【摘要】 采用高温乳化蒸发-低温固化法制备9-硝基喜树碱(1)半固体脂质纳米粒,并考察其形态、粒径、包封率、z电位及大鼠静脉给药后体内药物动力学行为。结果表明,1半固体脂质纳米粒为圆形,具有明显可见的亲水性聚乙二醇“外壳”,粒径为223.3～249.1nm,包封率为77.9%～83.5%,z电位为-28.4～-22.2mV。分别用1半固体脂质纳米粒和溶液对大鼠静脉给药,体内药物动力学参数分别为:t1/2 (14.9±0.3)h和(1.2±0.6)h,AUC0～t(486±37)mg·h·L-1和(117±64)mg·h·L-1,MRT (19.3±0.7)h和(1.7±1.0)h。表明1半固体脂质纳米粒可延长体循环时间,提高生物利用度。更多还原

【Abstract】 Nitrocamptothecin(1)semi-solid lipid nanoparticles(SSLN)were prepared by emulsification at a hightemperature and solidification at a low temperature. The shape, particle size, encapsulation efficiency, z potential andpharmacokinetics in rats of 1 SSLN were investigated. The results showed that the prepared SSLN was spherical andcovered with PEG chain on the surface. The size of the particles was 223.3～249.1nm and encapsulation efficiency was77.9%～83.5%. The z potential was -28.4～-22.2mV. 1 SSLN and its solution were intravenously injected into rats,respectively. And their pharmacokinetic parameters were as follows: t1/2 (14.9±0.3)h and(1.2±0.6)h, AUC0～t(486±37)mg·h·L-1 and (117±64)mg·h·L-1, MRT (19.3±0.7)h and (1.7±1.0)h. It indicated that 1 SSLN couldprolong circulation time in blood and improve drug bioavailability.更多还原