Synergistically enhanced anticancer effect of codelivered curcumin and siPlk1 by stimuli-responsive α-lactalbumin nanospheres
Synergistically enhanced anticancer effect of codelivered curcumin and siPlk1 by stimuli-responsive α-lactalbumin nanospheres
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DOI：
10.2217/nnm-2018-0291
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发表时间：
2019-03-01
期刊：
影响因子：
5.5
通讯作者：
Li, Yuan
中科院分区：
文献类型：
--
作者：
Li, Dan;Shi, Mengxuan;Li, Yuan
利用α -乳清蛋白（α -lac）纳米载体递送siPlk1和姜黄素（cur）联合治疗，提高抗癌效果。材料与方法：将α - lac部分水解成两亲肽，然后自组装成纳米球（NS）。在自组装过程中，Cur被装载到它们的疏水核心中。siPlk1-SH与NS上的内源性半胱氨酸交联。将CRGDK肽偶联在NS上，靶向HeLa细胞中过表达的整合素。结果与结论：Cur和siPlk1复合NS制剂具有较强的肿瘤靶向性和抗肿瘤活性。药物响应性地从RGD-NS/Cur/siPlk1交联的二硫键释放，对应于癌细胞细胞内高浓度的谷胱甘肽。体外细胞活力实验和体内抗肿瘤评价表明，共递送纳米球平台具有良好的肿瘤靶向性和协同抗肿瘤效果。
To achieve enhanced anticancer efficacy by combined siPlk1 and curcumin (cur) therapy using alpha-lactalbumin (alpha-lac) nanocarrier delivery. Materials & methods: alpha-Lac was partially hydrolyzed into amphiphilic peptides, and then self-assembled into nanospheres (NS). Cur was loaded into their hydrophobic core during the self-assembly process. siPlk1-SH was cross-linked with the endogenous cysteines on the NS. CRGDK peptide was conjugated on NS to target integrins overexpressed in HeLa cells. Results & conclusion: The Cur and siPlk1 coloaded NS formulations possessed an enhanced tumor targeting and antitumor properties. Drugs were responsively released from disulfide bonds cross-linked RGD-NS/Cur/siPlk1 corresponding to the high intracellular glutathione concentrations of cancer cells. Both in vitro cell viability experiments and in vivo antitumor evaluations demonstrated that the codelivered nanosphere platform exhibited excellent tumor targeting and synergistic antitumor efficacy.