The limitations of anticancer drugs, including poor tumor targeting and weak uptake efficiency, are important factors affecting tumor therapy. According to characteristics of the tumor microenvironment, in this study, we aimed to synthesize matrix metalloproteinase (MMP)-responsive curcumin (Cur)-loaded nanoparticles (Cur-P-NPs) based on amphiphilic block copolymer (MePEG-peptide-PET-PCL) with MMP-cleavable peptide (GPLGIAGQ) and penetrating peptide (r9), modified to improve tumor targeting and cellular uptake. The average size of Cur-P-NPs was 176.9 nm, with a zeta potential of 8.1 mV, and they showed drug entrapment efficiency and a loading capacity of 87.07% ± 0.63% and 7.44% ± 0.16%, respectively. Furthermore, Cur release from Cur-P-NPs was sustained for 144 h at pH 7.4, and the release rate was accelerated under enzyme reaction condition. The MTT assay demonstrated that free P-NPs had favorable biosafety, and the anti-proliferative activity of Cur-P-NPs was positively correlated with Cur concentration in MCF-7 cells. Additionally, the results of cellular uptake, in vivo pharmacokinetics, and biodistribution showed that Cur-P-NPs had a good effect on cellular uptake and tumor targeting, resulting in the best bioavailability in tumor therapy. Therefore, Cur-P-NPs, as a promising drug delivery system, might lead to a new and efficient route for targeted therapy in clinical practice.

译文

:抗癌药的局限性包括不良的肿瘤靶向性和较弱的摄取效率,是影响肿瘤治疗的重要因素。根据肿瘤微环境的特征,本研究旨在基于两亲嵌段共聚物(MePEG-Peptide-PET-PCL)合成基质金属蛋白酶(MMP)响应姜黄素(Cur)负载的纳米颗粒(Cur-P-NPs)。 ),可修饰MMP裂解肽(GPLGIAGQ)和穿透肽(r9),以改善肿瘤靶向性和细胞摄取。 Cur-P-NPs的平均大小为176.9 nm,ζ电位为8.1 mV,显示出药物的包封率和载药量分别为87.07%±0.63%和7.44%±0.16%。此外,在pH 7.4下,Cur-P-NPs的Cur释放持续了144 wash,并且在酶反应条件下加速了释放速率。 MTT分析表明,游离的P-NP具有良好的生物安全性,Cur-P-NP的抗增殖活性与MCF-7细胞中的Cur浓度呈正相关。另外,细胞摄取,体内药代动力学和生物分布的结果表明,Cur-P-NPs对细胞摄取和肿瘤靶向具有良好的作用,从而在肿瘤治疗中产生了最佳的生物利用度。因此,Cur-P-NP作为一种有前途的药物递送系统,可能会为临床实践中的靶向治疗带来新的有效途径。

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