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目的:通过磁性阿霉素聚氰基丙烯酸正丁酯纳米粒(ADM-PBCA-MNPS)的制备,研究ADM-PBCA-MNPS的理化性质并分析该微粒药代动力学特点。方法:乳化聚合法合成磁性阿霉素聚氰基丙烯酸正丁酯纳米粒,观察纳米粒的物理形态;检测纳米粒的饱和磁化强度和药物的包封率、载药量,通过体内外实验探讨磁性纳米微粒的释药性。结果:合成的磁性阿霉素聚氰基丙烯酸正丁酯纳米粒(ADM-PBCA-MNPS)平均直径194.30 nm;纳米粒的饱和磁化强度为0.488 emu/g,药物包封率为89.63%,载药量为9.73%;在体外条件下ADM-PBCA-MNPS显示出良好的缓释性能,体内药-时数据符合二室模型,ADM-PBCA-MNPS在大鼠体内的血药浓度-时间曲线下面积(AUC)、达峰浓度(Cmax)、消除半衰期(T1/2Beta)、平均滞留时间(MRT)均明显大于游离阿霉素(F-ADM)(P<0.01)。结论:制备的磁性纳米粒溶液性质稳定,符合在机体血管中随循环流动而不会沉淀的条件。实验组药物可在体内外缓慢释放阿霉素,有较高的生物利用度。
OBJECTIVE: To study the physicochemical properties of ADM-PBCA-MNPS and to analyze the pharmacokinetics of ADM-PBCA-MNPS by preparing magnetic doxorubicin-loaded polybutylcyanoacrylate nanoparticles (ADM-PBCA-MNPS). Methods: The magnetic doxorubicin polybutylcyanoacrylate nanoparticles were synthesized by emulsion polymerization. The physical morphology of the nanoparticles was observed. The saturation magnetization, encapsulation efficiency and drug loading of the nanoparticles were measured. Release of Magnetic Nanoparticles. Results: The average diameter of the synthesized doxorubicin-loaded polybutylcyanoacrylate nanoparticles (ADM-PBCA-MNPS) was 194.30 nm. The saturation magnetization of the nanoparticles was 0.488 emu / g and the entrapment efficiency was 89.63% The drug dose was 9.73%. ADM-PBCA-MNPS showed good sustained-release properties in vitro. The in vivo drug-time data conformed to the two-compartment model. The plasma concentration-time curve of ADM-PBCA-MNPS in rats AUC, Cmax, T1 / 2Beta, and MRT were significantly higher than those of free ADM (P <0.01). CONCLUSION: The prepared magnetic nanoparticle solution is stable in nature and conforms to the condition of circulating in the body blood vessel without sedimentation. The experimental group of drugs can slowly release doxorubicin in vivo and in vitro, with high bioavailability.