Formulating a poorly water-soluble drug substance into nanocrystals offers many advantages. Understanding of the in vivo fate of drug nanocrystals is however very limited. In this study, we utilized the hybrid nanocrystal concept and studied the kinetic process of dissolution in cancer cells. By taking advantage of aggregation-induced emission (AIE), hybrid paclitaxel (PTX) nanocrystals integrated with tetraphenylethene (TPE) enabled a novel way for estimating the intracellular dissolution process of the nanocrystals. When TPE is entrapped in a nanocrystal, fluorescence is emitted when the nanocrystal is optically excited. When an entrapped TPE molecule is released to a liquid medium due to the dissolution of the nanocrystal, its fluorescence is quenched. By monitoring the change in fluorescence, it is possible to quantify the dissolution of nanocrystals in a biological environment. Cellular uptake studies of hybrid nanocrystals were conducted with KB and HT-29 cell lines and characterized by confocal microscopy, flow cytometry, and HPLC. The results suggest that drug nanocrystals were taken up directly by the cells, and subsequently dissolved in the cytoplasm. The extent to which the drug nanocrystal dissolved was estimated according to the fluorescence measurement. The cellular uptake and intracellular dissolution could be influenced by drug concentration, incubation time, and surface coating, as well as the type of cell line.

将水溶性差的药物配制成纳米晶体具有许多优点。了解体内然而，药物纳米晶体的命运非常有限。在这项研究中，我们利用了杂化纳米晶体的概念，并研究了在癌细胞中溶解的动力学过程。通过利用聚集诱导发射（AIE），与四苯乙烯（TPE）集成的杂化紫杉醇（PTX）纳米晶体实现了估算纳米晶体细胞内溶解过程的新方法。当TPE被截留在纳米晶体中时，当纳米晶体被光学激发时发射荧光。当由于纳米晶体的溶解而将截留的TPE分子释放到液体介质中时，其荧光被猝灭。通过监测荧光的变化，可以量化纳米晶体在生物环境中的溶解。用KB和HT-29细胞系进行杂交纳米晶体的细胞摄取研究，并通过共聚焦显微镜，流式细胞术和HPLC对其进行表征。结果表明药物纳米晶体被细胞直接吸收，随后溶解在细胞质中。根据荧光测量估计药物纳米晶体溶解的程度。细胞吸收和细胞内溶解可能会受到药物浓度，孵育时间和表面涂层以及细胞系类型的影响。根据荧光测量估计药物纳米晶体溶解的程度。细胞吸收和细胞内溶解可能会受到药物浓度，孵育时间和表面涂层以及细胞系类型的影响。根据荧光测量估计药物纳米晶体溶解的程度。细胞吸收和细胞内溶解可能会受到药物浓度，孵育时间和表面涂层以及细胞系类型的影响。