MI Lab and Department of Circulation and Medical Imaging, The Norwegian University of Science and Technology, Trondheim, Norway.
ACS Nano. 2012 Jun 26;6(6):5648-58. doi: 10.1021/nn301630n. Epub 2012 Jun 6.
The development and application of nanoparticles as in vivo delivery vehicles for therapeutic and/or diagnostic agents has seen a drastic growth over the last decades. Novel imaging techniques allow real-time in vivo study of nanoparticle accumulation kinetics at the level of the cell and targeted tissue. Successful intravenous application of such nanocarriers requires a hydrophilic particle surface coating, of which polyethylene glycol (PEG) has become the most widely studied and applied. In the current study, the effect of nanoparticle PEG surface density on the targeting efficiency of ligand-functionalized nanoemulsions was investigated. We synthesized 100 nm nanoemulsions with a PEG surface density varying from 5 to 50 mol %. Fluorescent and paramagnetic lipids were included to allow their multimodal detection, while RGD peptides were conjugated to the PEG coating to obtain specificity for the α(v)β(3)-integrin. The development of a unique experimental imaging setup allowed us to study, in real time, nanoparticle accumulation kinetics at (sub)-cellular resolution in tumors that were grown in a window chamber model with confocal microscopy imaging, and at the macroscopic tumor level in subcutaneously grown xenografts with magnetic resonance imaging. Accumulation in the tumor occurred more rapidly for the targeted nanoemulsions than for the nontargeted versions, and the PEG surface density had a strong effect on nanoparticle targeting efficiency. Counterintuitively, yet consistent with the PEG density conformation models, the highest specificity and targeting efficiency was observed at a low PEG surface density.
在过去几十年中,纳米颗粒作为治疗和/或诊断试剂的体内输送载体在发展和应用方面取得了迅猛的发展。新型成像技术使得能够实时研究纳米颗粒在细胞和靶向组织水平上的积累动力学。成功地静脉内应用此类纳米载体需要亲水性颗粒表面涂层,其中聚乙二醇(PEG)已成为研究和应用最广泛的。在当前的研究中,研究了纳米颗粒 PEG 表面密度对配体功能化纳米乳液靶向效率的影响。我们合成了具有 5 至 50 mol%PEG 表面密度的 100nm 纳米乳液。荧光和顺磁脂质被包含在内,以允许它们进行多模态检测,而 RGD 肽被连接到 PEG 涂层上以获得对 α(v)β(3)-整联蛋白的特异性。独特的实验成像装置的开发使我们能够实时研究在窗室模型中生长的肿瘤中的(亚)细胞分辨率下的纳米颗粒积累动力学,并在皮下生长的异种移植物中进行宏观肿瘤水平的磁共振成像。与非靶向纳米乳液相比,靶向纳米乳液在肿瘤中的积累更快,PEG 表面密度对纳米颗粒的靶向效率有很大的影响。与 PEG 密度构象模型相反,但具有一致性,在低 PEG 表面密度下观察到最高的特异性和靶向效率。
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