Development of curcumin-loaded ultra deformable lipid vesicles for enhanced anti-melanoma activity: in vitro, ex-vivo, and cell line studies

Abstract

This research aims to formulate and characterize transfersomes containing curcumin (CUR-TFS) for the enhanced melanoma activity. Thin film hydration was used to prepare the CUR-TFS with Phospholipon® 90 G and sodium cholate. The formulated transfersomes were studied for their size, zeta potential (ZP), entrapment efficiency (EE), skin penetration and ex-vivo skin permeation. Differential scanning calorimetry (DSC) and x-ray diffraction (XRD) were used to determine the physical state of the drug in the optimized curcumin transfersomes (OPT-CUR-TFS). In vitro cytotoxicity, cellular uptake, live and dead cell assay, soft agar colony assay, and apoptosis analysis were carried out using the A375 melanoma cell line. The size and EE of the OPT-CUR-TFS were 191 ± 5.25 nm and 91.72 ± 0.36%, respectively. When compared to conventional liposomes, transfersomes showed significantly increased drug permeation and deposition in the skin layers. The penetration of transfersomes into the deeper skin layers was illustrated through fluorescence microscopy. The DSC and XRD analysis suggested that CUR in transfersomes was amorphous, demonstrating its successful encapsulation inside the transfersomes. The OPT-CUR-TFS was found to significantly decrease the cell viability in A375 cell lines due to their higher cellular uptake. In addition, the OPT-CUR-TFS showed enhanced antiproliferative action by suppressing the clonogenic potential of A375 cells. Furthermore, the OPT-CUR-TFS induced apoptosis-mediated cell death in A375 cells. These findings could offer a powerful justification for CUR transfersomes as a viable treatment strategy for the management of melanoma.