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目的制备单壁碳纳米管(SWNTs)靶向抗肿瘤药物载体,初步分析其药学特性和细胞学特性。方法功能化处理SWNTs后,在其表面负载各种生物活性分子,包括表面改性分子叶酸-聚乙二醇(PEG-FA)、抗肿瘤化疗药物阿霉素(DOX)以及荧光标记分子异硫氰酸荧光素(FITC),考察各生物分子负载情况及该药物载体的体外细胞学特性。结果酸处理及PEG-FA功能化后的SWNT能稳定分散于水中,长度为200~500 nm,浓度最高可达50μg.mL-1;DOX及FITC能在SWNTs表面稳定结合,最佳结合值pH7;药物载体能通过叶酸分子的靶向介导进入肿瘤细胞,较游离DOX有更强的体外抑癌效能。结论碳纳米管靶向抗肿瘤药物载体能靶向作用于肿瘤细胞,性状稳定,载药量可控,增加了化疗药物的抗癌活性。
Objective To prepare single-walled carbon nanotubes (SWNTs) targeting antitumor drug carrier and preliminary analysis of its pharmacological and cytological properties. Methods Functionalized SWNTs were loaded on their surface with various biologically active molecules, including surface-modified molecules folate-polyethylene glycol (PEG-FA), antitumor chemotherapeutic drug doxorubicin (DOX) Fluorescein cyanate (FITC), investigate the biomolecule loading situation and in vitro cytological characteristics of the drug carrier. Results The acid-treated and PEG-FA-functionalized SWNTs were stably dispersed in water with a length of 200-500 nm and a maximum concentration of 50 μg · mL-1. DOX and FITC could stably bind to the surface of SWNTs with the best pH7 ; Drug carriers can be introduced into tumor cells through the targeting of folic acid molecules and have stronger anti-cancer activity in vitro than DOX. CONCLUSION: CNTs-targeting antitumor drug carriers can target tumor cells in a targeted manner with controlled drug loading and increased anticancer activity of chemotherapeutic agents.