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基于可生物降解的两亲性 ε-己内酯和碳酸酯共聚物的载抗癌药物纳米球。

Anticancer drug-loaded nanospheres based on biodegradable amphiphilic ε-caprolactone and carbonate copolymers.

机构信息

School of Material Science and Engineering, Wuhan Institute of Technology, Wuhan, China.

出版信息

Pharm Res. 2010 Dec;27(12):2743-52. doi: 10.1007/s11095-010-0275-7. Epub 2010 Sep 22.

DOI:10.1007/s11095-010-0275-7
PMID:20859660
Abstract

PURPOSE

The aim was to investigate anticancer drug-loaded poly(carbonate-ester) nanospheres as potential drug delivery systems for cancer therapy.

METHODS

Functional poly(carbonate-ester) copolymers (HPCP-SD) were synthesized by the incorporation of sulfadiazine as the tumor-targeting groups to hydroxyl groups of poly(carbonate-ester) copolymers. Two types of anticancer drug-loaded poly(carbonate-ester) nanospheres I and II were further prepared by dialysis method and high-voltage electrostatic field-assisted atomization, respectively, using HPCP-SD as polymeric carriers. These carriers and anticancer drug-loaded nanospheres were characterized, and their properties in vitro and in vivo were evaluated.

RESULTS

These anticancer drug-loaded poly(carbonate-ester) nanospheres had steady drug release rates and good controlled release properties. Moreover, anticancer drug-loaded poly(carbonate-ester) nanospheres II had faster drug release rates than those of anticancer drug-loaded nanospheres I. These anticancer drug-loaded nanospheres possessed lower cytotoxicity to HEK 293 cells and exhibited obviously higher anticancer efficiencies to the HeLa tumor cells than that of 5-fluorouracil. Anticancer drug-loaded nanospheres I possessed lower cytotoxicity to HEK 293 cells and higher anticancer activity to HeLa cells than those of anticancer drug-loaded nanospheres II.

CONCLUSIONS

These anticancer drug-loaded poly(carbonate-ester) nanospheres showed the potential as drug delivery systems for cancer therapy.

摘要

目的

研究载抗癌药物的聚（碳酸酯-酯）纳米球作为癌症治疗的潜在药物传递系统。

方法

通过将磺胺嘧啶作为肿瘤靶向基团掺入到聚（碳酸酯-酯）共聚物的羟基中来合成功能化的聚（碳酸酯-酯）共聚物（HPCP-SD）。进一步分别通过透析法和高压静电场辅助雾化法，使用 HPCP-SD 作为聚合物载体制备两种载抗癌药物的聚（碳酸酯-酯）纳米球 I 和 II。对这些载体和载抗癌药物的纳米球进行了表征，并评估了它们的体外和体内性质。

结果

这些载抗癌药物的聚（碳酸酯-酯）纳米球具有稳定的药物释放率和良好的控制释放性能。此外，载抗癌药物的聚（碳酸酯-酯）纳米球 II 比载抗癌药物的纳米球 I 具有更快的药物释放速率。这些载抗癌药物的纳米球对 HEK 293 细胞的细胞毒性较低，对 HeLa 肿瘤细胞的抗癌效率明显高于 5-氟尿嘧啶。载抗癌药物的纳米球 I 对 HEK 293 细胞的细胞毒性较低，对 HeLa 细胞的抗癌活性高于载抗癌药物的纳米球 II。

结论

这些载抗癌药物的聚（碳酸酯-酯）纳米球显示出作为癌症治疗的药物传递系统的潜力。

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