grant No. 2015CB932100).

Preparation and characterization of intestine PepT1-targeted calcium carbonate nanoparticles

Yunqiang Deng, Yao Jin, Chuyu He, Yang Zou, Yuanhang Zhou, Shidi Han, Chuhang Zhou, Qi Liu, Xinru Li, Yanxia Zhou, Yan Liu^*

Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China

Received:2018-04-23 Revised:2018-05-10 Online:2018-06-30 Published:2018-05-17
Contact: Tel.: +86-010-82801508, E-mail: yanliu@bjmu.edu.cn
Supported by:
The National Natural Science Foundation of China (Grant No. 81673366) and the National Key Science Research Program of China (973 Program, Grant No. 2015CB932100).

摘要/Abstract

摘要：

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(PepT1)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PepT1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: 碳酸钙纳米粒, 寡肽转运体, 甘氨酰肌氨酸, 体外释放, 小肠吸收

Abstract:

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 (PepT1) 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-scaledsize 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 PepT1-targeted calcium carbonate nanoparticles might have a promising potential for oral delivery of poorly water-soluble drugs.

Key words: Calcium carbonate nanoparticles, Oligopeptide transporter, Gly-Sar, In vitro release, Intestinal absorption

中图分类号:

R944

Supporting:

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. 靶向小肠PepT1的碳酸钙纳米颗粒的制备与表征[J]. 中国药学(英文版), 2018, 27(6): 397-407.

Yunqiang Deng, Yao Jin, Chuyu He, Yang Zou, Yuanhang Zhou, Shidi Han, Chuhang Zhou, Qi Liu, Xinru Li, Yanxia Zhou, Yan Liu . Preparation and characterization of intestine PepT1-targeted calcium carbonate nanoparticles[J]. Journal of Chinese Pharmaceutical Sciences, 2018, 27(6): 397-407.

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靶向小肠PepT1的碳酸钙纳米颗粒的制备与表征

Preparation and characterization of intestine PepT1-targeted calcium carbonate nanoparticles

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