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首页> 外文期刊>Nanotechnology >PEG-PLA diblock copolymer micelle-like nanoparticles as all-trans-retinoic acid carrier: in vitro and in vivo characterizations
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PEG-PLA diblock copolymer micelle-like nanoparticles as all-trans-retinoic acid carrier: in vitro and in vivo characterizations

机译：PEG-PLA二嵌段共聚物胶束状纳米颗粒作为全反式维甲酸载体：体外和体内表征

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The purpose of this study was to characterize the properties in vitro, i.e. release, degradation, hemolytic potential and anticancer activity, and in vivo disposition of all-trans-retinoic acid (ATRA) in rats after administration of ATRA-loaded micelle-like nanoparticles. The amphiphilic block copolymers consisted of a micellar shell-forming mPEG block and a core-forming PLA block. The mPEG-PLA nanoparticles prepared by an acetone volatilization dialysis procedure were identified as having core-shell structure by H-1 NMR spectroscopy. Critical association concentration, drug contents, loading efficiency, particle size and xi potential were evaluated. The release of ATRA from the nanoparticles and the degradation of PLA were found to be mostly associated with the compositions of the nanoparticles. ATRA release was faster at smaller molecular weight of copolymer and lower drug contents. In vitro, the incorporation of ATRA in mPEG-PLA nanoparticles reduced the hemolytic potential of ATRA. Furthermore, anticancer activity of ATRA against HepG2 cell was increased by encapsulation, which showed an enhancement of tumor treatment of ATRA. In vivo, after intravenous injection to rats, the levels of ATRA in the blood stream and the bioavailability were higher for ATRA-loaded mPEG-PLA nanoparticles than those for ATRA solution. In conclusion, the structure of the mPEG-PLA diblock copolymer could be modulated to fit the demand of in vitro and in vivo characterizations of nanoparticles. The mPEG-PLA nanoparticles' loading ATRA have a promising future for injection administration.
机译：这项研究的目的是表征给予ATRA的胶束状纳米颗粒给药后大鼠体内的全反式维甲酸（ATRA）的释放，降解，溶血潜能和抗癌活性以及体内处置特性。 。两亲嵌段共聚物由形成胶束壳的mPEG嵌段和形成芯的PLA嵌段组成。通过H-1 NMR光谱鉴定通过丙酮挥发渗析程序制备的mPEG-PLA纳米颗粒具有核-壳结构。评估了临界缔合浓度，药物含量，负载效率，粒径和xi电位。发现ATRA从纳米颗粒的释放和PLA的降解主要与纳米颗粒的组成有关。在较小的共聚物分子量和较低的药物含量下，ATRA释放更快。在体外，在mPEG-PLA纳米颗粒中掺入ATRA降低了ATRA的溶血潜力。此外，通过包封增加了ATRA对HepG2细胞的抗癌活性，这表明ATRA的肿瘤治疗增强。在体内，向大鼠静脉内注射后，载有ATRA的mPEG-PLA纳米颗粒的血流中ATRA的水平和生物利用度均高于ATRA溶液。总之，可以调节mPEG-PLA二嵌段共聚物的结构，以适应纳米粒子体外和体内表征的需求。 mPEG-PLA纳米颗粒的负载ATRA在注射给药方面有广阔的前景。

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