Department of Pharmacy Science, Binzhou Medical University, Yantai, 264003, China.
Sci Rep. 2019 Sep 20;9(1):13670. doi: 10.1038/s41598-019-50162-8.
β-CD-DPPE molecule was synthesized through the conjugation of β-CD-NH 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.
β-CD-DPPE 分子通过β-CD-NH 和 DPPE 分子的共轭连接合成,其水溶性优于传统的磷脂分子。β-CD-DPPE 分子在水溶液中形成球形胶束,通过将 Dox(阿霉素)载入胶束中制备β-CD-DPPE-Dox 纳米药物,载药量约为 82.3±7.27%。同时,纳米药物中的 Dox 释放行为具有持续释放和 pH 控制释放的特点,体外释放实验表明,较低 pH 值下的 Dox 释放速度快于正常 pH 值(pH=7.4),这表明在肿瘤微环境中的释放速度快于正常组织。生物学试验表明,胶束具有低细胞毒性,在相同 Dox 浓度下,β-CD-DPPE-Dox 纳米药物的细胞毒性低于 Dox,β-CD-DPPE-Dox 纳米药物能有效诱导癌细胞凋亡并抑制肿瘤生长。