EGFR targeted thermosensitive liposomes: A novel multifunctional platform for simultaneous tumor targeted and stimulus responsive drug delivery
EGFR targeted thermosensitive liposomes: A novel multifunctional platform for simultaneous tumor targeted and stimulus responsive drug delivery
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DOI：
10.1016/j.colsurfb.2016.06.012
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发表时间：
2016-10-01
影响因子：
5.8
通讯作者：
Koning, Gerben A.
中科院分区：
文献类型：
--
作者：
Haeri, Azadeh;Zalba, Sara;Koning, Gerben A.
表皮生长因子受体（EGFR）是抗癌治疗的一个有前景的靶标。本研究的目的是设计热敏脂质体 (TSL)，用抗 EGFR 配体进行功能化，用于靶向递送和局部触发化疗药物的释放。使用EGFR特异性肽(GE11)和西妥昔单抗的Fab'片段进行靶向，并研究配体密度对体外肿瘤靶向的影响。配体缀合没有显着改变脂质体的理化特性。与GE11修饰的TSL相比，Fab'修饰的TSL（Fab'-TSL）可以特异性且更有效地结合EGFR过表达的癌细胞。钙黄绿素标记的 Fab'-TSL 在 37°C 的血清中表现出足够的稳定性（
The epidermal growth factor receptor (EGFR) is a promising target for anti-cancer therapy. The aim of this study was to design thermosensitive liposomes (TSL), functionalized with anti-EGFR ligands for targeted delivery and localized triggered release of chemotherapy. For targeting, EGFR specific peptide (GE11) and Fab' fragments of cetuximab were used and the effect of ligand density on in vitro tumor targeting was investigated. Ligand conjugation did not significantly change the physicochemical characteristics of liposomes. Fab'-decorated TSL (Fab'-TSL) can specifically and more efficiently bind to the EGFR over expressed cancer cells as compared to GE11 modified TSL. Calcein labeled Fab'-TSL showed adequate stability at 37 degrees C in serum (