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首页> 外文期刊>Advanced Functional Materials >Molecular Probe Crossing Blood-Brain Barrier for Bimodal Imaging-Guided Photothermal/Photodynamic Therapies of Intracranial Glioblastoma
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Molecular Probe Crossing Blood-Brain Barrier for Bimodal Imaging-Guided Photothermal/Photodynamic Therapies of Intracranial Glioblastoma

机译：分子探针穿越血脑屏障的颅内成胶质细胞瘤双峰成像指导光热/光动力疗法。

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Currently, treatment of intracranial diseases still remains a great challenge because the blood-brain barrier (BBB) blocks access of most drugs to the central nervous system. Herein, a theranostic small molecular probe, iRGD-ICG-Lys-DTPA@Gd (iRGD-ILD), capable of crossing BBB is developed. Owing to the small molecular size and alpha(v)beta(3) integrin receptor-mediated transcytosis, this tailor-made molecular probe integrating the fluorescence and magnetic resonance imaging functions effectively passes through BBB to target tumor cells even in the early stage of glioblastoma multiforme (GBM), thereby allowing a bimodal imaging-guided therapy of GBM. The reactive oxygen species and heat generated by the ICG moiety under the 808 nm laser irradiation exert photodynamic/photothermal therapeutic effects, which results in significantly inhibited tumor growth and prolonged median survival of C6-Luc glioma-bearing mice. Notably, the integration of FDA-approved clinically available agents, e.g., ICG, DTPA and Gd, into a molecular probe may ensure desirable biocompatibility and biosafety for in vivo applications. Overall, the results highlight the potential of a water-soluble small molecule as a novel theranostic probe for highly effective GBM treatment.
机译：目前，颅内疾病的治疗仍然是一个巨大的挑战，因为血脑屏障（BBB）阻止了大多数药物进入中枢神经系统。本文中，开发了一种能够穿过血脑屏障的治疗性小分子探针，iRGD-ICG-Lys-DTPA @ Gd（iRGD-ILD）。由于分子大小小且α（v）β（3）整合素受体介导的胞吞作用，这种定制的分子探针结合了荧光和磁共振成像功能，即使在胶质母细胞瘤的早期，也能有效地通过BBB靶向肿瘤细胞多形式（GBM），从而允许双峰成像指导治疗GBM。 ICG部分在808 nm激光照射下产生的活性氧和热量发挥了光动力/光热治疗作用，从而显着抑制了C6-Luc胶质瘤小鼠的肿瘤生长并延长了其中位生存期。值得注意的是，将FDA批准的临床可用药物（例如ICG，DTPA和Gd）整合到分子探针中，可以确保体内应用具有理想的生物相容性和生物安全性。总的来说，结果突出了水溶性小分子作为新型治疗疗法探针的潜力，可用于高效GBM治疗。

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