表皮生长因子受体靶向肽修饰的聚合物-脂质杂化纳米粒递药系统用于骨肉瘤的黏菌素治疗
EGFR-targeting peptide conjugated polymer-lipid hybrid nanoparticles for delivery of salinomycin to osteosarcoma.
机构信息
Department of Orthopedics, Jinshan Hospital, Fudan University, Shanghai, China.
Department of Orthopedics, Huashan Hospital of Fudan University, Shanghai, China.
出版信息
J Cancer Res Ther. 2023 Dec 1;19(6):1544-1551. doi: 10.4103/jcrt.jcrt_2503_22. Epub 2023 Dec 28.
CONTEXT
Salinomycin (SAL) is a chemotherapeutic drug with anti-osteosarcoma efficacy, but its hydrophobic properties have hindered its application. Nanoparticles have been widely used as drug carriers to improve the solubility of hydrophobic drugs. The dodecapeptide GE11 has been shown to have great binding affinity to the epidermal growth factor receptor (EGFR), which is highly overexpressed in osteosarcoma.
MATERIALS AND METHODS
We designed novel SAL-loaded GE11-conjugated polymer-lipid hybrid nanoparticles (GE11-NPs-SAL) to target osteosarcoma. The characterization and antitumor activity of GE11-NPs-SAL were evaluated both in vitro and in vivo.
RESULTS
The results showed that GE11-NPs-SAL had a size of ~100 nm with a high encapsulation efficacy of ~80%. Compared with the non-targeted nanoparticles, GE11-NPs-SAL showed increased internalization in osteosarcoma cells and improved therapeutic efficacy in osteosarcoma both in vitro and in vivo.
CONCLUSIONS
GE11-NPs-SAL is a promising treatment for osteosarcoma.
背景
盐霉素（SAL）是一种具有抗骨肉瘤疗效的化疗药物，但由于其疏水性，限制了其应用。纳米粒已广泛用作药物载体，以提高疏水性药物的溶解度。十二肽 GE11 已被证明与表皮生长因子受体（EGFR）具有很强的结合亲和力，而 EGFR 在骨肉瘤中高度过表达。
材料和方法
我们设计了新型负载 SAL 的 GE11 缀合聚合物-脂质杂化纳米粒（GE11-NPs-SAL），以靶向骨肉瘤。评估了 GE11-NPs-SAL 的体外和体内的特性和抗肿瘤活性。
结果
结果表明，GE11-NPs-SAL 的粒径约为 100nm，包封率高达约 80%。与非靶向纳米粒相比，GE11-NPs-SAL 在骨肉瘤细胞中的内化增加，并在体外和体内均提高了骨肉瘤的治疗效果。
结论
GE11-NPs-SAL 是一种有前途的骨肉瘤治疗方法。
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