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Journal of Chinese Pharmaceutical Sciences ›› 2018, Vol. 27 ›› Issue (6): 397-407.DOI: 10.5246/jcps.2018.06.040

• Original articles • Previous Articles     Next Articles

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*   

  1. 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).

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

CLC Number: 

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