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Preparation of β-CD-DPPE-Dox Nanomedicine and Its’ Application as the Anticancer and Antitumor Drug

机译:β-CD-DPPE-Dox纳米药物的制备及其作为抗癌和抗肿瘤药的应用

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摘要

β-CD-DPPE molecule was synthesized through the conjugation of β-CD-NH2 and the DPPE molecule, and its’ water-solubility was more excellent than the traditional phospholipid molecule. The spherical micelles was formed by β-CD-DPPE molecule in aqueous solution, and the β-CD-DPPE-Dox nanomedicine can be prepared through loading Dox (Doxorubicin) into the micelles, and the Dox loading ratio was about 82.3 ± 7.27%. At the same time the Dox release behavior from the nanomedicine was sustained-release and pH controlled release, and the release test in vitro showed that the release rate of the Dox at the lower pH was faster than that of normal pH (pH = 7.4), which indicated that the rate of release in the tumor microenvironment is faster than in the normal tissue. Biological test showed that the micelles was low cytotoxicity, and the cytotoxicity of β-CD-DPPE-Dox nanomedicine was lower than the Dox under the same Dox concentration, and the β-CD-DPPE-Dox nanomedicine could effectively induce cancer cell apoptosis and inhibit the tumor growth.
机译:β-CD-DPPE分子是通过β-CD-NH2与DPPE分子的结合合成的,其水溶性比传统的磷脂分子优异。 β-CD-DPPE分子在水溶液中形成球形胶束,通过将Dox(阿霉素)加载到胶束中可以制备β-CD-DPPE-Dox纳米药物,Dox的加载率为约82.3±7.27% 。同时,纳米药物的Dox释放行为是缓释和pH控释,体外释放试验表明,较低pH值下Dox的释放速率比正常pH值(pH faster = 7.4)快。 ,这表明肿瘤微环境中的释放速率比正常组织中更快。生物学测试表明,在相同的Dox浓度下,胶束的细胞毒性较低,β-CD-DPPE-Dox纳米药物的细胞毒性低于Dox,且β-CD-DPPE-Dox纳米药物可有效诱导癌细胞凋亡并促进细胞凋亡抑制肿瘤的生长。

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