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A novel fluorescent probe for more effective monitoring of nanosized drug delivery systems within the cells.

机译:一种新型荧光探针,可更有效地监控细胞内的纳米级药物递送系统。

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To improve visualization of nanoparticles within the cells' compartments, we synthesized a coumarin based fluorescent derivative, tetradecyl diethylamino coumarin amid, 14-DACA. In this compound the coumarin chromophore is linked with a tetradecyl alkyl chain that contributes to lipophilicity and slightly amphiphilic character of this probe. 14-DACA exhibits good biocompatibility, its solubility and emission spectrum are not sensitive to changes in pH value. Solid lipid nanoparticles (SLN) labeled with 14-DACA (SLN-D) and frequently used 6-coumarin (SLN-C) were utilized to evaluate probes' properties in the trafficking and intracellular localization of nanoparticles. SLN-D were seen as distinct blue dots in the cellular environment in contrast to SLN-C which were hardly to recognize due to the self-quenching of 6-coumarin, its leakage and distribution in intracellular compartments. Spectra of 14-DACA indicated the possibility of spectral resolution from both green and red fluorophores allowing clear multicolor imaging of organelles in both fixed and living cells. The results showed valuableness of new probe for trafficking of the drug nanocarriers intracellularly in a kinetic and sensitive manner. Such studies are of great importance in investigations aimed to clarify subcellular targeted drug delivery, controlled release and even to identify toxicological changes.
机译:为了改善细胞室内纳米粒子的可视化,我们合成了一种基于香豆素的荧光衍生物,十四烷基二乙氨基香豆素酰胺,14-DACA。在该化合物中,香豆素生色团与十四烷基烷基链连接,该烷基有助于该探针的亲脂性和两亲性。 14-DACA具有良好的生物相容性,其溶解度和发射光谱对pH值的变化不敏感。用14-DACA(SLN-D)和常用的6-香豆素(SLN-C)标记的固体脂质纳米颗粒(SLN)用于评估探针在纳米颗粒的运输和细胞内定位中的特性。与SLN-C相比,SLN-D在细胞环境中被视为明显的蓝点,由于6-香豆素的自猝灭,其在细胞内区室的泄漏和分布而难以识别。 14-DACA的光谱表明,绿色和红色荧光团均具有光谱分辨率,从而可以对固定细胞和活细胞中的细胞器进行清晰的多色成像。结果表明,新探针对于以动力学和灵敏的方式在细胞内转运药物纳米载体是有价值的。此类研究在旨在弄清亚细胞靶向药物递送,控释甚至确定毒理学变化的研究中非常重要。

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