a School of Pharmacy , Shenyang Pharmaceutical University , Shenyang , P. R. China.
b Beijing National Laboratory for Molecular Sciences, College of Chemistry and Molecular Engineering , Peking University , Beijing , P. R. China.
Drug Deliv. 2018 Nov;25(1):623-631. doi: 10.1080/10717544.2018.1440448.
We report a simple strategy to prepare Tween 60@2β-CD self-assembly vesicles in aqueous solution as a new drug delivery carrier for cancer chemotherapy. The spherical shape of vesicles was confirmed by transmission electron microscopy (TEM) and mean particle sizes were about 33.7 nm, as measured by dynamic light scattering, micro-IR results indicated that the self-assembly vesicles was driven by hydrogen bonding. Hydrophilic doxorubicin (DOX) was successfully loaded into the self-assembly vesicles with drug loading content of 7.85% and loading efficiency of 42%. In addition, an in vitro cytotoxicity study and cellular uptake assays demonstrated that the DOX-loaded Tween 60@2β-CD vesicles markedly enhanced the cellular uptake and cytotoxicity of DOX toward the Hela cells. Furthermore, when used to evaluate the in vivo therapeutic efficacy in mice bearing the breast cell line (4T1), DOX-loaded vesicles exhibited superior inhibition of tumor growth compared with the DOX solutions.
我们报告了一种简单的策略，即在水溶液中制备吐温 60@2β-CD 自组装囊泡作为癌症化疗的新药物输送载体。通过透射电子显微镜（TEM）证实了囊泡的球形形状，通过动态光散射测量，平均粒径约为 33.7nm，微红外结果表明自组装囊泡是由氢键驱动的。亲水性阿霉素（DOX）成功负载到自组装囊泡中，载药量为 7.85%，载药效率为 42%。此外，体外细胞毒性研究和细胞摄取实验表明，载 DOX 的 Tween 60@2β-CD 囊泡显著增强了 DOX 对 Hela 细胞的细胞摄取和细胞毒性。此外，当用于评估携带乳腺癌细胞系（4T1）的小鼠体内治疗效果时，与 DOX 溶液相比，载 DOX 的囊泡表现出优异的肿瘤生长抑制作用。
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