Stem Cell Research Center, Tabriz University of Medical Sciences, Tabriz, Iran; Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
Mater Sci Eng C Mater Biol Appl. 2018 Nov 1;92:599-611. doi: 10.1016/j.msec.2018.07.019. Epub 2018 Jul 10.
The clinical applications of anticancer drugs are restricted due to the incomplete delivery to the cancerous tissue and the numerous drug resistance mechanisms involved in malignant cells. In this regard, stimuli-responsive nanomaterials offer a promising prospect to deal with these concerns. In the present study, ternary responsive hybrid gold/nanogels (Au/NGs) were synthesized as a new nanoplatform to simultaneously carry two anticancer drugs, i.e., doxorubicin (DOX) and 6-mercaptopurine (MP). For this purpose, these drugs were successfully loaded (the loading capacity of 23% and 11%, respectively) into the hybrid Au/NGs by electrostatic interaction (DOX) and AuS bonds (MP). The triggered drug release ability of hybrid Au/NGs was assessed by comparing the environments of simulated physiological and tumor tissue. The incorporation of disulfide bond linkers, pH sensitive, and thermosensitive polymeric segments endowed the NGs with an excellent property in reducing acidic and hyperthermia environments, which greatly facilitates drug release in tumor cells. Intracellular tracking of DOX@MP-Au/NGs confirmed efficient accumulation and cellular uptake of developed NGs and the cytotoxicity studies showed a pronounced tumor inhibition compared with free DOX@MP. It was concluded that the new ternary-responsive NGs have great potential for co-delivery of DOX and MP and can be used in efficient cancer therapy.
由于抗癌药物在癌症组织中的不完全传递以及恶性细胞中涉及的众多耐药机制,其临床应用受到限制。在这方面,刺激响应型纳米材料为解决这些问题提供了有希望的前景。在本研究中,合成了三元响应性杂化金/纳米凝胶(Au/NGs)作为一种新的纳米平台,以同时携带两种抗癌药物,即阿霉素(DOX)和 6-巯基嘌呤(MP)。为此,通过静电相互作用(DOX)和 AuS 键(MP)成功地将这些药物负载(分别为 23%和 11%的载药量)到杂化 Au/NGs 中。通过比较模拟生理和肿瘤组织的环境来评估杂化 Au/NGs 的触发式药物释放能力。引入二硫键连接物、pH 敏感和温敏聚合物段,使 NGs 在还原酸性和高热环境方面具有优异的性能,这极大地促进了肿瘤细胞中的药物释放。DOX@MP-Au/NGs 的细胞内追踪证实了所开发的 NGs 的有效积累和细胞摄取,细胞毒性研究表明与游离 DOX@MP 相比具有明显的肿瘤抑制作用。结论是,新的三元响应性 NGs 具有共递送 DOX 和 MP 的巨大潜力,并可用于有效的癌症治疗。