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Cai M.-X.,Fujian Medical University | Chen Z.-K.,Fujian Medical University | Lin L.-W.,Fujian Medical University | Xue E.-S.,Fujian Medical University | And 4 more authors.
Journal of Clinical Rehabilitative Tissue Engineering Research | Year: 2010

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.

Chen Z.-K.,Fujian Medical University | Cai M.-X.,Second Hospital of Longyan City | Yang J.,Fujian Medical University | Lin L.-W.,Fujian Medical University | And 5 more authors.
Medical Oncology | Year: 2012

To investigate the antiangiogenic effect of sustained-release poly (lactic-co-glycolic acid) microspheres containing docetaxel (PMCD) in human hepatoma xenograft. PMCD were prepared by solvent evaporation method with an encapsulation efficiency of 98.7% and a release period of about 3 weeks in vitro. PMCD were intratumorally injected once for mice bearing a human hepatocellular carcinoma. On day 21 post-treatment, the inhibition rate of tumor growth was 72.7% in the high-dose group, indicating a significant antitumor activity. Meanwhile, excellent antiangiogenic effect was observed based on the contrast-enhanced ultrasonography as well as microvessel density determination. Additionally, the realtime fluorescence quantitative PCR revealed that the expressions of vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), and angiopoietin-2 (Ang2) genes were down-regulated significantly. Interstitial chemotherapy using PMCD was highly effective and safe for the treatment of the human hepatoma xenograft and that decreasing angiogenesis could be one of the most important mechanisms involved in the antitumor activity. © 2011 Springer Science+Business Media, LLC.

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