肽接枝自组装聚（γ-谷氨酸）-苯丙氨酸纳米颗粒将喜树碱靶向递送至神经胶质瘤
Peptide grafted and self-assembled poly(γ-glutamic acid)-phenylalanine nanoparticles targeting camptothecin to glioma.
作者信息
Kulhari Hitesh, Telukutla Srinivasa R, Pooja Deep, Shukla Ravi, Sistla Ramakrishna, Bansal Vipul, Adams David J
机构信息
Ian Potter NanoBioSensing Facility, NanoBiotechnology Research Laboratory, School of Science, RMIT University, Melbourne, VIC 3001, Australia.
Health Innovations Research Institute, RMIT University, Melbourne, VIC 3083, Australia.
出版信息
Nanomedicine (Lond). 2017 Jul;12(14):1661-1674. doi: 10.2217/nnm-2017-0067. Epub 2017 Jun 21.
AIM
To synthesize cRGDfK peptide conjugated poly(γ-glutamic acid)-phenylalanine nanoparticles to improve the therapeutic efficacy of camptothecin (CPT) against glioblastoma multiforme.
METHODS
Peptide-conjugated, drug-loaded nanoparticles (cRGDfK-conjugated camptothecin-loaded PGA-PA nanoparticles [RCPN]) were prepared and physico-chemically characterized using different techniques. Nanoparticles were evaluated for in vitro anticancer activity, cellular uptake, induction of apoptosis and wound healing cell migration against U87MG human glioblastoma cells.
RESULTS
RCPN, with a particle size of <100 nm and 65% CPT encapsulation efficiency, exhibited a dose- and time-dependent cytotoxicity to glioblastoma cells. Compared with native CPT or unconjugated nanoparticles, RCPN induced apoptosis, increased reactive oxygen species generation and inhibited U87MG cell migration.
CONCLUSION
cRGDfK-mediated and amphiphilic copolymer-based nanomedicines represent a new approach for improved delivery of anticancer drugs to and treatment of glioblastoma multiforme.
目的
合成cRGDfK肽偶联的聚（γ-谷氨酸）-苯丙氨酸纳米颗粒，以提高喜树碱（CPT）对多形性胶质母细胞瘤的治疗效果。
方法
制备肽偶联的载药纳米颗粒（cRGDfK偶联的载喜树碱的聚谷氨酸-苯丙氨酸纳米颗粒 [RCPN]），并使用不同技术对其进行物理化学表征。评估纳米颗粒对U87MG人胶质母细胞瘤细胞的体外抗癌活性、细胞摄取、凋亡诱导和伤口愈合细胞迁移情况。
结果
RCPN粒径小于100 nm，喜树碱包封率为65%，对胶质母细胞瘤细胞表现出剂量和时间依赖性细胞毒性。与天然喜树碱或未偶联的纳米颗粒相比，RCPN诱导凋亡，增加活性氧生成并抑制U87MG细胞迁移。
结论
cRGDfK介导的两亲性共聚物基纳米药物代表了一种改进抗癌药物向多形性胶质母细胞瘤递送和治疗的新方法。
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