Scintigraphic evaluation of the pharmacokinetics of a soluble polymeric drug carrier
Identifieur interne : 000307 ( Main/Exploration ); précédent : 000306; suivant : 000308Scintigraphic evaluation of the pharmacokinetics of a soluble polymeric drug carrier
Auteurs : RBID : ISTEX:259_1992_Article_BF00177374.pdfEnglish descriptors
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Abstract
There is a growing interest in the use of macromolecular carriers for therapeutic agents. If these carriers can be labelled with an appropriate gamma-emitter, their biodistribution could be followed by scintigraphy. We have imaged the biodistribution of a synthetic branched polypeptide, based on a poly-L-lysine backbone (average molecular mass 45 kDa). The polymer was conjugated to diethylene triamine penta-acetic acid and labelled by chelation with indium-111. Mice were injected i.v. with labelled material and imaged with a gamma-camera with a pin-hole collimator. Images showed the majority of tracer remaining in the blood pool, but about 35% appeared in the urinary bladder within 1.5 h. When the 111In-polymer was fractionated by gel filtration chromatography on S-300, the imaging showed that the early eluting material was retained, the intermediate showed some renal clearance, and the late was rapidly excreted. These findings show the value of gamma-scintigraphy for biodistribution studies with such polymeric drug carriers and its potential for clinical pharmacokinetic studies.
DOI: 10.1007/BF00177374
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<author><name>Malcolm V. Pimm</name>
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<author><name>Alan C. Perkins</name>
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<author><name>Ference Hudecz</name>
<affiliation wicri:level="1"><mods:affiliation>Research Group for Peptide Chemistry, Hungarian Academy of Science, L. Eötvös University, 1120, Budapest, Hungary</mods:affiliation>
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<front><div type="abstract" xml:lang="eng">There is a growing interest in the use of macromolecular carriers for therapeutic agents. If these carriers can be labelled with an appropriate gamma-emitter, their biodistribution could be followed by scintigraphy. We have imaged the biodistribution of a synthetic branched polypeptide, based on a poly-L-lysine backbone (average molecular mass 45 kDa). The polymer was conjugated to diethylene triamine penta-acetic acid and labelled by chelation with indium-111. Mice were injected i.v. with labelled material and imaged with a gamma-camera with a pin-hole collimator. Images showed the majority of tracer remaining in the blood pool, but about 35% appeared in the urinary bladder within 1.5 h. When the 111In-polymer was fractionated by gel filtration chromatography on S-300, the imaging showed that the early eluting material was retained, the intermediate showed some renal clearance, and the late was rapidly excreted. These findings show the value of gamma-scintigraphy for biodistribution studies with such polymeric drug carriers and its potential for clinical pharmacokinetic studies.</div>
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<abstract lang="eng">There is a growing interest in the use of macromolecular carriers for therapeutic agents. If these carriers can be labelled with an appropriate gamma-emitter, their biodistribution could be followed by scintigraphy. We have imaged the biodistribution of a synthetic branched polypeptide, based on a poly-L-lysine backbone (average molecular mass 45 kDa). The polymer was conjugated to diethylene triamine penta-acetic acid and labelled by chelation with indium-111. Mice were injected i.v. with labelled material and imaged with a gamma-camera with a pin-hole collimator. Images showed the majority of tracer remaining in the blood pool, but about 35% appeared in the urinary bladder within 1.5 h. When the 111In-polymer was fractionated by gel filtration chromatography on S-300, the imaging showed that the early eluting material was retained, the intermediate showed some renal clearance, and the late was rapidly excreted. These findings show the value of gamma-scintigraphy for biodistribution studies with such polymeric drug carriers and its potential for clinical pharmacokinetic studies.</abstract>
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<topic>Scintigraphy</topic>
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<relatedItem type="series"><titleInfo type="abbreviated"><title>Eur J Nucl Med</title>
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<titleInfo><title>European Journal of Nuclear Medicine</title>
<partNumber>Year: 1992</partNumber>
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<identifier type="issn">0340-6997</identifier>
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