%0 Journal Article %T The role of caveolin-1 in the biofate and efficacy of anti-tumor drugs and their nano-drug delivery systems. %A Yang C %A He B %A Dai W %A Zhang H %A Zheng Y %A Wang X %A Zhang Q %J Acta Pharm Sin B %V 11 %N 4 %D Apr 2021 %M 33996409 %F 14.903 %R 10.1016/j.apsb.2020.11.020 %X As one of the most important components of caveolae, caveolin-1 is involved in caveolae-mediated endocytosis and transcytosis pathways, and also plays a role in regulating the cell membrane cholesterol homeostasis and mediating signal transduction. In recent years, the relationship between the expression level of caveolin-1 in the tumor microenvironment and the prognostic effect of tumor treatment and drug treatment resistance has also been widely explored. In addition, the interplay between caveolin-1 and nano-drugs is bidirectional. Caveolin-1 could determine the intracellular biofate of specific nano-drugs, preventing from lysosomal degradation, and facilitate them penetrate into deeper site of tumors by transcytosis; while some nanocarriers could also affect caveolin-1 levels in tumor cells, thereby changing certain biophysical function of cells. This article reviews the role of caveolin-1 in tumor prognosis, chemotherapeutic drug resistance, antibody drug sensitivity, and nano-drug delivery, providing a reference for the further application of caveolin-1 in nano-drug delivery systems.