紫杉醇纳米粒-微球系统的研制

发布时间：2018-10-08 15:01

【摘要】：目的制备紫杉醇纳米粒-微球系统(taxol nanoparticals-in-microsphere system,TAX-NiMS),并考察其体外释放特性。方法以聚乳酸-羟基乙酸共聚物(poly(lactic-co-glycolic acid),PLGA)为载体,采用乳化溶剂挥发法制备紫杉醇纳米粒(taxol nanoparticals,TAX-NPs)。以包封率、载药量及粒径为考察指标,采用单因素试验法优化处方。采用内源乳化凝胶法,以海藻酸钙为包裹材料,制备包覆TAX-NPs的微球系统。在扫描电镜和透射电镜下观察TAX-NiMS的表面和内部形态,并测定其粒径及体外释放特性。结果纳米粒优化处方:PLGA质量浓度为100 g·L-1,聚乙烯醇质量浓度为10 g·L-1,油相与水相体积比为1∶10,超声功率为300 W。微球优化处方:海藻酸钠(NaALG)质量浓度为15 g·L-1,Span-80质量浓度为10 g·L-1,Ca CO3与Na ALG质量比为1∶3,油相与水相体积比为1∶5。此条件下制备的TAX-NiMS的包封率、载药量和平均粒径分别为(84.33±1.11)%、(1.12±0.15)%和(2.678±0.014)μm。TAX-NiMS的12h释放量仅达到16.51%。结论 TAX-NiMS的制备方法稳定可控,且突释效应显著减小,为药物新剂型的开发提供了思路。
[Abstract]:Objective to prepare paclitaxel nanoparticles-microspheres system (taxol nanoparticals-in-microsphere system,TAX-NiMS) and investigate its release characteristics in vitro. Methods the paclitaxel nanoparticles (taxol nanoparticals,TAX-NPs) were prepared by emulsifying solvent volatilization with polylactic acid-glycolic acid copolymer (poly (lactic-co-glycolic acid) as the carrier. The encapsulation efficiency, drug loading and particle size were used to optimize the formulation. The microspheres coated with TAX-NPs were prepared using calcium alginate as encapsulation material by internal emulsifying gel method. The surface and internal morphology of TAX-NiMS were observed by SEM and TEM, and its particle size and release characteristics in vitro were measured. Results the optimized formulation was 100 g / L ~ (-1), 10 g / L ~ (-1) of polyvinyl alcohol, 1: 10 of volume ratio of oil to water, and 300 W of ultrasonic power. The optimized formulation of microspheres was as follows: the mass concentration of sodium alginate (NaALG) was 15 g / L ~ (-1) Span-80, the mass ratio of Ca CO3 to Na ALG was 1: 3, and the volume ratio of oil phase to water phase was 1: 5. The encapsulation efficiency, drug loading and average particle size of TAX-NiMS prepared under these conditions were (84.33 卤1.11) and (1.12 卤0.15)% and (2.678 卤0.014) 渭 m.TAX-NiMS, respectively. Conclusion the preparation method of TAX-NiMS is stable and controllable, and the effect of sudden release is significantly reduced, which provides a way for the development of new dosage forms of TAX-NiMS.
【作者单位】：河北科技大学化学与制药工程学院;
【基金】：河北省杰出青年科学基金项目(H2014208004)
【分类号】：R943

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