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首页> 外文期刊>European journal of pharmaceutical sciences >Tyrosine kinase inhibitor conjugated quantum dots for non-small cell lung cancer (NSCLC) treatment
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Tyrosine kinase inhibitor conjugated quantum dots for non-small cell lung cancer (NSCLC) treatment

机译：非小细胞肺癌（NSCLC）治疗酪氨酸激酶抑制剂缀合量子点

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Non-small cell lung cancer is a major sub-type of lung cancer that is associated with a poor diagnosis resulting in poor therapy for the disorder. In order to achieve a better prognosis, innovative multi-functional systems need to be developed which will aide in diagnosis as well as therapy for the disorder. One such multi-functional delivery system fabricated is Quantum Dots (QDs). QDs are photo-luminescent inorganic nanoparticles utilized for tumor detection, preclinically. Erlotinib hydrochloride, a tyrosine kinase inhibitor, is a first-generation drug developed to treat NSCLC. Its active metabolite, Desmethyl Erlotinib (OSI-420), exhibits similar anticancer activity as erlotinib. OSI-420 was conjugated to QDs to fabricate a delivery system and was then characterized by FT-IR, H NMR, UV-VIS, particle size, zeta potential, fluorescence spectroscopy and TEM. Drug loading was estimated using UV-VIS spectroscopy (52.2 +/- 7.5%). A concentration-dependent release of OSI-420 was achieved using esterase enzymes, which was further confirmed using LC-MS. A cellular uptake study revealed the internalization potential of QDs and QD-OSI 420. A cellular recovery study was performed to confirm the internalization potential. Cell viability studies revealed that QD-OSI 420 conjugates had significantly better efficacy than pure drugs in all tested cell lines. QD conjugated OSI-420 demonstrated an IC60 of 2.5 mu M in erlotinib-resistant A549 cell lines, where erlotinib or OSI-420 alone could not exhibit 60% inhibition when evaluated up to 20 mu M. Similar cytotoxic enhancement of erlotinib was seen with QD-OSI 420 in other NSCLC cell lines as well. These results were strengthened by 3D-SCC model of A549 which revealed that QD-OSI 420 was significantly better in reducing in-vitro 3D tumor volume, as compared to pure drugs. This study, being one of its kind, explores the feasibility of conjugating OSI-420 with QDs as an alternative to traditional anti-cancer therapy, by improving intracellular drug delivery.
机译：非小细胞肺癌是肺癌的主要亚型，与诊断不良有关，导致对疾病的疗法不良。为了实现更好的预后，需要开发创新的多功能系统，这将助攻诊断以及对疾病的治疗。制造的一种这样的多功能递送系统是量子点（QDS）。 QD是用于肿瘤检测的光发光无机纳米颗粒，尿动检测呈肿瘤检测。盐酸替替尼盐酸盐，酪氨酸激酶抑制剂是开发治疗NSCLC的第一代药物。其活性地代谢物Desmethyl Erlotinib（OSI-420）表现出类似的抗癌活性作为Erlotinib。 OSI-420与QD缀合以制造递送系统，然后通过FT-IR，H NMR，UV-Vis，粒度，Zeta电位，荧光光谱和TEM表征。使用UV-Vis光谱（52.2 +/- 7.5％）估计药物载荷。使用酯酶酶实现OSI-420的浓度依赖性释放，其使用LC-MS进一步证实。蜂窝摄取研究揭示了QD和QD-OSI 420的内化电位。进行细胞恢复研究以确认内化潜力。细胞活力研究表明，QD-OSI 420缀合物在所有测试细胞系中的纯药物具有显着更好的疗效。 QD缀合的OSI-420在替代抗替代A549细胞系中证明了2.5μm的IC60，仅当评估高达20亩m时，单独的Erlotinib或OSI-420不能表现出60％的抑制。用QD看到厄洛替尼的相似细胞毒性增强-OSI 420在其他NSCLC细胞系中也是如此。通过A549的3D-SCC模型加强了这些结果，显示QD-OSI 420在减少体外3D肿瘤体积时显着更好，与纯药物相比。本研究是其一种类型的研究，通过改善细胞内药物递送，探讨了与QDS与QDS的替代品作为传统抗癌治疗的替代方案的可行性。

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