Chinese Journal of Tissue Engineering Research ›› 2010, Vol. 14 ›› Issue (21): 3856-3860.doi: 10.3969/j.issn.1673-8225.2010.21.013　

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Preparation, characterization and drug stability of poly (lactic-co-glycolic acid) microspheres containing docetaxel

Cai Min-xian1, Chen Zhi-kui1, Lin Li-wu1, Xue En-sheng1, Lai Yuan-fa2, Zhou Xiao-ling3, Yang Jing4, Wei Hong-fen5   

  1. 1 Department of Ultrasound, 3 Central Laboratory, 4 Department of Pharmacy, Affiliated Union Hospital, Fujian Medical University, Fuzhou 350001, Fujian Province, China; 2 Fujian Provincial Institute for Drug Control, Fuzhou 350001, Fujian Province, China; 5 Ultrasonic Medicine Institute of Fujian Province, Fuzhou 350001, Fujian Province, China
  • Online:2010-05-21 Published:2010-05-21
  • Contact: Lin Li-wu, Professor, Department of Ultrasound, Affiliated Union Hospital, Fujian Medical University, Fuzhou 350001, Fujian Province, China llwus@163.com
  • About author:Cai Min-xian★, Studying for master’s degree, Department of Ultrasound, Affiliated Union Hospital, Fujian Medical University, Fuzhou 350001, Fujian Province, China cmx1980@21cn.com
  • Supported by:

    the Natural Science Foundation of Fujian Province, No. 2009J05066*

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Abstract:

BACKGROUND: Docetaxel injection and the solubilizer Tween 80 have a variety of side effects, while poly (lactic-co-glycolic acid) (PLGA) microspheres containing docetaxel used as interstitial chemotherapy can not only promote the drug concentration, but also reduce systemic toxicity.
OBJECTIVE: To prepare sustained-release PLGA microspheres containing docetaxel for tumor interstitial chemotherapy, and investigate the physiochemical properties, in vitro release, and drug stability.
MEHTODS: Sustained-release PLGA microspheres containing docetaxel were prepared by solvent evaporation method; thereafter, morphology and particle size were measured by scanning electron microscope, while drug loading, encapsulation efficiency, and in vitro release were examined by HPLC. The microspheres were performed with irradiation sterilization of 5, 15, 25 kGy 60Co. The effects of irradiation sterilization were examined.
RESULTS AND CONCLUSION: Drug-loaded microspheres were round, smooth, and well scattered, with the mean diameter of 23.1 µm. The optimal drug loading rate (4.82%) and encapsulation efficiency (96.3%) were gained when the feed ratio of PLGA to docetaxel was 100 mg/5 mg. The cumulative release of docetaxel from microspheres was 81.6% within 4 weeks without occurrence of burst release, and docetaxel encapsulated in microspheres, detected by HPLC, kept stability of structure. No bacillus pumilus colony was cultured in microspheres after irradiation at three dosages of 60Co. Sustained-release PLGA microspheres containing docetaxel were successfully prepared by solvent evaporation method with optimal particle size and encapsulation efficiency, suitable release period, and high drug stability.

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