表皮生长因子脂质体在异种移植结肠癌模型中促进表皮生长因子受体的有效靶向作用。
EGF-liposomes promote efficient EGFR targeting in xenograft colocarcinoma model.
作者信息
Zalba Sara, Contreras Ana Margarita, Merino María, Navarro Iñigo, de Ilarduya Conchita Tros, Trocóniz Iñaki F, Koning Gerben, Garrido María J
机构信息
Department of Pharmacy & Pharmaceutical Technology, School of Pharmacy, University of Navarra, Pamplona, Spain.
Innovative Targeting, Laboratory Experimental Surgical Oncology, Department of Surgery, Erasmus Medical Center, Rotterdam, The Netherlands.
出版信息
Nanomedicine (Lond). 2016;11(5):465-77. doi: 10.2217/nnm.15.208. Epub 2016 Feb 19.
AIM
Development of EGF-liposomes (LP-EGF) for selective molecules delivery in tumors expressing EGFR.
MATERIAL & METHODS: In vitro cellular interaction of EGF-LP and nontargeted liposomes (LP-N) was assayed at 37 and 4 °C in cells expressing different EGFR levels. Receptor-mediated uptake was investigated by competition with a monoclonal antibody anti-EGFR. Selective intracellular drug delivery and efficacy was tested by oxaliplatin encapsulation. In vivo biodistribution of LP-N and LP-EGF was done in xenograft model.
RESULTS
LP-EGF was internalized by an active and selective mechanism through EGFR without receptor activation. Oxaliplatin LP-EGF decreased IC50 between 48 and 13% in cell EGFR+. LP-EGF was accumulated in tumor over 72 h postdosing, while LP-N in spleen.
CONCLUSION
LP-EGF represents an attractive nanosystem for cancer therapy or diagnosis.
目的
开发表皮生长因子脂质体（LP-EGF）用于在表达表皮生长因子受体（EGFR）的肿瘤中进行选择性分子递送。
材料与方法
在37℃和4℃下，在表达不同EGFR水平的细胞中检测EGF-LP和非靶向脂质体（LP-N）的体外细胞相互作用。通过与抗EGFR单克隆抗体竞争来研究受体介导的摄取。通过奥沙利铂包封测试选择性细胞内药物递送和疗效。在异种移植模型中进行LP-N和LP-EGF的体内生物分布研究。
结果
LP-EGF通过EGFR以一种活跃且选择性的机制内化，而不激活受体。奥沙利铂LP-EGF使EGFR+细胞中的半数抑制浓度（IC50）在48%至13%之间降低。给药后72小时以上，LP-EGF在肿瘤中蓄积，而LP-N在脾脏中蓄积。
结论
LP-EGF是一种用于癌症治疗或诊断的有吸引力的纳米系统。
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