体内评价紫杉醇载药脂质纳米囊经静脉和口服给药在耐药肿瘤上的作用。
In vivo evaluation of paclitaxel-loaded lipid nanocapsules after intravenous and oral administration on resistant tumor.
机构信息
INSERM U1066 MINT, Micro et Nanomédecines Biomimétiques, LUNAM Université, 4 Rue Larrey, 49033 Angers, CEDEX 09, France.
出版信息
Nanomedicine (Lond). 2015 Mar;10(4):589-601. doi: 10.2217/nnm.14.124.
AIM & METHODS: The aim of the present work was to encapsulate paclitaxel (Ptx) in various lipid nanocapsules (LNCs) formulations and then to compare their pharmacokinetics and efficacy on a subcutaneous isograft model in rats.
RESULTS
Three different Ptx formulations were obtained. Drug payloads ranged from 1.32 to 3.62 mg Ptx/g of formulation. After oral administration the area under concentration-time curve was higher (p < 0.05) if Ptx was encapsulated, (1,2 Distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino(PEG)] (DSPE-PEG-NH2)) LNCs displaying the highest area under concentration-time curve (p < 0.05). Efficacy was better than control for standard LNCs after oral administration (p < 0.05) and for (DSPE-PEG-NH2) LNCs after intravenous administration. Despite good absorption, (DSPE-PEG-NH2) LNCs failed to remain efficient after oral route.
CONCLUSION
This study highlights the importance of efficacy studies paired to pharmacokinetic studies for nanomedicines.
目的与方法
本研究旨在将紫杉醇（Ptx）封装于不同的脂质纳米胶囊（LNC）制剂中，然后在大鼠皮下同种异体移植模型中比较其药代动力学和疗效。
结果
得到了三种不同的 Ptx 制剂。药物载药量范围为 1.32 至 3.62mg Ptx/g 制剂。口服后，药物浓度-时间曲线下面积（AUC）更高（p<0.05），如果 Ptx 被包封（1,2-二硬脂酰-sn-甘油-3-磷酸乙醇胺-N-[氨基（PEG）]（DSPE-PEG-NH2））LNCs 显示出最高的 AUC（p<0.05）。与口服标准 LNCs 相比，口服后（p<0.05）和静脉注射后（DSPE-PEG-NH2）LNCs 的疗效更好。尽管吸收良好，但（DSPE-PEG-NH2）LNCs 经口服途径后未能保持有效。
结论
本研究强调了对于纳米医学，将药效学研究与药代动力学研究相结合的重要性。
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