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环孢素A微球的体外释放影响因素

赵彬, 杨丽娟, 王坚成*, 张强   

  1. 北京大学药学院 药剂学系, 北京 100083
  • 收稿日期:2007-04-20 修回日期:2007-11-10 出版日期:2007-12-15 发布日期:2007-12-15
  • 通讯作者: 王坚成*

Studies on in vitro release of cyclosporine A-loaded microspheres

Bin Zhao, Li-Juan Yang, Jian-Cheng Wang*, Qiang Zhang   

  1. Department of Pharmaceutics, school of Pharmaceutical Sciences, Peking University, 100083 Beijing
  • Received:2007-04-20 Revised:2007-11-10 Online:2007-12-15 Published:2007-12-15
  • Contact: Jian-Cheng Wang*

摘要: 目的 以环孢素A为模型药, 使用生物可降解材料乳酸/羟基乙酸PLGA制备微球。并评价微球的体外释放。 方法 使用乳化溶剂挥发法制备环孢素微球, 并对微球的外观, 粒径和载药量进行评价。通过衡量温度, pH值和表面活性剂等因素筛选体 外释放介质。结果 制得的微球外观圆整, 粒径统, 平均粒径50 μm左右, 载药量为13%DSC结果表明环孢素APLGA有结合作用。体外释放实验表明微球的释放受温度, pH值和表面活性剂的影响, 加入30%的异丙醇可使微球在2周内释放完全。结论 乳化溶剂挥发法可制备得到质量符合要求的环孢素微球, 30%异丙醇的释放介质是微球体外释放评价的理想介质。

关键词: 环孢素A CyA, 环孢素A CyA, 环孢素A CyA, 微球 Ms, 微球 Ms, 微球 Ms, PLGA, PLGA, PLGA, 体外释放, 体外释放, 体外释放

Abstract:

Aim This study was to prepare cyclosporine A (CyA) microspheres (Ms) using 75:25 poly (D, L-lactide-co-glycolide) polymer (PLGA), and to evaluate the in vitro release of the CyA microspheres. Methods CyA-Ms were prepared by an oil-in-water (o/w) emulsion solvent extraction/evaporation process and characterized for drug content, particle size, surface morphology, and differential scanning calorimeter (DSC). Accelerated in vitro release of cyclosporine A from the micropsheres was studied at various conditions, such as temperatures, surfactants, pH values and organic solvents for a short period. Results CyA-Ms were in spherical shape with average particle size of 50 μm and loading efficiency of 13.0%. The results of DSC measurements suggested that at the dry state, CyA did interact very strongly with the hydrophilic PLGA polymer. In vitro release test in various release medium showed slight increase of CyA-Ms release profiles under various conditions of temperatures, surfactants and pH values. However, dramatical increase of CyA-Ms release was seen in the medium containing 30% isopropanol. Conclusion It was demonstrated that CyA could be incorporated into polymeric Ms prepared from PLGA using a solvent evaporation technique. The release medium containing 30% isopropanol might be the ideal condition for CyA-PLGA microspheres in vitro quality control test.

Key words: Cyclosporine A CyA, Cyclosporine A CyA, Microspheres Ms, Microspheres Ms, PLGA, PLGA, In vitro release, In vitro release

中图分类号: 

Supporting: Foundation item: Science and Technology Program of Beijing (Grant No. D0205003040621).
*Corresponding author. Tel./fax: 86-10-82802683