2-脱氧葡萄糖聚乳酸微球的制备及其体外释药性能的研究

目的采用W/O/O乳化溶剂挥发法制备2-脱氧葡萄糖聚乳酸微球(2-Deoxyglucoseloadedpoly(DL-lactide)microspheres,2DG-PLA-MS),并研究其体外释药性能。方法考察3个因素(即投药比、水丙酮体积比和丙酮液体石蜡体积比)对微球的粒径、载药量和包封率的影响,应用正交实验优选最佳制备工艺条件。结果2DG-PLA-MS的制备工艺稳定,重复性好,微球表面圆整,粒径分布均匀,微球平均粒径45μm,平均载药量为42.41%,平均包封率为72.63%。该微球在14d的药物累积释放率达82.96%。结论2DG-PLA-MS具有明显的缓慢释放作用,能够实现延长药物作用时间、减少给药次数、降低药用剂量和减少不良反应等作用。

Preparation and in vitro release behavior of poly(DL-lactide) microspheres contai-ning 2-deoxyglucose

Objective To study the method for preparing poly(DL-lactide)microspheres for 2-deoxyglucose by W/O/O emulsification solvent-evaporation process and to research its release behaviours in vitro.Methods Microspheres size,drug loading and incorporation efficiency were three main parameters effected the preparations of microspheres.The formulation parameters evaluated in this study included the weight ratio of 2-DG to PLA,the volume ratio of water to acetone,the volume ratio of acetone to liquid paraffin,and orthogonal design was used to optimize the formulation.Results The 2DG-PLA-MS was shown to have good spherical geometry,a smooth surface and suitable size distribution under scanning electronic micrographs.The average diameter of microspheres was 45 μm,drug loading was 42.41% and incorporation efficiency was 72.63%.The cumulative release rate was 82.96% after 14 d.Conclusion The 2DG-PLA-MS had distinct sustained release effect,and could prolong medicine action time,reduce the number of times of medicine,decrease the medicine dosage and the side effect,etc.