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Synthesis, Characterization, and Biodistribution of Quantum Dot-Celecoxib Conjugate in Mouse Paw Edema Model

机译:小鼠爪水肿模型中量子点-塞来昔布偶联物的合成,表征和生物分布

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Increased risk of cardiovascular side effects has been reported with many of the drugs in the market, including nonsteroidal anti-inflammatory drugs (NSAIDs). Hence, it is critical to thoroughly evaluate the biodistribution and pharmacokinetic properties of the drugs. Presently nanotechnology in combination with noninvasive imaging techniques such as magnetic resonance imaging (MRI), computed axial tomography (CAT), and positron emission tomography (PET) provides a better estimate of the spatio-temporal distribution of therapeutic molecules. Optical imaging using quantum dot- (QD-) tagged biological macromolecules is emerging as a fast, economical, sensitive, and safer alternative for theranostic purposes. In the present study, we report the nanoconjugates of mercaptopropionic acid- (MPA-) capped CdTe quantum dots (QDs) and Celecoxib for bio-imaging in carrageenan-induced mouse paw edema model of inflammation. QD-Celecoxib conjugates were characterized by fluorescence, FT-IR, NMR, and zeta-potential studies. In vivo imaging of QD-Celecoxib conjugates showed clear localization in the inflamed tissue of mouse paw within 3 h, with a gradual increase reaching a maximum and a later decline. This decrease of fluorescence in the paw region is followed by an increase in urinary bladder region, suggesting the possible excretion of QD-drug conjugates from mice within 24 h.
机译:据报道,市场上许多药物,包括非甾体类抗炎药(NSAIDs),都有增加心血管副作用的风险。因此,全面评估药物的生物分布和药代动力学特性至关重要。当前,纳米技术与非侵入性成像技术(例如磁共振成像(MRI),计算机轴向断层扫描(CAT)和正电子发射断层扫描(PET))的结合提供了对治疗分子的时空分布的更好估计。使用量子点-(QD-)标记的生物大分子的光学成像正在成为用于治疗诊断目的的快速,经济,敏感和安全的替代方案。在本研究中,我们报道了巯基丙酸-(MPA-)封端的CdTe量子点(QDs)和Celecoxib的纳米共轭物,用于在角叉菜胶诱发的小鼠爪水肿模型中进行生物成像。通过荧光,FT-IR,NMR和ζ电位研究对QD-塞来昔布共轭物进行了表征。 QD-塞来昔布偶联物的体内成像显示在3h内清楚地定位在小鼠爪发炎的组织中,逐渐增加达到最大值,然后逐渐下降。爪部区域荧光的下降随后是膀胱区域的增大,这表明QD-药物偶联物可能在24小时内从小鼠中排出。

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