文獻(xiàn)：Design of pH-sensitive methotrexate prodrug-targeted curcumin nanoparticles for efficient dual-drug delivery and combination cancer therapy

文獻(xiàn)鏈接：https://www.tandfonline.com/doi/full/10.2147/IJN.S152312#d1e205

作者：Jiajiang Xie,Zhongxiong Fan,Yang Li,Yinying Zhang,Fei Yu,Guanghao Su

摘要：

Preparation and characterization of pH-sensitive DSPE-PEG-Imide-MTX assembling micellar nanoparticles loaded with CUR (MTX-Imine-M-CUR)

Because of inherent amphiphilicity, DSPE-PEG-Imine-MTX and DSPE-MPEG could spontaneously self-assemble into micellar nanoparticles (MTX-Imine-M) composed of an inner hydrophobic DSPE core and an outside hydrophilic PEG shell with a self-targeting prodrug corona when exposed to the aqueous solution. The CUR drug could be encapsulated within the hydrophobic core of MTX-Imine-M (MTX-Imine-M-CUR) through hydrophobic interactions. The MTX-Imine-M-CUR nanoparticles were characterized by dynamic light scattering (DLS) and transmission electron microscope (TEM). In addition, the M-CUR (nanocarriers were self-assembled by DSPE-MPEG) and the MTX-Amide-M-CUR (nanocarriers were self-assembled by DSPE-PEG-Amide-MTX and DSPE-MPEG) were fabricated as comparative formulations (Figure 1B). The TEM observation of all drug formulations (Figure 2A–C) confirmed the monodispersed spherical nanoparticles. With DLS measurement, all nanoparticles showed a mean hydrodynamic particle size of 20–30 nm with negative surface charge (Figure 2A–C), which might facilitate preventing potential aggregations via electrostatic repulsion and decrease the nonspecific interaction between nanoparticles and plasma protein/red blood cells. 

由于其固有的兩親性，當(dāng)暴露于水溶液中時(shí)，DSPE-PEG-Imine-MTX和DSPE-MPEG可以自發(fā)地自組裝成膠束納米粒子（MTX-Imine-M），該納米粒子由內(nèi)部疏水性DSPE核心和外部親水性PEG外殼組成，具有自靶向前藥冠。

CUR藥物可以通過(guò)疏水相互作用包封在MTX-Imine-M（MTX-Imine-M-CUR）的疏水核心內(nèi)。通過(guò)動(dòng)態(tài)光散射（DLS）和透射電子顯微鏡（TEM）對(duì)MTX-Imine-M-CUR納米粒子進(jìn)行了表征。

此外，M-CUR（納米載體由DSPE-MPEG自組裝）和MTX-酰胺-MCUR（納米粒子由DSPE-PEG-酰胺-MTX和DSPE-MPEG自行組裝）被制備為比較制劑。所有藥物制劑的TEM觀察證實(shí)了單分散的球形納米顆粒。通過(guò)DLS測(cè)量，所有納米粒子的平均流體動(dòng)力學(xué)粒徑為20-30nm，表面帶負(fù)電荷，這可能有助于通過(guò)靜電排斥防止?jié)撛诘木奂�，并減少納米粒子與血漿蛋白/紅細(xì)胞之間的非特異性相互作用。

相關(guān)推薦產(chǎn)品：

DSPE-PEG-SC

DSPE-PEG-SCM

DSPE-PEG-SG

DSPE-PEG-SH

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DSPE-PEG-SP2-AA

DSPE-PEG-SS

DSPE-PEG-TCO

DSPE-PEG-Tetrazine

DSPE-PEG-TMS

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