Liposomes have been extensively used as effective nanocarriers, providing better solubility, higher stability and slower release of drugs compared to free drug administration. They are also preferred due to their nontoxic nature as well as their biodegradability and cell membrane mimicking abilities. In this study, we examined noncovalent integration of a cell penetrating arginine-rich peptide amphiphile into a liposomal formulation of negatively charged 1,2-dioleoyl-sn-glycero-3-[phospho-rac-(1-glycerol)] (DOPG) phospholipids in the presence of cholesterol due to its amphipathic character. We studied changes in the physical characteristics (size, surface potential and membrane polarity) of the liposomal membrane, as well as in the encapsulation of hydrophilic and hydrophobic agents due to peptide amphiphile incorporation. The activities of peptide integrated liposomal systems as drug delivery agents were investigated by using anti-cancer drugs, doxorubicin-HCl and paclitaxel. Enhancement in liposomal uptake due to arginine-rich peptide integration, and enhanced efficacy of the drugs were observed with peptide functionalized liposomes compared to free drugs. © 2013 The Royal Society of Chemistry.