Lipid-based drug carriers, such as liposomes or drug/lipid complexes, have been extensively investigated in a large number of therapeutic protocols such as gene therapy, drug delivery, drug targeting and antibacterial treatments, in preclinical and clinical trials. Many formulations composed of natural and/or synthetic amphiphiles have been studied. Many synthetic lipids and surfactants have been designed and tested in order to improve liposomes and lipid complexes performances, such as fusion with cellular membrane, cellular uptake, target selectivity, transfection efficiency, low toxicity. Among these, gemini surfactants have been shown to be highly effective in delivering genetic material to cells, and also have been shown promising as synthetic additives in liposome formulations for drug delivery. The encouraging results obtained in gene therapy have given impulse to chemist creativity: an extensive selection of pH sensitive, sugar-, aminoacid- , and peptide-based gemini surfactants have been developed, many of which have shown good biological features. This review focuses on recent progress in gemini surfactant based formulations and their applications in different therapeutic protocols.