Journal of Peking University(Health Sciences) ›› 2014, Vol. 46 ›› Issue (4): 629-634.

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Preparation and property study of doxorubicin loaded microspheres

SA Er-a1,LU Xiao-jing1,CUI Dai-chao1,GUAN Hai-tao2,LV Tian-shi2,ZHANG Shui-sheng2,YAN Zi-guang2,SONG Li2,ZOU Ying-hua2,FAN Tian-yuan1△   

  1. (1.Department of Pharmaceutics,Peking University School of Pharmaceutical Sciences,Beijing 100191,China;2.Department of Interventional Radiology and Vascular Surgery,Peking University First Hospital,Beijing 100034,China)
  • Online:2014-08-18 Published:2014-08-18

Abstract: Objective:
To prepare doxorubicin-loaded polyvinylalcohol-acrylic acid (PVA-AA) microspheres and evaluate properties of this chemoembolic agent. Methods: PVA-AA microspheres were synthesized by inverse suspension polymerization method and then verified by infrared spectroscopy. drug loading (DL) and entrapment efficiency (EE%) were measured after doxorubicinwas loaded on PVA-AA microspheres. Their morphology and elasticity were investigated by optical microscope,environmental scanning electron microscope and texture analyzer,respectively. T-cell apparatus was used to evaluate the in vitro release behavior of doxorubicin-loaded microspheres.The external carotid of the rabbit was chosen as an embolization site to evaluate the in vivo embolic property of the microspheres. Results:PVA-AA microspheres, which were transparent spheres,turned into red spheres after doxorubicin loading. DL of the microspheres was (20.56±0.69)g/L and (23.25±0.27)g/L,and EE% was 82.22%±2.76% and 93.00%±1.06% within 20 min and 6 h,respectively. The in vitro release results showed a significantly delayed release of the drug for 10.32%±0.47% after 24 h. The Young’s modulus was (178.30±12.33) kPa and (213.29±15.61) kPa for blank microspheres and doxorubicinloaded microspheres,respectively. Both blank microspheres and doxorubicinloaded microspheres exhibited good elasticity. In vivo embolization showed that 0.3 mL of microspheres could produce distal embolic efficiency. Conclusion:The doxorubicin-loaded microspheres are expected to be a promising new chemoembolic agent.

Key words: Doxorubicin, Microspheres, Chemoembolization, therapeutic, Ion exchange

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