Liposomal Nanoformulation of Piperlongumine for Improved Aqueous Solubility and Enhanced Anti-tumour Activity In-vitro

Piperlongumine(PL) is an alkaloid isolated from the Piper species, which can induce apoptosis in cancer cells but has little inhibitory effect on the growth of normal cells. However, its poor aqueous solubility has largely limited its therapeutic applications. To address this issue, we developed liposomal nanoformulations for PL (nanoPLs) in this study. The optimized nanoPLs exhibited a small average diameter in the range of 100-160 nm and narrow size distribution as well as high encapsulation efficiency. NanoPLs also demonstrated excellent storage stability at 4°C for 12 weeks. The apparent solubility of PL in NanoPLs was improved up to 312 folds than in PBS. NanoPLs also markedly increased the cytotoxicity of PL to human prostate cancer PC-3 cells when compared to freePL. NanoPLs represent promising and convenient injectable formulations of PL for further preclinical and clinical investigation.