Journal of Chinese Pharmaceutical Sciences ›› 2017, Vol. 26 ›› Issue (8): 574-581.DOI: 10.5246/jcps.2017.08.064

• Original articles • Previous Articles     Next Articles

Preparation, characterization and pharmacokinetics of 10-hydroxy-camptothecin nanosuspension

Yi Zhang1,2, Ying Zhan1,2, Ning Pang1,2, Yujie Liu1,2, Shixuan Cheng1,2, Ji Li1,2, Yitian Du1,2, Xianrong Qi1,2*   

  1. 1. Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
    2. Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery System, Peking University Health Science Center, Beijing 100191, China
  • Received:2017-04-21 Revised:2017-05-14 Online:2017-08-31 Published:2017-05-22
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  • Supported by:

    NSFC (Grant No. 81473156, 81673365) and Fangzheng Foundation for funding of the work.


10-Hydroxycamptothecin (HCPT) is a broad-spectrum anticancer drug, while its low solubility and instability severely limit its application. In this study, HCPT nanosuspension (HCPT-NSP), also known as nanocrystal, was prepared by micro-precipitationcombined with high-pressure homogenization method. This nanosuspension was characterized by size, shape, zeta potential, drug loading efficiency and in vitro drug release behavior. Preferred formulation and process showed that particle size was (129.8±13.9) nm, PDI was 0.20±0.07, and drug loading efficiency was 36.5%±9.5%. Moreover, HCPT nanocrystal concentration reached(1.35±0.2) mg/mL in HCPT-NSP, which was more than 1000-fold higher than that of HCPT. Transmission electron microscopy (TEM) results showed that the nanosuspension was short rod in shape. X-ray powder diffraction (XRD), thermogravimetric analysis (TGA), derivative thermogravimetric analysis (DTA) and differential scanning calorimetry (DSC) further elaborated the crystal state of the HCPT. The drug concentration-time curve of HCPT-NSP in rats was in accordance with the three-compartment model, showing prolonged half-life. Taken together, our data suggested that HCPT-NSP was a promising drug delivery system.

Key words: 10-Hydroxycamptothecin, Nanosuspension, Nanocrystal, High-pressure homogenization, Pharmacokinetics

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