In order to facilitate the intracellular delivery of macromolecules, Pep-1 peptide-modified liposomal (Pep1-Lipo) nanocarriers were designed and examined for their in vitro cell translocation capability. Pep-1 peptides were coupled via thiol-maleimide linkage to small unilamellar vesicles composed of phosphatidylcholine, Tween 80, and N-[4-(p-maleimidophenyl)butyryl]-phosphatidylethanolamine (MPB-PE). The amount of Pep-1 peptide conjugated to the vesicle was effectively controlled by the amounts of maleimide groups on the vesicular surface, ranging from 70 to 700 molecules per vesicle. Systems were evaluated for cell uptake capacity by monitoring entrapped fluorescence-labeled bevacizumab, a model protein for poorly permeable macromolecule, using confocal microscopy. The novel carriers rapidly bound to the cell membrane and migrated into the cells within 1 h, exhibiting better translocation of macromolecules compared to that of conventional liposomes. Cellular uptake of Pep1-Lipo was proportional to the amount of Pep-1 peptide on the liposomal surface. In conclusion, we found that the Pep1-Lipo formulation was a promising nanocarrier system for intracellular delivery of macromolecules.

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