硫酸长春碱乳酸-羟基醋酸共聚物微球的处方和制备工艺研究

Effects of formulation factors on encapsulation efficiency and release profiles of vinblastine sulfate loaded microspheres

目的:制备硫酸长春碱生物可降解注射微球,考察处方和制备工艺对微球包封率及释放度的影响。方法:以乳酸-羟基醋酸共聚物(PLGA)为载体材料,分别采用O/O型和W/O/W乳化溶剂挥发法制备微球。结果:采用O/O型乳化溶剂挥发法制备的微球表面光滑无孔洞,内部结构致密;W/O/W型微球表面有较多皱褶,内部结构多孔。采用O/O型乳化溶剂挥发法制备的微球包封率在70%左右,明显高于W/O/W型乳化溶剂挥发法制备的微球,释药速度明显低于第2种方法制备的微球。采用O/O型乳化溶剂挥发法,以PLGA(50∶50.10000)制备的微球在体外可持续释药21d以上。结论:硫酸长春碱PLGA微球的制备工艺可行,缓释特征明显,无突释效应。

OBJECTIVE To study the effects of formulation factors on encapsulation efficiency and drug release profile of vinblastine sulfate loaded mierospheres. METHODS Vinblastine sulfate loaded microsphere was prepared with poly（lactic-co- glycolic acid） （PLGA） by O/O and W/O/W emulsion solvent evaporation method. RESULTS Drug loaded microspheres prepared by O/O emulsion solvent evaporation method showed a relative smooth surface and dense interior structures, while microspheres prepared by the latter method possessed rough surface with very porous interior structures. The encapsulation efficiency and drug release rate of mierospheres prepared by the first method was significant higher and faster than that of the microspheres prepared by the latter method. The microspheres prepared with PLGA（50：50. 10000） could sustain release for 21 days. CONCLUSION The preparation and the formulation of drug loaded microspheres is simple and available. The microspheres showed a good controlled release characteristics without burst release.