Chinese Journal of Tissue Engineering Research ›› 2012, Vol. 16 ›› Issue (34): 6339-6342.doi: 10.3969/j.issn. 2095-4344.2012.34. 015

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Preparation and characterization of hepatocyte-targeting liposome containing hydroxycamptothecin

Zhang Xiu-juan1, Ke Li-ming1, Yang Jing2, Lin Li-wu1,3, Xue En-sheng1,3, Yu Li-yun1,3, Chen Zhi-kui1,3   

  1. 1福建医科大学附属协和医院，1超声科，
    2药学部，福建省福州市 350001；
    3福建省超声医学研究所，福建省福州市 350001
  • Received:2012-01-04 Revised:2012-02-17 Online:2012-08-19 Published:2012-08-19
  • Contact: Chen Zhi-kui, Doctor, Associate chief physician, Department of Ultrasound, Affiliated Union Hospital of Fujian Medical University, Fuzhou 350001, Fujian Province, China; Ultrasound Medical Institute of Fujian Province, Fuzhou 350001, Fujian Province, China jimchen2003@ 163.com
  • About author:Zhang Xiu-juan★, Studying for master’s degree, Physician, Department of Ultrasound, Affiliated Union Hospital of Fujian Medical University, Fuzhou 350001, Fujian Province, China jenifer81@126.com

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Abstract:

BACKGROUND: Because of poor water solubility of hydroxycamptothecin, carboxylic acid salt that is formed by opening lactone ring is mostly used in clinic. Hydroxycamptothecin widely distributes in all kinds of the tissues and the organs in vivo following intravenous injection, which will result in serious toxicity and side effects.
OBJECTIVE: To prepare a hepatocyte-targeting liposome containing hydroxycamptothecin to improve its water solubility and local drug concentration in tumor.
METHODS: The hepatocyte-targeting liposome containing hydroxycamptothecin was prepared by thin film dispersion- high pressure homogeneous method. Its morphology was examined by scanning electron microscope. The particle size, distribution and zeta potential were measured by laser scattering instrument. The encapsulation efficiency and in vitro release period were measured by high-performance liquid chromatography.
RESULTS AND CONCLUSION: The prepared liposome was spherical with a mean size of 205.6 nm, dispersion coefficient of 0.39, and zeta potential of -38.6 mV. The encapsulation efficiency was 78.1%, and the in vitro cumulative release rate was 83.5% within 48 hours. The above results indicate that thin film dispersion-high pressure homogeneous method can prepare an ideal hepatocyte-targeting liposome containing hydroxycamptothecin, which has even particle, high encapsulation efficiency and stable release.

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