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首页> 外文期刊>RSC Advances >Paclitaxel prodrug based mixed micelles for tumor-targeted chemotherapy
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Paclitaxel prodrug based mixed micelles for tumor-targeted chemotherapy

机译：基于紫杉醇前药的混合胶束用于肿瘤靶向化疗

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An effective chemotherapy is usually subject to an insufficient loading of hydrophobic drugs as well as severe side effects. In order to address these dilemmas in one formulation, we herein construct paclitaxel prodrug based mixed micelles (MMs) for tumor-targeted chemotherapy. The paclitaxel prodrug containing a hydrophobic PTX and a hydrophilic PEG chain can self-assemble into uniform MMs with distearoyl phosphoethanolamine–polyethylene glycol–folate (DSPE–PEG–FA). The resultant MMs with preferable stability and hemolysis compatibility could improve the cellular uptake of nanoparticles via FA receptor-mediated endocytosis as compared to the single micelles (SMs). This tumor targetability was also confirmed in vivo by fluorescent imaging. MMs with a stable drug loading as well as tumor targetability displayed elevated in vitro cytotoxicity and in vivo antitumor efficacy compared with Taxol, which could be a potential formulation for cancer therapy.
机译：有效的化学疗法通常承受疏水性药物的不足负荷以及严重的副作用。为了解决一种制剂中的这些难题，我们在此构建了基于紫杉醇前药的混合胶束（MM），用于肿瘤靶向化疗。含有疏水性PTX和亲水性PEG链的紫杉醇前药可以与二硬脂酰基磷酸乙醇胺-聚乙二醇-叶酸（DSPE-PEG-FA）自组装成均一的MM。与单个胶束（SMs）相比，具有较好稳定性和溶血相容性的所得MMs可通过FA受体介导的内吞作用改善纳米粒对细胞的摄取。还通过荧光成像体内证实了这种肿瘤的可靶向性。与紫杉醇相比，具有稳定载药量和肿瘤靶向性的MM具有更高的体外细胞毒性和体内抗肿瘤功效，这可能是一种潜在的癌症治疗方法。

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