| Differential effects of cyclodextrins and derivatives on the biological behavior of the myocardial perfusion imaging agent 99mTcN-NOET. | |
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MedLine Citation:
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PMID: 16000249 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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In addition to improving drug solubilization, cyclodextrins (CDs) also affect the biological behavior of the included compound. We evaluated the effects of two natural CDs beta-CD and gamma-CD, and six beta-CD derivatives, Dimeb, Trimeb, SBb, 2-HP, 6AD, and 6 MTU on the biological behavior of (99m)TcN-NOET, a technetium-99m-labeled, lipophilic compound readily detectable through radioactivity assessment. Determination of CDs' affinities for (99m)TcN-NOET indicated that the cavity size of gamma-CD was not suitable for (99m)TcN-NOET inclusion, and that beta-CD derivatization mostly resulted in decreased CDs affinities for (99m)TcN-NOET to various extents compared with the natural beta-CD. In vitro and ex vivo experiments performed on newborn rat cardiomyocytes and isolated perfused rat hearts, respectively, showed 1.7- and 2.3-fold maximal differences in (99m)TcN-NOET cellular and tissue activities. Regression analyzes indicated no significant correlation between these observed biological differences and the affinities of the eight CDs tested for (99m)TcN-NOET or for cellular membranes. In conclusion, CD derivatization often resulted in impaired affinity of the derivatives for the lipophilic compound (99m)TcN-NOET. Moreover, the in vitro and ex vivo biological behavior of (99m)TcN-NOET was greatly affected depending on the CD used for inclusion of the tracer. |
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Authors:
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Laurent Riou; Catherine Ghezzi; Denis Wouessidjewe; Ho Law; Jean-Paul Mathieu; Jacques Defaye; René Bontron; Roberto Pasqualini; Daniel Fagret |
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Publication Detail:
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Type: In Vitro; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik e.V Volume: 61 ISSN: 0939-6411 ISO Abbreviation: Eur J Pharm Biopharm Publication Date: 2005 Sep |
Date Detail:
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Created Date: 2005-08-08 Completed Date: 2005-11-10 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 9109778 Medline TA: Eur J Pharm Biopharm Country: Netherlands |
Other Details:
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Languages: eng Pagination: 40-9 Citation Subset: IM |
Affiliation:
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INSERM E0340 Radiopharmaceutiques Biocliniques, Faculté de Médecine de Grenoble, Domaine de la Merci, La Tronche, France. laurent.riou@ujf-grenoble.fr |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Animals, Newborn Cyclodextrins / chemistry*, pharmacokinetics Dogs Heart / radionuclide imaging* Linear Models Male Myocardium / metabolism* Myocytes, Cardiac / metabolism* Organotechnetium Compounds / chemistry, pharmacokinetics* Rats Rats, Wistar Solubility Thiocarbamates / chemistry, pharmacokinetics* |
| Chemical | |
Reg. No./Substance:
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0/Cyclodextrins; 0/Organotechnetium Compounds; 0/Thiocarbamates; 0/technetium Tc 99m, bis(N-ethoxy-N-ethyldithiocarbamato)nitrido- |
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