Chinese Journal of Tissue Engineering Research ›› 2012, Vol. 16 ›› Issue (29): 5331-5335.doi: 10.3969/j.issn.2095-4344.2012.29.003

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Preparation and pharmacokinetics of brucine immuno-nanoparticles

Qin Jian-min1, Yang Lin1, Sa Zhong-qiu1, Huang Tao1, Sheng Xia2, Li Qi3, Yin Pei-hao1, Zhang Min1, Gao Ke-pan4, Chen Qing-hua4, Ma Jing-wei5, Shen He-bai5   

  1. 1Department of General Surgery,
    2Department of Pathology,
    3Department of Oncology, Putuo Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai 200062, China;
    4Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China;
    5Shanghai Normal University, Shanghai 200234, China
  • Received:2012-01-02 Revised:2012-05-09 Online:2012-07-15 Published:2012-07-15
  • About author:Qin Jian-min☆, Doctor, Chief physician, Department of General Surgery, Putuo Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai 200062, China jianminqin68@ hotmail.com

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Abstract:

BACKGROUND: Brucine is highly toxic and insoluble in water, as well as has narrow intravenous therapeutic window. The amount of poisoning and treatment is close. Therefore, brucine is limited in clinical treatment of liver cancer and other malignant tumors.
OBJECTIVE: To prepare the brucine immuno-nanoparticles and to observe the characteristics of the drug metabolism in vivo.
METHODS: Anionic polymerization and chemical modification technology were used to prepare carboxylated polyethylene glycol-poly lactic acid copolymer. Phacoemulsification technology was employed to prepare carboxylated polyethylene glycol-polylactic acid copolymer brucine nanoparticles. Then, chemical coupling technology was utilized to combine the anti-human alpha-fetoprotein monoclonal antibody with the polyethylene glycol-poly lactic acid copolymer brucine nanoparticles to prepare the brucine immuno-nanoparticles with immune targeting.
RESULTS AND CONCLUSION: Brucine immuno-nanoparticles showed uniform size with an average particle size of (249±77) nm and Zeta potential of (-18.7±4.19) mV. The encapsulation efficiency was (76.0±2.3)% and the drug load was (5.6±0.2)%. Brucine immuno-nanoparticles were very stable in the medium with an accumulative release rate of over 80% in 24 hours and 100% in 48 hours. Brucine immuno-nanoparticles belonged to non-compartment model during in vivo metabolic process. The half life period of brucine immuno-nanoparticles was (15.69±3.77) hours, which was longer than that of the brucine (P < 0.01). The brucine immuno-nanoparticles with immune targeting are successfully prepared that belong to non-compartment model during in vivo metabolic process, and show sustained-release properties.

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