T. Tanaka et al., THE DISPOSITION OF SERUM-PROTEINS AS DRUG-CARRIERS IN MICE BEARING SARCOMA-180, Biological & pharmaceutical bulletin, 16(12), 1993, pp. 1270-1275
The tumor distribution and the disposition of serum proteins, such as
albumin, fetuin, transferrin, and IgG, were investigated in mice beari
ng Sarcoma 180. Serum proteins labeled with fluoresceinisothiocyante (
FITC) we mice in order to investigate the effect of chemical modificat
ion. The plasma concentration of each glutarylated serum protein was s
ignificantly lower, about 15 to 46-fold, in comparison to that of the
non-acylated protein at 24 h after administration. The tissue distribu
tions of the glutarylated serum proteins were also decreased compared
to those of the non-acylated proteins. Especially, the hepatic distrib
ution of albumin and IgG was significantly reduced with glutarylation.
The urinary excretion of albumin and transferrin, and fecal excretion
of IgG, were significantly increased with glutarylation. The serum pr
oteins were accumulated effectively in the tumor tissue in mice bearin
g Sarcoma 180. It was found that the tumor distributions were not impa
ired by the glutarylation, except involving fetuin. It was suggested,
therefore, that the glutarylated serum proteins were valuable for rela
tive tumor-selectivity and might be utilized in a macromolecular carri
er system for antitumor drugs.