biostudies-literatureBiswas SNCI NIH HHS517-25https://www.ebi.ac.uk/biostudies/studies/S-EPMC4157068biostudies-literatureUnknown84(3)Doxorubicin-loaded PEGylated liposomes (commercially available as DOXIL or Lipodox) were surface functionalized with a cell-penetrating peptide, octa-arginine (R8). For this purpose, R8-peptide was conjugated to the polyethylene glycol-dioleoyl phosphatidylethanolamine (PEG-DOPE) amphiphilic co-polymer. The resultant R8-PEG-PE conjugate was introduced into the lipid bilayer of liposomes at 2 mol% of total lipid amount via spontaneous micelle-transfer technique. The liposomal modification did not alter the particle size distribution, as measured by Particle Size Analyzer and transmission electron microscopy (TEM). However, surface-associated cationic peptide increased zeta potential of the modified liposomes. R8-functionalized liposomes (R8-Dox-L) markedly increased the intracellular and inEuropean journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.VSurface functionalization of doxorubicin-loaded liposomes with octa-arginine for enhanced anticancer activity.PMC4157068R01 CA 128486R01 CA121838R01 CA128486Deshpande PPBiswas SDodwadkar NSParab STorchilin VPfalseSurface functionalization of doxorubicin-loaded liposomes with octa-arginine for enhanced anticancer activity.Doxorubicin-loaded PEGylated liposomes (commercially available as DOXIL or Lipodox) were surface functionalized with a cell-penetrating peptide, octa-arginine (R8). For this purpose, R8-peptide was conjugated to the polyethylene glycol-dioleoyl phosphatidylethanolamine (PEG-DOPE) amphiphilic co-polymer. The resultant R8-PEG-PE conjugate was introduced into the lipid bilayer of liposomes at 2 mol% of total lipid amount via spontaneous micelle-transfer technique. The liposomal modification did not alter the particle size distribution, as measured by Particle Size Analyzer and transmission electron microscopy (TEM). However, surface-associated cationic peptide increased zeta potential of the modified liposomes. R8-functionalized liposomes (R8-Dox-L) markedly increased the intracellular and in2013-01-01T00:00:00Z2013 Aug2025-04-19T08:54:56.37Z2019-03-27T01:35:20ZS-EPMC41570682333389910.1016/j.ejpb.2012.12.021