Pentapeptide YIGSR‐mediated HT‐1080 fibrosarcoma cells targeting of adriamycin encapsulated in sterically stabilized liposomes

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Abstract
In the peptide‐targeted therapy for cancer, peptides are used to reach a selective and specific target in cancer cells. Peptides are used free or coupled to chemotherapeutic drugs, phagues, proteins, polymers, liposomes, and polymer‐grafted liposomes. Using this latter approach, the pentapeptide YIGSR was coupled to the distal end from carboxyl groups of liposome‐grafted polyethyleneglycol (PEG) chains (YIGSR‐PEG‐liposome). As a control, the peptide PEAGD coupled to PEG‐liposome was used. The biological activity of YIGSR‐PEG‐liposome was tested using HT‐1080 human fibrosarcoma cells. In adhesion assays, the YIGSR‐PEG‐liposome coated to plastic plates promoted 30% of the specific cell attachment. In competition assays, YIGSR‐PEG‐liposome inhibited the specific attachment of cells to laminin‐1‐coated plates by 25%. Following this, we prepared peptide‐PEG‐liposomes encapsulating adriamycin (ADR). In vitro cytotoxicity assays against HT‐1080 cells gave IC50 values 2.1 times lower for YIGSR‐PEG‐liposomal ADR in comparison to PEAGD‐PEG‐liposomal ADR. The free peptide added in excess increased the IC50 value of YIGSR‐PEG‐liposomal ADR by 72%, while the IC50 value of control liposomal ADR was unaffected, supporting a receptor‐mediated mechanism of targeting. In addition, the lower IC50 value is correlated with a higher total of ADR accumulation in the cells. © 2004 Wiley Periodicals, Inc. J Biomed Mater Res 69A: 155–163, 2004

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