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Galactosylated bovine serum albumin nanoparticles for parenteral delivery of oridonin: tissue distribution and pharmacokinetic studies

机译:半乳糖基化牛血清白蛋白纳米颗粒用于胃肠外注射冬凌草甲素:组织分布和药代动力学研究

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摘要

Bovine serum albumin (BSA) nanoparticle is a promising drug carrier system. Oridonin (ORI)-loaded galactosylated BSA nanoparticle (ORI-GB-NP) was prepared for liver targeting delivery of ORI. This work was designed to investigate the in vitro release, in vivo pharmacokinetics and tissue distribution of ORI-GB-NP. ORI-GB-NP was prepared by the desolvation method. The particle size of ORI-GB-NP was 172.0 +/- 8.3 nm with narrow size distribution. The in vitro release of ORI-GB-NP exhibited biphasic drug release pattern with an initial burst release and consequently sustained release. Pharmacokinetic analysis displayed that ORI-GB-NP and ORI-loaded BSA nanoparticle (ORI-BSA-NP) could enhance the drug plasma level and prolong the circulation time in contrast with ORI solution. Meanwhile, compared with ORI-BSA-NP, ORI-GB-NP could deliver more ORI to liver and simultaneously reduce the toxicity of ORI to heart, lung and kidney. In conclusion, ORI-GB-NP could be a promising drug delivery system for liver cancer therapy.
机译:牛血清白蛋白(BSA)纳米颗粒是一种有前途的药物载体系统。制备了含有Oridonin(ORI)的半乳糖基化BSA纳米颗粒(ORI-GB-NP),用于ORI的肝脏靶向递送。这项工作旨在研究O​​RI-GB-NP的体外释放,体内药代动力学和组织分布。通过去溶剂化方法制备ORI-GB-NP。 ORI-GB-NP的粒径为172.0 +/- 8.3 nm,粒径分布较窄。 ORI-GB-NP的体外释放表现出双相药物释放模式,具有初始爆发释放和因此的持续释放。药代动力学分析表明,与ORI溶液相比,ORI-GB-NP和ORI负载的BSA纳米颗粒(ORI-BSA-NP)可以提高药物血浆水平并延长循环时间。同时,与ORI-BSA-NP相比,ORI-GB-NP可以向肝脏输送更多的ORI,同时降低ORI对心脏,肺和肾脏的毒性。总之,ORI-GB-NP可能是有前途的肝癌治疗药物递送系统。

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