通过表面杂交 DSPE-PEG2000 来提高紫杉醇纳米晶体的全身循环。
Improving systemic circulation of paclitaxel nanocrystals by surface hybridization of DSPE-PEG2000.
机构信息
School of Pharmacy, Guilin Medical University, Guilin, 541004, China; School of Pharmacy, Institute of Nanotechnology and Health, Shanghai University of Medicine & Health Sciences, Shanghai, 201318, China.
School of Pharmacy, Institute of Nanotechnology and Health, Shanghai University of Medicine & Health Sciences, Shanghai, 201318, China.
出版信息
Colloids Surf B Biointerfaces. 2019 Oct 1;182:110337. doi: 10.1016/j.colsurfb.2019.06.066. Epub 2019 Jul 12.
This paper aims to improve the systemic circulation of paclitaxel (PTX) by modifying nanocrystals with DSPE-PEG 2000. PTX nanocrystals (PNCs) were prepared by an anti-solvent method and DSPE-PEG 2000 was inserted into PNCs by hybridization. The average size of DSPE-PEG-PNCs did not change obviously compared to the naked PNCs, but the negative charge increased after hybridization. The saturated attachment ratio of DSPE-PEG 2000 was 0.4%. In vitro release rate of DSPE-PEG-PNCs was significantly slower than that of PTX solution and the naked PNCs, which indicated that DSPE-PEG 2000 hindered the release of PTX. Moreover, pharmacokinetics results showed that DSPE-PEG-PNCs achieved a higher area-under-the-curve (AUC, 4.43 ± 0.19 mg/Lh) and lower clearance rate (1.08 ± 0.16 L/h/kg) compared to PNCs with an AUC of 2.48 ± 0.18 mg/Lh and a clearance rate of 1.89 ± 0.15 L/h/kg. Therefore, DSPE-PEG-PNCs could have a significant potential in clinical use by improving the systemic circulation of the drug.
本文旨在通过用 DSPE-PEG2000 修饰纳米晶体来提高紫杉醇（PTX）的全身循环。PTX 纳米晶体（PNCs）通过反溶剂法制备，并用杂交法将 DSPE-PEG2000 插入 PNCs。与裸 PNCs 相比，DSPE-PEG-PNCs 的平均粒径没有明显变化，但杂交后带负电荷增加。DSPE-PEG2000 的饱和附着比为 0.4%。DSPE-PEG-PNCs 的体外释放率明显慢于 PTX 溶液和裸 PNCs，表明 DSPE-PEG2000 阻碍了 PTX 的释放。此外，药代动力学结果表明，与 AUC 为 2.48±0.18mg/Lh、清除率为 1.89±0.15L/h/kg 的 PNCs 相比，DSPE-PEG-PNCs 的 AUC（4.43±0.19mg/Lh）更高，清除率（1.08±0.16L/h/kg）更低。因此，通过提高药物的全身循环，DSPE-PEG-PNCs 在临床应用中具有很大的潜力。
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