使用脂质纳米载体将药物储备递送至过表达血小板衍生生长因子受体的胶质瘤细胞。
Delivery of a drug cache to glioma cells overexpressing platelet-derived growth factor receptor using lipid nanocarriers.
作者信息
Miller Kayla, Dixit Suraj, Bredlau Amy-Lee, Moore Alfred, McKinnon Emilie, Broome Ann-Marie
机构信息
Department of Radiology & Radiological Sciences, Medical University of South Carolina, 68 President Street, MSC 120/BEB 213, Charleston, SC 29425, USA.
Center for Biomedical Imaging, Medical University of South Carolina, Charleston, SC 29425, USA.
出版信息
Nanomedicine (Lond). 2016 Mar;11(6):581-95. doi: 10.2217/nnm.15.218. Epub 2016 Mar 22.
AIM
Glioblastoma multiforme is a devastating disease with no curative options due to the difficulty in achieving sufficient quantities of effective chemotherapies into the tumor past the blood-brain barrier. Micelles loaded with temozolomide (TMZ) were designed to increase the delivery of this drug into the brain.
MATERIALS & METHODS: pH-responsive micelles composed of distearoyl phosphoethanolamine-PEG-2000-amine and N-palmitoyl homocysteine were surface-functionalized with PDGF peptide and Dylight 680 fluorophore.
RESULTS & CONCLUSION: PDGF-micelles containing TMZ have specific uptake and increased killing in glial cells compared with untargeted micelles. In vivo studies demonstrated selective accumulation of PDGF-micelles containing TMZ in orthotopic gliomas implanted in mice. Targeted micelle-based drug carrier systems hold potential for delivery of a wide variety of hydrophobic drugs thereby reducing its systemic toxicity.
目的
多形性胶质母细胞瘤是一种毁灭性疾病，由于难以越过血脑屏障将足够量的有效化疗药物输送到肿瘤中，因此没有治愈方案。设计负载替莫唑胺（TMZ）的胶束以增加该药物向脑内的递送。
材料与方法
由二硬脂酰磷脂酰乙醇胺-聚乙二醇-2000-胺和N-棕榈酰高半胱氨酸组成的pH响应性胶束用血小板衍生生长因子（PDGF）肽和DyLight 680荧光团进行表面功能化。
结果与结论
与未靶向的胶束相比，含TMZ的PDGF胶束在胶质细胞中具有特异性摄取并增强了杀伤作用。体内研究表明，含TMZ的PDGF胶束在植入小鼠的原位胶质瘤中具有选择性积累。基于靶向胶束的药物载体系统具有递送多种疏水性药物的潜力，从而降低其全身毒性。
Zotero 插件