oregon-green-488-carboxylic-acid and Carcinoma

The synthesis of a 10.5 kDa and a 52.5 kDa polymer, based on pHPMA functionalized with tyramine for (18) F-labeling and a folate derivative as targeting moiety, is reported. FCS studies are conducted using Oregon Green-labeled conjugates. No aggregation is observed for the 10.5 kDa conjugate, but strong aggregation for the 52.5 kDa conjugate. In vivo studies are conducted using Walker-256 mammary carcinoma model to determine body distribution as function of size and especially targeting unit. These in vivo studies show a higher short time (2 h) accumulation for both conjugates in the tumor than for untargeted pHPMA, confirmed by blockade studies. The 10.5 kDa polymer accumulates with 0.46% ID g(-1) and the 52.5 kDa polymer with 0.28% ID g(-1) in the tumor after 2 h, demonstrating the potential of the folate-targeting concept.

Topics: Animals; Benzenesulfonates; Carboxylic Acids; Carcinoma; Cell Line, Tumor; Contrast Media; Drug Carriers; Female; Fluorine Radioisotopes; Folate Receptors, GPI-Anchored; Folic Acid; Gene Expression; Isotope Labeling; Mammary Neoplasms, Animal; Molecular Targeted Therapy; Polymethacrylic Acids; Positron-Emission Tomography; Rats; Tissue Distribution; Tyramine