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GE11 修饰的 PLGA/TPGS 纳米粒靶向递送萨利霉素至乳腺癌细胞。

GE11 Modified PLGA/TPGS Nanoparticles Targeting Delivery of Salinomycin to Breast Cancer Cells.

机构信息

Department of Oncology, Shanghai Fourth People's Hospital Affiliated to Tongji University, Shanghai, China.

Institute of Translational Medicine, Shanghai University, Shanghai, China.

出版信息

Technol Cancer Res Treat. 2021 Jan-Dec;20:15330338211004954. doi: 10.1177/15330338211004954.

Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e34/8182624/5bdf5f1203fc/10.1177_15330338211004954-fig1.jpg

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