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Journal of Chinese Pharmaceutical Sciences ›› 2014, Vol. 23 ›› Issue (8): 558-564.DOI: 10.5246/jcps.2014.08.072

• Original articles • Previous Articles     Next Articles

Preparation and characterization of sunitinib-loaded microspheres for arterial embolization

Ziming Zhao, Jialin Li, Yongjie Yang, Daichao Cui, Xiaojing Lu, Tianyuan Fan*   

  1. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2013-11-06 Revised:2013-11-25 Online:2014-08-31 Published:2013-12-06
  • Contact: Tel.: 86-10-82805123
  • Supported by:
    State Key Projects (Grant No. 2009ZX09310-001).

Abstract:

Drug-loaded microspheres have been caused much attention in embotherapy in recent years. In this study, polyvinyl alcohol/acrylic acid microspheres were prepared by inverse suspension polymerization method. Sunitinib malate (SU) was used as a model drug and loaded on microspheres through ion-exchange mechanism. We investigated the characterization of blank microspheres (B-Ms) and sunitinib-loaded microspheres (SU-Ms) in vitro, including morphology, size distribution, equilibrium water content (EWC), elasticity, drug loading and drug release. The result showed that both B-Ms and SU-Ms were spherical withsmooth surface. The particle size of B-Ms and SU-Ms were both suitable for embolization. Compared with that of B-Ms, the EWC of SU-Ms was decreased and the rigidity of SU-Ms was increased. Drug loading and entrapment efficiency ofmicrospheres were mainly affected by the concentration of sunitinib solution than by the size of microspheres. SU-Ms exhibited a sustained release in phosphate buffer solution (PBS). Thus, the SU-Ms may have potential application for arterial embolization.                    

Key words: Microspheres, Embolization, Sunitinib, Sustained release

CLC Number: 

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