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Peptidic Monodisperse PEG "Comb" as Multifunctional "Add-On" Module for Imaging-Traceable and Thermo-Responsive Theranostics.
Advanced Healthcare Materials ( IF 10.0 ) Pub Date : 2019-12-18 , DOI: 10.1002/adhm.201901331
Junfei Zhu 1 , Huaibin Zhang 1, 2 , Kexin Chen 3 , Yu Li 2 , Zhigang Yang 1 , Shizhen Chen 2 , Xing Zheng 3 , Xin Zhou 2 , Zhong-Xing Jiang 1
Affiliation  

Monodisperse polyethylene glycols-modified (M-PEGylated) biomaterials exhibit high structural accuracy, biocompatibility, and fine-tunable physicochemical properties. To develop "smart" drug delivery systems in a controllable and convenient manner, a peptidic M-PEG "comb" with fluorinated L-lysine side chains and a fluorescent N-terminal is conveniently prepared as a 19 F magnetic resonance imaging (19 F MRI) and fluorescence dual-imaging traceable and thermo-responsive "add-on" module for liposomal theranostics in cancer therapy. The peptidic M-PEG "comb" has high biocompatibility, thermo-responsivity with a sharp lower critical solution temperature, an aggregation-induced emission fluorescence, and high 19 F MRI sensitivity. As a highly branched amphiphile, it self-assembles and firmly anchors on the doxorubicin-loaded liposomal nanoparticles, which M-PEGylates the liposomes and facilitates the thermo-responsive drug release and drug tracking with dual-imaging technologies. In a rodent xenograft model of human liver cancer HepG2 cells, the M-PEGylated liposomes exhibit long in vivo half time, low toxicity, high tumor accumulation, "hot spot" 19 F MRI, and therapeutic efficacy. With accurately programmable chemical structure, fine-tunable physicochemical and biological properties to meet the demands of diagnosis, drug delivery, and therapy, the M-PEG "comb" is promising as a versatile "add-on" module for rapid and convenient formulation of various "smart" theranostics.

中文翻译:

肽单分散PEG“ Comb”作为多功能的“附加”模块,用于成像跟踪和热响应治疗学。

单分散聚乙二醇修饰的(M-PEG化)生物材料具有很高的结构精度,生物相容性和微调的理化特性。为了以可控制和方便的方式开发“智能”药物输送系统,可以方便地将具有氟化L-赖氨酸侧链和荧光N端的肽M-PEG“梳”制备为19 F磁共振成像(19 F MRI) )和荧光双成像可追踪且具有热响应性的“附加”模块,用于癌症治疗中的脂质体治疗学。肽型M-PEG“梳”具有高生物相容性,临界值温度急剧降低的热响应性,聚集诱导的发射荧光和19 F MRI灵敏度高。作为高度分支的两亲物,它可以自组装并牢固地固定在负载阿霉素的脂质体纳米颗粒上,该颗粒通过M-PEG化脂质体,并通过双成像技术促进热响应性药物的释放和药物追踪。在人类肝癌HepG2细胞的啮齿类动物异种移植模型中,M-PEG化脂质体表现出较长的体内半衰期,低毒性,高肿瘤蓄积性,“热点” 19 F MRI和治疗功效。M-PEG“梳子”具有精确可编程的化学结构,可调节的理化和生物学特性,可满足诊断,药物输送和治疗的需求,有望成为一种多功能“附加”模块,可快速便捷地配制各种“智能”治疗法。M-PEG化脂质体,并通过双重成像技术促进热响应性药物的释放和药物追踪。在人类肝癌HepG2细胞的啮齿类动物异种移植模型中,M-PEG化脂质体在体内的半衰期长,毒性低,肿瘤蓄积高,“热点” 19 F MRI和治疗效果高。M-PEG“梳子”具有精确可编程的化学结构,可调节的理化和生物学特性,可满足诊断,药物输送和治疗的需求,有望成为一种多功能“附加”模块,可快速便捷地配制各种“智能”治疗法。M-PEG化脂质体,并通过双重成像技术促进热响应性药物的释放和药物追踪。在人类肝癌HepG2细胞的啮齿类动物异种移植模型中,M-PEG化脂质体在体内的半衰期长,毒性低,肿瘤蓄积高,“热点” 19 F MRI和治疗效果高。M-PEG“梳子”具有精确可编程的化学结构,可调节的理化和生物学特性,可满足诊断,药物输送和治疗的需求,有望成为一种多功能“附加”模块,可快速便捷地配制各种“智能”治疗法。M-聚乙二醇化脂质体在体内的半衰期长,毒性低,肿瘤积累高,“热点” 19 F MRI和治疗效果好。M-PEG“梳子”具有精确可编程的化学结构,可调节的理化和生物学特性,可满足诊断,药物输送和治疗的需求,有望成为一种多功能“附加”模块,可快速便捷地配制各种“智能”治疗法。M-聚乙二醇化脂质体在体内的半衰期长,毒性低,肿瘤积累高,“热点” 19 F MRI和治疗效果好。M-PEG“梳子”具有精确可编程的化学结构,可调节的理化和生物学特性,可满足诊断,药物输送和治疗的需求,有望成为一种多功能“附加”模块,可快速便捷地配制各种“智能”治疗法。
更新日期:2020-02-06
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