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
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  • 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).


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

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