Design, synthesis and biological evaluation of novel cationic liposomes loaded with melphalan for the treatment of cancer

Therapeutically active lipids in drug delivery systems offer customization for enhanced pharmaceutical and biological effects, improving safety and efficacy. Biologically active N, N-didodecyl-3,4-dimethoxy-N-methyl-benzenaminium lipid (Q) was synthesized and employed to create a liposome formulation (FQ) encapsulating melphalan (M) through a thin film hydration method. Synthesized cationic lipids and their liposomal formulation underwent characterization and assessment for additive anti-cancer effects on myeloma and melanoma cancer cell lines. These effects were evaluated through various studies, including cytotoxicity assessments, cell cycle arrest analysis, apoptosis measurements, mitochondrial membrane potential depolarization, DNA fragmentation, and a significant reduction in tumorigenic potential, as evidenced by a decrease in both the number and percentage area of cancer spheroids.

Automated summary

Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.