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Targeting of somatostatin receptors expressed in blood cells using quantum dots coated with vapreotide

机译:使用涂有维普肽的量子点靶向血细胞中表达的生长抑素受体

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Cancer may be difficult to target, however, if cancer targeted this provides the chance for a better and more effective treatment. Q uantum dots (Qdots) coated vapreotide (VAP) as a somatostatin receptors (SSTRs) agonist can be efficient targeting issue since may reduce side effects and increase drug delivery to the target tissue. This study highlights the active targeting of cancer cells by cells imaging with improving the therapeutic outcomes. VAP was conjugated to Qdots using amine-to-sulfhydryl crosslinker. The synthesized Qdots-VAP was characterized by determination of size, measuring the zeta-potential and UV fluorometer. The cellular uptake was studied using different cell lines. Finally, the Qdots-VAP was injected into a rat model. The results showed a size of 479.8?±?15 and 604.88?±?17?nm for unmodified Qdots and Qdots-VAP respectively, while the zeta potential of particles went from negative to positive charge which proved the conjugation of VAP to Qdots. The fluorometer recorded a redshift for Qdots-VAP compared with unmodified Qdots. Moreover, cellular uptake exhibited high specific binding with cells which express SSTRs using confocal microscopy and flow cytometry (17.3 MFU comparing to 3.1 MFU of control, P??0.001). Finally, an in vivo study showed a strong accumulation of Qdots-VAP in the blood cells (70%). In conclusion, Qdots-VAP can play a crucial role in cancer diagnosis and treatment of blood cells diseases when conjugated with VAP as SSTRs agonist.
机译:癌症可能难以靶向,但是,如果靶向癌症,则可以提供更好,更有效的治疗方法。作为生长抑素受体(SSTRs)激动剂的Q量子点(Qdots)包覆的vapreotide(VAP)可能是有效的靶向问题,因为它可以减少副作用并增加药物向靶组织的递送。这项研究强调了通过细胞成像积极靶向癌细胞并改善治疗效果。使用胺至巯基交联剂将VAP与Qdot偶联。合成的Qdots-VAP通过确定大小,测量Zeta电位和UV​​荧光计进行表征。使用不同的细胞系研究了细胞摄取。最后,将Qdots-VAP注入大鼠模型。结果表明,未修饰的Qdots和Qdots-VAP的尺寸分别为479.8?±?15和604.88?±?17?nm,而粒子的ζ电势从负电荷变为正电荷,证明了VAP与Qdot的共轭。与未修改的Qdot相比,荧光计记录了Qdots-VAP的红移。此外,使用共聚焦显微镜和流式细胞术,细胞摄取表现出与表达SSTR的细胞的高特异性结合(与对照的3.1MFU相比,为17.3MFU,P << 0.001)。最后,一项体内研究显示,血细胞中Qdots-VAP大量积聚(70%)。总之,当Qdo​​ts-VAP与VAP作为SSTR激动剂结合时,在癌症诊断和血细胞疾病的治疗中起着至关重要的作用。

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