EGF修饰的紫杉醇微粒和EGF修饰的大黄素微粒复合配方可增强治疗卵巢癌的效果。
A compound formulation of EGF-modified paclitaxel micelles and EGF-modified emodin micelles enhance the therapeutic effect of ovarian cancer.
发表日期:2022 Jun 15
作者:
Ling Tang, Xiu-Xiu Liu, Xiao-Dan Yang, Shuang Tan, Zhong-Wen Zou
来源:
JOURNAL OF LIPOSOME RESEARCH
摘要:
卵巢癌是女性健康的严重威胁,尽管发病率相对较低,但由于其强烈的侵袭和转移作用,其死亡率仍然很高。因此,迫切需要探索卵巢癌的新治疗策略。本研究将紫杉醇和大黄素包裹在不同的胶束中,并以表皮生长因子(EGF)为靶向分子,按比例制成复合配方。本研究对比表征了EGF修饰的紫杉醇胶束和EGF修饰的大黄素胶束,研究了它们对SKOV3细胞在体内和体外的增殖和侵袭的抑制作用,并证实了它的靶向能力。结果表明,EGF修饰的紫杉醇胶束加上EGF修饰的大黄素胶束的形状、粒子大小、ζ电位、释放速率、封装率、聚分散指数和其他物理和化学性质符合要求,并且EGF对胶束表面的修饰可以明显提高SKOV3细胞的摄取量和抑制SKOV3细胞的增殖。复合配方通过抑制低氧诱导因子-α、MMP-2、MMP-9和VE- 链蛋白的表达,可以抑制卵巢癌的侵袭和转移。体内研究也显示了显著的药效学结果。这些结果表明,EGF修饰的紫杉醇胶束加上EGF修饰的大黄素胶束为卵巢癌的治疗提供了新的策略。
Ovarian cancer is a serious threat to female health, although the incidence of it is relatively low, its mortality rate remains high due to its intense invasion and metastasis. Therefore, it is urgent to explore new treatment strategies for ovarian cancer. In this study, paclitaxel and emodin were encapsulated in different micelles, and loaded on the surface of the micelles with epidermal growth factor (EGF) as the targeting molecule, made compound formulations in proportion. In this study, EGF-modified paclitaxel micelles and EGF-modified emodin micelles were characterized, their inhibitory effects on SKOV3 cell proliferation and invasion were studied in vivo and in vitro, and its targeting ability was confirmed. The results showed that the shape, particle size, zeta potential, release rate, encapsulation rate, polydispersity index, and other physical and chemical properties of EGF-modified paclitaxel micelles plus EGF-modified emodin micelles meet the requirements, and the modification of EGF on the micelle surface could obviously improve the uptake of SKOV3 cells and inhibit the proliferation of SKOV3 cells. The compound formulation can inhibit the invasion and metastasis of ovarian cancer by inhibiting the expression of hypoxia inducible factor-α, MMP-2, MMP-9, and VE-cadherin. The in vivo studies have also showed significant pharmacodynamics results. These results indicated that EGF-modified paclitaxel micelles plus EGF-modified emodin micelles provide a new strategy for the treatment of ovarian cancer.