PMID- 18277609 OWN - NLM STAT- MEDLINE DCOM- 20080306 LR - 20190917 IS - 0253-6269 (Print) IS - 0253-6269 (Linking) VI - 31 IP - 1 DP - 2008 Jan TI - Differential receptor targeting of liver cells using 99mTc-neoglycosylated human serum albumins. PG - 60-6 AB - Neolactosyl human serum albumin (LSA) targets asialoglycoprotein receptor and shows high liver uptake due to accumulation in hepatocytes. Although neomannosyl human serum albumin (MSA) also shows high liver uptake, it has been reported to be taken up by Kupffer cells and endothelial cells. We compared the biological properties of LSA and MSA. 99mTc-LSA and 99mTc-MSA biodistribution in mice were investigated after intravenous injection. In vivo localization of rhodaminisothiocyanate (RITC)-LSA and fluoresceineisothiocyanate (FITC)-MSA were investigated in mouse liver. Excretion routes of 99mTc-LSA and 99mTc-MSA metabolites were examined. Both 99mTc-LSA and 99mTc-MSA showed high liver uptakes. RITC-LSA was taken up by hepatocytes whereas FITC-MSA was taken up by Kupffer cells and endothelial cells. 99mTc-MSA showed higher spleen and kidney uptakes than 99mTc-LSA. 99mTc-LSA metabolites excreted in urine and feces accounted for 44.4 and 50.0% of 99mTc-LSA injected, respectively, while 99mTc-MSA metabolites accounted for 51.5 and 10.3%, respectively. In conclusion, LSA is specifically taken up by hepatcytes while MSA by Kupffer cells and endothelial cells. After taken up by the liver, LSA is metabolized by the hepatocytes and then excreted through both the hepatobiliary tract and kidney, whereas MSA is metabolized by Kupffer cells and endoghelial cells and then excreted mainly through the kidney. FAU - Kim, Sungeun AU - Kim S AD - Department of Nuclear Medicine, Seoul National University College of Medicine, Seoul 110-744, Korea. FAU - Jeong, Jae Min AU - Jeong JM FAU - Hong, Mee Kyung AU - Hong MK FAU - Jang, Ja-June AU - Jang JJ FAU - Lee, Jaetae AU - Lee J FAU - Lee, Dong Soo AU - Lee DS FAU - Chung, June-Key AU - Chung JK FAU - Lee, Myung Chul AU - Lee MC LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - Korea (South) TA - Arch Pharm Res JT - Archives of pharmacal research JID - 8000036 RN - 0 (Albumins) RN - 0 (Carrier Proteins) RN - 0 (Radiopharmaceuticals) RN - 0 (Receptors, Drug) RN - 0 (Rhodamines) RN - 0 (Serum Albumin) RN - 0 (Technetium Tc 99m Aggregated Albumin) RN - 0 (lactosylated serum albumin) RN - 0 (mannosyl-neoglycoalbumin) RN - 7440-26-8 (Technetium) RN - BA7THR07HH (rhodamine isothiocyanate) RN - TPY09G7XIR (Fluorescein) SB - IM MH - Albumins/chemical synthesis/*pharmacokinetics MH - Animals MH - Carrier Proteins/*pharmacokinetics MH - Fluorescein/chemistry MH - Hepatocytes/diagnostic imaging MH - Humans MH - Isotope Labeling MH - Kupffer Cells/diagnostic imaging MH - Liver/cytology/*diagnostic imaging MH - Male MH - Mice MH - Mice, Inbred ICR MH - Microscopy, Confocal MH - Radionuclide Imaging MH - Radiopharmaceuticals/chemical synthesis/*pharmacokinetics MH - Rats MH - Rats, Sprague-Dawley MH - Receptors, Drug/*drug effects MH - Rhodamines/chemistry MH - Serum Albumin/chemical synthesis/*pharmacokinetics MH - Technetium/chemistry/pharmacokinetics MH - Technetium Tc 99m Aggregated Albumin/chemical synthesis/*pharmacokinetics MH - Tissue Distribution EDAT- 2008/02/19 09:00 MHDA- 2008/03/07 09:00 CRDT- 2008/02/19 09:00 PHST- 2008/02/19 09:00 [pubmed] PHST- 2008/03/07 09:00 [medline] PHST- 2008/02/19 09:00 [entrez] AID - 10.1007/s12272-008-1121-x [doi] PST - ppublish SO - Arch Pharm Res. 2008 Jan;31(1):60-6. doi: 10.1007/s12272-008-1121-x.