文献:Lymphatic transport of orally administered probucol-loaded mPEG-DSPE micelles
作者:Limei Han,Qiushi Yang,Teng Shen,Jin Qing &Jianxin Wang
文献链接:https://www.tandfonline.com/doi/full/10.3109/10717544.2015.1028600#abstract
Objective: The formulation of polymer micelle was developed for probucol to improve its intestinal lymphatic transport.
Materials and methods: Methoxy-polyethylenelglycol-distearyl phosphatidyl-ethanolamine (mPEG-DSPE) polymer was chosen to develop the micelles for probucol. The physicochemical properties were characterized. Caco-2 cell model, unconscious and conscious lymph duct cannulated rat models were established for in vitro and in vivo evaluation of lymphatic transport.
Results: In vitro evaluation in the Caco-2 cell model showed that the micellar formulation could significantly increase the uptake and transport of probucol. The study in unconscious and conscious lymph duct cannulated rat models further verified the significant enhancement of lymphatic transport of probucol by mPEG-DSPE micelles.
Discussion and conclusion: These results suggested that mPEG-DSPE micellar formulation could provide a useful alternative approach for improving the lymphatic transport of hydrophobic compounds.
目的:研制普罗布考聚合物胶束制剂,以改善其肠道淋巴转运。
材料和方法:选择甲氧基聚乙二醇二硬脂基磷脂酰乙醇胺(mPEG-DSPE)聚合物开发普罗布考胶束。对其理化性质进行了表征。建立Caco-2细胞模型、无意识和有意识淋巴管插管大鼠模型,用于体外和体内淋巴转运评估。
结果:在Caco-2细胞模型中的体外评估表明,胶束制剂可以显著增加普罗布考的摄取和转运。在无意识和意识淋巴管插管大鼠模型中的研究进一步证实了mPEG-DSPE胶束对普罗布考淋巴转运的显著增强。
讨论和结论:这些结果表明,mPEG-DSPE胶束制剂可以为改善疏水性化合物的淋巴转运提供一种有用的替代方法。
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Cy7-PEG-DPPE
DSPE-PEG-Cy7
DSPE-PEG-cRGD
DPPE-PEG-cRGD
DMPE-PEG-cRGD
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DPPE-PEG-RGD
DMPE-PEG-RGD
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4-Arm PEG-DSPE
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