Tumor targeting properties

The experiments reviewed in Section 13.1 demonstrated in detail that LCM can be labeled with lipophilic fluorescent dye and still retain their tumor-targeting properties. Furthermore, these lipophilic-dye-labeled LCM were shown to become internalized by tumor cells both in vitro and in vivo. This tumor-targeting ability of dye-labeled LCM, and their in vivo persistence at the tumor site and/or within the tumor cell for many minutes, suggested a potential use of LCM as a targeted drug-delivery agent or vehicle (ref. 532). Thus, a search was started for lipophilic anticancer drugs (preferably already FDA-approved for clinical use) that could be incorporated into the LCM and carried specifically to the tumor site. 

Song R, Kim Y-S, Sohn YS. Synthesis and selective tumor targeting properties of water soluble porphyrin-Pt(II) conjugates. J Inorg Biochem 2002 83 83-8. 

Heppeler A, Froidevaux S, Maecke HR, Jermann E, Behe M, Powell P, Hennig M. Radiometal-labelled macrocyclic chelator-derivatised somatostatin analogue with superb tumor-targeting properties and potential for receptor-mediated internal radiotherapy. Chem Eur J 1999 5 1974-1981. 

Shielded polyplexes with improved blood circulating properties are interesting tools for systemic cancer therapy (see Sect. 4.2). Nanoparticles can take advantage of the enhanced permeability and retention (EPR effect) [89] for passive tumor targeting. The EPR effect is based on the leakiness of tumor vasculature, due to neovascularization in growing tumors, combined with an inadequate lymphatic drainage. Nanoparticles with an elongated plasma circulation time can extravasate and passively accumulate at the tumor site. 

Milenic, D.E., Yokota, T., Filpula, D.R., Finkelman, M.A., Dodd, S.W., Wood, J.F. et al. (1991) Construction, binding properties, metabolism, and tumor targeting of a single-chain Fv derived from the pancarcinoma monoclonal antibody CC49. Cancer Res., 51, 6363-6371. 

Ishida O et al (2001) Liposomes bearing polyethyleneglycol-coupled transferrin with intracellular targeting property to the solid tumors in vivo. Pharm Res 18 1042-1048... 

Tumor and Normal Tissue Targeting Properties of mAbs and Peptides 885... 

TUMOR AND NORMAL TISSUE TARGETING PROPERTIES OF MABS AND PEPTIDES... 

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