College of Pharmacy, Shandong University, Jinan 250012, PR China.
Int J Pharm. 2012 Oct 15;436(1-2):379-86. doi: 10.1016/j.ijpharm.2012.06.039. Epub 2012 Jun 23.
In this study, oridonin-loaded nanoparticles coated with galactosylated chitosan (ORI-GC-NP) were prepared for tumor targeting and their characteristics were evaluated for the morphologies, particle size and zeta potential. Oridonin-loaded nanoparticles (ORI-NP) without galactosylated chitosan were prepared as a control. The entrapment efficiency of ORI-GC-NP and ORI-NP were 72.15% and 85.31%, respectively. The in vitro drug release behavior from nanoparticles displayed biphasic drug release pattern with initial burst release and consequently sustained release. Next, the pharmacokinetics and tissue distribution of ORI-GC-NP, ORI-NP and ORI solution were carried out. Pharmacokinetic analysis showed that ORI-GC-NP and ORI-NP could prolong the drug plasma levels compared with ORI solution. Meanwhile, the distribution of ORI-GC-NP to liver was higher than that of ORI-NP and free drug. In conclusion, ORI-GC-NP, as a promising intravenous drug delivery system for ORI, could be developed as an alternative to the conventional ORI preparations.
在这项研究中，制备了载有冬凌草甲素的纳米粒，其表面包覆有半乳糖化壳聚糖（ORI-GC-NP），用于肿瘤靶向，并对其形态、粒径和 Zeta 电位进行了评价。同时，制备了不含半乳糖化壳聚糖的载冬凌草甲素纳米粒（ORI-NP）作为对照。ORI-GC-NP 的包封率为 72.15%，ORI-NP 的包封率为 85.31%。纳米粒的体外药物释放行为呈现出双相药物释放模式，具有初始突释和随后的持续释放。接下来，对 ORI-GC-NP、ORI-NP 和 ORI 溶液的药代动力学和组织分布进行了研究。药代动力学分析表明，与 ORI 溶液相比，ORI-GC-NP 和 ORI-NP 能够延长药物的血浆水平。同时，ORI-GC-NP 向肝脏的分布高于 ORI-NP 和游离药物。综上所述，ORI-GC-NP 作为一种有前途的冬凌草甲素静脉给药系统，可作为传统 ORI 制剂的替代品进行开发。
