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Abstract

Mitomycin C-Dextran conjugates (MMC-D) were intravenously (iv) injected in mice bearing subcutaneous sarcoma 180. The tissue distribution was determined for three 14-C-labeled anionic conjugates (MMC-Dan) with molecular weights of 10, 70, and 500 kd and one cationic 70-kd 14C-conjugate (MMC-Dcat). The anionic conjugates were slowly cleared from the plasma, and their elimination rate decreased with increasing molecular weight. Radioactivity accumulated in liver, spleen, lymph nodes, and tumor but not in heart, lung, intestines, kidney, or muscle after iv injection of all types of 14C-MMC-Dan. In contrast, the cationic conjugate was rapidly cleared from the plasma and accumulated mostly in the liver and spleen, while tumor levels remained low. The antitumor effect of the 70-kd MMC-Dan, which afforded the highest tumor concentration, was superior to that of free MMC. Therefore, anionic mitomycin C-dextran conjugates with a high molecular weight may be useful for tumor targeting in cancer chemotherapy.

Biodistribution and Pharmacokinetics of O-Palmitoyl Tilisolol, a Lipophilic Prodrug of Tilisolol, after Intravenous Administration in Rats.

“…13) Palmitic acid is a biological lipid component. Therefore, it is expected that the palmitoyl functional group may enhance the affinity of the parent drug on the hydrophobic components in systemic circulation, resulting in increasing their apparent molecular weight.…”

Receptor Mediated Endocytosis and Cytotoxicity of Transferrin-Mitomycin C Conjugate in the HepG2 Cell and Primary Cultured Rat Hepatocyte.

“…The drug targeting system is expected to overcome the side effects and increase its therapeutic efficacy. A variety of macromolecular conjugates of MMC have been demonstrated, e.g., antibodies, [10][11][12] glycoprotein, 13) albumin, 14,15) dextran, 16) and synthetic macromolecules such as polylysine. 17) Transferrin receptors were found to be more widely distributed on the tumor tissues than the normal tissues.…”

Antitumor Properties of Irinotecan-Containing Nanoparticles Prepared Using Poly(DL-lactic acid) and Poly(ethylene glycol)-block-poly(propylene glycol)-block-poly(ethylene glycol).

“…As a control, saline alone of similar volume was injected on the same schedule. Tumor volume (V, cm 3 ) was calculated from the length of the longest axis (L, cm) and the length of the vertical axis to the longest one, width, (W, cm) by the following equation 17) :…”