Pharmacokinetic Evaluation of Biodistribution Data Obtained with Radiolabeled Proteins in Mice
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概要
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Radiolabeling of proteins is a widely used approach to study their in vivo disposition patterns. However, the obtained results may largely depend on the radiolabeling method used. The purpose of the present study was to investigate the effect of the radiolabeling method on the pharmacokinetic analysis of liver targeted protein in mice. Galactosylated bovine serum albumin (Gal-BSA) was labeled with ^<125>I or ^<111>In, using diethylenetriaminepentaacetic dianhydride (cDTPA) or 1-(4-isothiocyanobenzyl)ethylenediaminetetraacetic acid (SCN-Bz-EDTA) as bifunctional chelating agents. The Gal-BSA was then injected in mice by a bolus intravenous injection. Samples of plasma, urine, liver, kidney, intestine and feces were collected at various time intervals and their radioactivity was measured. In none of the samples examined was there any significant difference in radioactivity distribution originating from the radiolabeling methods within 5 min after administration. After this period, ^<125>I radioactivity in the liver started to decrease significantly faster than that of ^<111>In, which would indicate the intracellular degradation of the protein. Consequently, the reappearance of trichloracetic acid (TCA) soluble ^<125>I radioactivity in the plasma occurred. But whereas the hepatic uptake clearance (CL_<liver>) of [^<111>In]DTPA-Gal-BSA remained constant during 8 h postinjection, the CL_<liver> of [^<125>I]Gal-BSA at 30 min represented only one eighth of its initial values. The CL_<liver> of [^<111>In]SCN-Bz-EDTA-Gal-BSA resembled that of [^<111>In]DTPA-Gal-BSA within 1 h of the ecperiment but it started to decline after this interval. The observed discrepancies most probably resulted from the formation of different radiolabeled metabolites in the hepatocytes and their different capability of crossing biological membranes. Our findings indicate that among the three methods employed, [^<111>In]DTPA radiolabeling of Gal-BSA is the most appropriate method to study its tissue disposition.
- 社団法人日本薬学会の論文
- 1999-02-15
著者
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Hashida Mitsuru
Department Of Basic Pharmaceutics Faculty Of Pharmaceutical Sciences Kyoto University
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Hashida Mitsuru
京都大学 薬学研究科病態情報薬学
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Hashida Mitsuru
Dep. Of Drug Delivery Res. Graduate School Of Pharmaceutical Sciences Kyoto Univ. 46-29 Yoshidashimo
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Hashida Mitsuru
Inst. Of Integrated Cell-material Sciences (icems) Kyoto Univ.
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NISHIKAWA Makiya
Department of Drug Delivery Research, Graduate School of Pharmaceutical Sciences, Kyoto University
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Hashida M
Department Of Drug Delivery Research Graduate School Of Pharmaceutical Sciences Kyoto University
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Hashida Mitsuru
Graduate School Of Pharmaceutical Sciences Kyoto University
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TAKAKURA Yoshinobu
Department of Drug Delivery Research, Graduate School of Pharmaceutical Sciences, Kyoto University
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HASHIDA Mitsuru
京大院薬
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STAUD Frantisek
Department of Drug Delivery Research, Graduate School of Pharmaceutical Sciences, Kyoto University
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TAKEMURA Shigeo
Department of Drug Delivery Research, Graduate School of Pharmaceutical Sciences, Kyoto University
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Nishikawa Makiya
Department Of Biopharmaceutics And Drug Metabolism Graduate School Of Pharmaceutical Science Kyoto U
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Takakura Yoshinobu
Department Of Basic Pharmaceutics Faculty Of Pharmaceutical Sciences Kyoto University
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Takakura Yoshinobu
Department Of Drug Delivery Research Graduate School Of Pharmaceutical Sciences Kyoto University
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Nishikawa Makiya
京都大学 薬学研究科病態情報薬学
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Staud Frantisek
Department Of Drug Delivery Research Graduate School Of Pharmaceutical Sciences Kyoto University
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Nishikawa Makiya
Department Of Biopharmaceutics And Drug Metabolism Graduate School Of Pharmaceutical Sciences Kyoto
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Takemura Shigeo
Department Of Drug Delivery Research Graduate School Of Pharmaceutical Sciences Kyoto University
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