Preparation and Evaluation of the Cytoprotective Activity of Micelles with DSPE-PEG-C60 as a Carrier Against Doxorubicin-Induced Cytotoxicity.
Preparation and Evaluation of the Cytoprotective Activity of Micelles with DSPE-PEG-C60 as a Carrier Against Doxorubicin-Induced Cytotoxicity.
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DSPE-PEG-C60为载体胶束的制备及抗阿霉素细胞毒性的细胞保护活性评价
DOI：
10.3389/fphar.2022.952800
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发表时间：
2022
影响因子：
5.6
通讯作者：
Qi, Xuchen
中科院分区：
文献类型：
--
作者：
Xu, Beihua;Ding, Zhongpeng;Hu, Ying;Zhang, Ting;Shi, Senlin;Yu, Guangmao;Qi, Xuchen
为了提高阿霉素(DOX)的体内给药效率和安全性，以两亲聚合物DSPE-PEGC60为载体，将C60(OH)22与DSPE-PEGNH2偶联，制备了富勒烯醇改性胶束。对其粒径、PDI、Zeta电位和包封率进行了研究。成功地将DOX负载到胶束中，得到了合适的粒径[97 nm，211 nm，260 nm，载体：DOx=5：1，10：1；15：1(W/W)]，负zeta电位约为−30 mV，以及可接受的包封率[86.1，95.4，97.5%，载体：DOx=5：1，10：1；15：1(W/W)]。DOX在DSPE-PEG-C60胶束中的释放行为与DSPE-PEG胶束一致，且具有缓释作用。DSPE-PEG-C60胶束对正常细胞株(L02、H9c2、GES-1)的细胞毒作用低于游离DOX和DSPE-PEG胶束。为探讨DSPE-PEG-C60对阿霉素诱导的H9c2细胞氧化应激、线粒体膜电位和细胞凋亡的保护作用，采用JC-1活性氧分析试剂盒和FITC Annexin V细胞凋亡检测试剂盒对DSPE-PEG-C60对H9c2细胞氧化应激、线粒体膜电位和细胞凋亡的影响进行了研究。结果表明，DSPE-PEG-C60胶束作用于H9c2细胞后，细胞内ROS减少，红色荧光(JC-1聚集体)/绿色荧光(JC-1单体)比值增加，细胞凋亡率低于对照组和DSPE-PEG胶束细胞。总之，制备的DOX-DSPE-PEG-C60胶束在安全、有效的肿瘤治疗方面具有很大的前景。
To deliver doxorubicin (DOX) with enhanced efficacy and safety in vivo, fullerenol-modified micelles were prepared with the amphiphilic polymer DSPE-PEG-C60 as a carrier, which was synthesized by linking C60(OH)22 with DSPE-PEG-NH2. Studies of its particle size, PDI, zeta potential, and encapsulation efficiency were performed. DOX was successfully loaded into the micelles, exhibiting a suitable particle size [97 nm, 211 nm, 260 nm, vector: DOX = 5:1, 10:1; 15:1 (W/W)], a negative zeta potential of around −30 mv, and an acceptable encapsulation efficiency [86.1, 95.4, 97.5%, vector: DOX = 5:1, 10:1; 15:1 (W/W)]. The release behaviors of DOX from DSPE-PEG-C60 micelles were consistent with the DSPE-PEG micelles, and it showed sustained release. There was lower cytotoxicity of DSPE-PEG-C60 micelles on normal cell lines (L02, H9c2, GES-1) than free DOX and DSPE-PEG micelles. We explored the protective role of DSPE-PEG-C60 on doxorubicin-induced cardiomyocyte damage in H9c2 cells, which were evaluated with a reactive oxygen species (ROS) assay kit, JC-1, and an FITC annexin V apoptosis detection kit for cellular oxidative stress, mitochondrial membrane potential, and apoptosis. The results showed that H9c2 cells exposed to DSPE-PEG-C60 micelles displayed decreased intracellular ROS, an increased ratio of red fluorescence (JC-1 aggregates) to green fluorescence (JC-1 monomers), and a lower apoptotic ratio than the control and DSPE-PEG micelle cells. In conclusion, the prepared DOX-loaded DSPE-PEG-C60 micelles have great promise for safe, effective tumor therapy.
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