| Biodistribution and pharmacokinetics of PEG-10kDa-cholecystokinin-10 in rats after different routes of administration. | |
| | |
MedLine Citation:
|
PMID: 20158487 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
Cholecystokinin, produced in the proximal small intestine, is a short acting satiating peptide hormone. CCK-10, before and after mono-iodination, was previously coupled to 10kDa polyethylene glycol (PEG). The formed conjugates PEG10kDa-CCK-10 and PEG10kDa-[(127)I]-CCK-10 show after i.p. administration to rats a sustained food intake reduction during 8h in comparison to 2h for free CCK-10. The present study examined the blood pharmacokinetics of this pharmacological interesting molecule by means of PEG10kDa-[(123)I]-CCK-10 following intravenous, intraperitoneal, intramuscular and nasal administration and the biodistribution after i.p. administration. HPLC analysis with radiometric detection allowed the differentiation between inorganic iodide and the intact tracer in blood. Blood kinetics after i.v. injection was fitted to a bi-exponential with a distribution half-life of 15 min and with an elimination half-life of 8 hours for intact PEG10kDa-[(123)I]-CCK-10. The biodistribution studies showed a higher accumulation of the tracer for all administration routes in organs expressing CCK receptors localized in the gastrointestinal tract such as pancreas, duodenum and small intestine. No indication of blood brain barrier crossing for the conjugate could be observed independently of the administration route. Main clearance was via the urinary pathway. |
| | |
Authors:
|
Fabián León-Tamariz; Isabelle Verbaeys; Maurits Van Boven; Marcel De Cuyper; Johan Buyse; Peter de Witte; Alfons Verbruggen; Marnix Cokelaere |
Related Documents
:
|
9475207 - Superior mesenteric artery blood flow in patients with small bowel diseases: evaluation... 12069257 - Equine endotoxemia: pathomorphological aspects of endotoxin-induced damage in equine me... 8901747 - Diminished postprandial hyperemia in patients with aortic and mesenteric arterial occlu... 976807 - Ischaemic colitis in the experimental animal. ii. role of hypovolaemia in the productio... 4092367 - Regional o2 supply/consumption in normal and ischaemic rabbit myocardium: effect of nif... 20655537 - Real-time assessment of flow reversal in an eccentric arterial stenotic model. |
Publication Detail:
|
Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
|
Title: Current drug delivery Volume: 7 ISSN: 1875-5704 ISO Abbreviation: Curr Drug Deliv Publication Date: 2010 Apr |
Date Detail:
|
Created Date: 2010-04-20 Completed Date: 2010-07-09 Revised Date: - |
Medline Journal Info:
|
Nlm Unique ID: 101208455 Medline TA: Curr Drug Deliv Country: United Arab Emirates |
Other Details:
|
Languages: eng Pagination: 137-43 Citation Subset: IM |
Affiliation:
|
Laboratory of Toxicology and Bromatology, Faculty of Pharmaceutical Sciences; Katholieke Universiteit Leuven, Leuven, Belgium. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Animals Cholecystokinin / administration & dosage, blood*, urine Drug Administration Routes Drug Carriers / administration & dosage, chemical synthesis, chemistry, pharmacokinetics* Half-Life Iodine Radioisotopes / blood*, urine Male Peptide Fragments / administration & dosage, blood*, urine Polyethylene Glycols / administration & dosage, chemistry, pharmacokinetics* Rats Rats, Wistar Tissue Distribution |
| Chemical | |
Reg. No./Substance:
|
0/Drug Carriers; 0/Iodine Radioisotopes; 0/Peptide Fragments; 0/Polyethylene Glycols; 25842-57-3/cholecystokinin 10 C-terminal fragment; 9011-97-6/Cholecystokinin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Characterization of Peptide Polymer Interactions in Poly(alkylcyanoacrylate) Nanoparticles: A Mass S...
Next Document: Dextran Carrier Macromolecule for Colon Specific Delivery of Celecoxib.