Nanoliposomal delivery of cytosolic phospholipase A2 inhibitor arachidonyl trimethyl ketone for melanoma treatment

Cytosolic PLA2 represents an attractive target for cancers in which inflammation plays a key role. Arachidonyl trifluoromethyl ketone (ATK) inhibits cytosolic PLA2 but the utility of ATK as a therapeutic agent has not been investigated due to its high lipophilicity and low solubility. A novel PEGylated nanoliposomal system called NanoATK was developed that delivers ATK to cancer cells. NanoATK enhances stability, increases circulation and lowers toxicity. NanoATK retarded xenografted melanoma tumor growth by up to 60% without affecting animal weight compared to 30% reduction in tumor development when the maximum tolerated dose of free ATK was administered.210