Department of Oncology, Shanghai Fourth People's Hospital Affiliated to Tongji University, Shanghai, China.
Institute of Translational Medicine, Shanghai University, Shanghai, China.
Technol Cancer Res Treat. 2021 Jan-Dec;20:15330338211004954. doi: 10.1177/15330338211004954.
Salinomycin (Sal) is a potent inhibitor with effective anti-breast cancer properties in clinical therapy. The occurrence of various side effect of Sal greatly limits its application. The epidermal growth factor receptor (EGFR) family is a family of receptors highly expressed in most breast cancer cells. GE11 is a dodecapeptide which shows excellent EGFR affinity. A series of nanoparticles derivatives with GE11 peptide conjugated PLGA/TPGS were synthesized. Nanoprecipitation method was used to prepare the Sal loaded nanoparticles at the optimized concentration. The characterization, targeting efficacy, and antitumor activity were detected both and . Encapsulation of Sal in GE11 modified PLGA/TPGS nanoparticles shows an improved therapy efficacy and lower systemic side effect. This represents the delivery system a promising strategy to enhance the therapeutic effect against EGFR highly expressed breast cancer.
盐霉素(Salinomycin,Sal)是一种有效的临床治疗乳腺癌的抑制剂。Sal 发生各种副作用极大地限制了其应用。表皮生长因子受体(Epidermal Growth Factor Receptor,EGFR)家族是一种在大多数乳腺癌细胞中高度表达的受体家族。GE11 是一种十二肽,对 EGFR 具有优异的亲和力。一系列带有 GE11 肽的 PLGA/TPGS 纳米粒衍生物被合成。采用纳米沉淀法在优化浓度下制备载 Sal 的纳米粒。对其进行表征、靶向效率和抗肿瘤活性进行检测。在 GE11 修饰的 PLGA/TPGS 纳米粒中包封 Sal 可提高治疗效果,降低全身副作用。这代表了一种有前途的策略,可增强针对 EGFR 高表达乳腺癌的治疗效果。