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  • Title: Design of folate-linked liposomal doxorubicin to its antitumor effect in mice.
    Author: Yamada A, Taniguchi Y, Kawano K, Honda T, Hattori Y, Maitani Y.
    Journal: Clin Cancer Res; 2008 Dec 15; 14(24):8161-8. PubMed ID: 19088031.
    Abstract:
    PURPOSE: Tumor cell targeting is a promising strategy for enhancing the therapeutic potential of chemotherapy agents. Polyethylene glycol (PEG)-coated (sterically stabilized) liposomes show enhanced accumulation on the surface of tumors, but steric hindrance by PEGylation reduces the association of the liposome-bound ligand with its receptor. To increase folate receptor (FR) targeting, we optimized the concentration and PEG spacer length of folate-PEG-lipid in liposomes. EXPERIMENTAL DESIGN: Three types of folate-linked liposomal doxorubicin were designed and prepared by optimizing the concentration and PEG spacer length of folate-PEG-lipid in PEGylated or non-PEGylated liposomes and by masking folate-linked liposomes where the folate ligand is "masked" by adjacent PEG spacers. The liposome targeting efficacy was evaluated in vitro and in vivo. RESULTS: In human oral carcinoma KB cells, which overexpress FR, modification with sufficiently long PEG spacer and a high concentration of folate ligand to non-PEGylated liposomes increased the FR-mediated association and cytotoxicity more than with PEGylated and masked folate-linked liposomes. On the contrary, in mice bearing murine lung carcinoma M109, modification with the folate ligand in PEGylated and masked folate-linked liposomes showed significantly higher antitumor effect than with non-PEGylated liposomes irrespective of the length of time in the circulation after intravenous injection. CONCLUSIONS: The results of this study will be beneficial for the design and preparation of ligand-targeting carriers for cancer treatment.
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