Construction of curcumin-loaded micelles and evaluation of the antitumor effect based on angiogenesis

Rui Liu, Zhongyan Liu, Changxiang Yu, Ying Zhang, Xiaojiao Feng, Qingqing Zhang, Wenli Dang, Xintao Jia, Bei Jia, Jiachen He, Bin Xing, Ziwei Li, Huihui Li, Xueli Guo, Dereje Kebebe, Jiaxin Pi, Pan Guo
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引用次数: 1

Abstract

Objective: Inhibition of tumor angiogenesis has become a new targeted tumor therapy. In this study, we established a micellar carrier with a tumor neovascularization-targeting effect modified by the neovascularization-targeting peptide NGR. Methods: The targeted polymer NGR-PEG-PLGA was prepared and characterized by 1 H nuclear magnetic resonance and Fourier-transform infrared spectrometry. NGR-PEG-PLGA was used to construct curcumin-loaded micelles by the solvent-evaporation method. The physicochemical properties of the micelles were also investigated. Additionally, we evaluated the antitumor efficacy of the polymer micelles using in vitro cytology experiments and in vivo animal studies. Results: The particle size of Cur-NGR-PM was 139.70±2.51 nm, and the drug-loading capacity was 14.37±0.06%. In vitro cytological evaluation showed that NGR-modified micelles showed higher cellular uptake through receptor-mediated endocytosis pathways than did unmodified micelles, leading to the apoptosis of tumor cells. Then, in vivo antitumor experiments showed that the modified micelles significantly inhibited tumor growth and were safe. Conclusions: NGR-modified micelles significantly optimized the therapeutic efficacy of curcumin. This strategy offers a viable avenue for cancer treatment.
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姜黄素负载胶束的构建及基于血管生成的抗肿瘤作用评价
目的:抑制肿瘤血管生成已成为一种新的肿瘤靶向治疗方法。在本研究中,我们建立了一种由新血管靶向肽NGR修饰的具有肿瘤新血管靶向作用的胶束载体。方法:制备了靶向聚合物NGR-PEG-PLGA,并采用1h核磁共振和傅里叶变换红外光谱对其进行了表征。用NGR-PEG-PLGA溶剂蒸发法制备了姜黄素负载胶束。研究了胶束的理化性质。此外,我们通过体外细胞学实验和体内动物实验评估了聚合物胶束的抗肿瘤功效。结果:cu - ngr - pm粒径为139.70±2.51 nm,载药量为14.37±0.06%。体外细胞学评价表明,与未修饰的胶束相比,ngr修饰的胶束通过受体介导的内吞途径表现出更高的细胞摄取,导致肿瘤细胞凋亡。体内抗肿瘤实验表明,改性胶束能明显抑制肿瘤生长,且安全。结论:ngr修饰胶束可显著优化姜黄素的治疗效果。这一策略为癌症治疗提供了一条可行的途径。
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