Table 1.

Nano-based strategies for caveolin-targeting drug delivery systems.

Strategy	Example	Description	Targeting cells	Mechanism	Ref.
Folic acid	Folate-modified polyplex	By combining folic acid with PEI, these polyplex would target to caveolae in Hela cells and enhance the gene delivery efficacy	Tumor cells	Bypasses lysosomes and helps gene delivery	65
Cholesterol	Cholesterol-modified PLGA nanoparticles encapsulating curcumin	Tumor targeting and antitumor efficacy are enhanced by caveolin-mediated endocytosis	Tumor cells	Bypass lysosomes and increase antitumor efficacy	67
Sphingolipid	Sphingolipid-decorated self-micellizing antitumor nanoparticles	High affinity between sphingolipid with caveolae enhances nanoparticles to actively target tumor cells without ligands modification	Tumor cells	Increases targeting ability and bypass lysosomes	68
Lipophilic polyelectrolytes	Polyelectrolytes with aromatic sulfonic acid backbone	Negatively charged aromatic sulfonic backbone modified polyelectrolytes would be selectively internalized by endothelial cells which are highly express caveolin-1 compared with epithelial cells	Endothelial cells	Transcytosis	69
Albumin	Albumin-bound paclitaxel	Increases the binding with endothelial cells in blood vessels and helps transport to tumor tissues for drug accumulation.	Endothelial cells	Transcytosis	70, 71, 72
	Albumin-coated gold nanoparticles	20 nm-sized albumin-coated gold NPs bind to gp60 to internalize into cells via caveolin-mediated pathway	Endothelial cells	Transcytosis	73,74
	Albumin-modified PS nanoparticles	Albumin-modified PS nanoparticles have highest co-localization with caveolin-1 in endothelial cells and pass through cells	Endothelial cells	Transcytosis	75
	Albumin-modified polyplex	Albumin-modified polyplex delivering siRNA enters cells via caveolin-mediated endocytosis and increases the silencing effect	Tumor cells	Bypasses lysosomes and increases gene transduction efficacy	76
Liposomes	Liposomes-loaded paclitaxel	By caveolae-targeting transcytosis in VEGFR2-inhibited blood vessels, the accumulation of paclitaxel to tumor tissues is enhanced by loading paclitaxel into liposomes	Endothelial cells	Transcytosis	77
Solid lipid nanoparticles	SLN-encapsulated paclitaxel	The overexpression of caveolin-1 in drug-resistant tumor cells helps SLN/paclitaxel internalization by caveolin-mediated endocytosis	Tumor cells	Bypasses lysosomes and increases drug response	78