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目的:将Caco-2细胞模型的改良研究特征及其在药物研究中的应用进展进行系统的总结,便于相同领域的研究人员能在实际研究中更科学有效的利用该细胞模型。方法:概述了近年来Caco-2细胞模型在药物相互作用、代谢及在药物剂型开发中应用情况,并查阅有关改良研究的文献,总结对Caco-2细胞模型进行的改良方法。结果与结论:Caco-2细胞模型在药物研究中有良好的吸收、代谢规律。其中包括通过基因重组、基因敲除或化学物质诱导改变转运蛋白表达和细胞内的代谢酶,增加私液层可以通过加入私蛋白或细胞共培养方式来完成,将培养周期缩短,增加药物溶解性与减少非特异性结合等。这些改良使该模型能更好地模拟体内生理条件,Caco-2细胞模型是药物体外研究十分稳定且良好的方法,能够使其在研究药物的吸收、代谢及高通量筛选中发挥及其显著的作用。
OBJECTIVE: To systematically summarize the improved research features of Caco-2 cell model and its application in drug research so that researchers in the same field can use the cell model more scientifically and effectively in practical research. Methods: The Caco-2 cell models in recent years were reviewed in the fields of drug interactions, metabolism and drug formulation development. The literature review on improvement studies was summarized and the improvement of Caco-2 cell models was summarized. RESULTS AND CONCLUSION: Caco-2 cell model has good absorption and metabolism in drug research. These include alteration of transporter expression and intracellular metabolic enzymes by genetic recombination, knockout or chemical induction, and augmentation of the primed layer by co-culturing with prion protein or cells, shortening the incubation period, and increasing drug solubility And reduce the non-specific binding. These improvements make the model better able to mimic physiological conditions in vivo. The Caco-2 cell model is a very stable and well-established method for drug in vitro studies that enables it to exert its promise in investigating drug absorption, metabolism and high-throughput screening Role.