Li Qing, Wen Yong, You Xinru, Zhang Fenghe, Shah Vishva, Chen Xing, Tong Dongdong, Wei Xiujuan, Yin Linlin, Wu Jun, Xu Xin
School of Stomatology, Shandong University, Jinan, Shandong 250012, P. R. China.
J Mater Chem B. 2016 Jul 21;4(27):4675-4682. doi: 10.1039/c6tb01016d. Epub 2016 Jun 23.
In this study, for effective oral cancer therapy, a new targeted and ROS-triggered drug delivery nanoplatform was developed from the RGD-PEG-TK-PLGA polymer, in which the ROS-responsive TK containing linker was connected with PEG and PLGA. RGD in the drug delivery system (DDS) presented here was used to target cancer cells. This new nanoplatform shows high stability, good targeting ability, excellent ROS sensitivity and excellent biocompatibility. Loaded with DOX and alpha-TOS, the formulated nanoparticles (NPs) demonstrate much better cellular uptake efficiency and higher inhibition performance towards the oral tongue Cal27 cancer cell line. In vivo anticancer evaluation indicates that DOX and alpha-TOS loaded RGD-PEG-TK-PLGA NPs have no toxicity to mice and showed significantly improved therapeutic efficacy against tumors. Therefore, this polymeric NP platform presents great potential as a new DDS for oral cancer chemotherapy.
在本研究中,为了实现有效的口腔癌治疗,我们从RGD-PEG-TK-PLGA聚合物开发了一种新型的靶向且由活性氧(ROS)触发的药物递送纳米平台,其中含ROS响应性连接子的硫代缩酮(TK)与聚乙二醇(PEG)和聚乳酸-羟基乙酸共聚物(PLGA)相连。此处呈现的药物递送系统(DDS)中的RGD用于靶向癌细胞。这种新型纳米平台具有高稳定性、良好的靶向能力、出色的ROS敏感性和优异的生物相容性。负载阿霉素(DOX)和α-生育三烯酚琥珀酸酯(alpha-TOS)的纳米颗粒(NPs)对口腔舌癌细胞系Cal27表现出更好的细胞摄取效率和更高的抑制性能。体内抗癌评估表明,负载DOX和alpha-TOS的RGD-PEG-TK-PLGA NPs对小鼠无毒,并对肿瘤显示出显著提高的治疗效果。因此,这种聚合物NP平台作为一种新型的口腔癌化疗DDS具有巨大潜力。