Ghaffari Fatemeh, Bahmanzadeh Maryam, Nili-Ahmadabadi Amir, Firozian Farzin
Department of Biology, College of Basic Science, Hamedan Branch, Islamic Azad University, Hamedan Branch, Hamedan, Iran. Email:
Asian Pac J Cancer Prev. 2018 Sep 26;19(9):2651-2655. doi: 10.22034/APJCP.2018.19.9.2651.
Objective: Paclitaxel (PTX) is a chemotherapeutic agent used for treating breast cancer. The study aimed to prepare PTX loaded dextran stearate (Dex-SA) and evaluate its efficacy against human breast cancer cell line MCF-7. Methods: Dex-SA/PTX micelles were prepared by dialysis method. The micelles size, zeta potential and particle size distribution were measured by dynamic laser light scattering method. Amount of loaded PTX on the polymer measured by HPLC. Release profiles of the drug from the micelles were obtained in buffer (phosphate pH=7.4). Then the cytotoxicity of blank micelles, Dex-SA/PTX micelles and free PTX were evaluated in the MCF-7 cells by MTT method. Result: Loading efficiency of PTX on the Dex-SA was measured about 84.24±9.07%. The smallest particles size was about 193.9±7.1 nm but the other formulation with larger particle size had better zeta potential (-33.5±6.74 mV). The drug release from the micelles was slowly and reached steady state after about 12 hours. The cytotoxicity experiment showed that Dex-SA/PTX micelles have more cytotoxicity compared to free PTX against MCF7 cell lines. Conclusions: Dex-SA polymeric micelle is a suitable carrier for hydrophobic cytotoxic drugs such as PTX.
紫杉醇（PTX）是一种用于治疗乳腺癌的化疗药物。本研究旨在制备负载紫杉醇的硬脂酸葡聚糖（Dex-SA）并评估其对人乳腺癌细胞系MCF-7的疗效。方法：采用透析法制备Dex-SA/PTX胶束。通过动态激光散射法测量胶束大小、zeta电位和粒径分布。用高效液相色谱法测定聚合物上负载的PTX量。在缓冲液（磷酸盐pH=7.4）中获得药物从胶束中的释放曲线。然后用MTT法在MCF-7细胞中评估空白胶束、Dex-SA/PTX胶束和游离PTX的细胞毒性。结果：PTX在Dex-SA上的负载效率约为84.24±9.07%。最小粒径约为193.9±7.1 nm，但其他粒径较大的制剂具有更好的zeta电位（-33.5±6.74 mV）。药物从胶束中缓慢释放，约12小时后达到稳态。细胞毒性实验表明，与游离PTX相比，Dex-SA/PTX胶束对MCF7细胞系具有更强的细胞毒性。结论：Dex-SA聚合物胶束是PTX等疏水性细胞毒性药物的合适载体。
