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AAPS J ; 15(2): 523-32, 2013 Apr.
Article in English | MEDLINE | ID: mdl-23389812

ABSTRACT

Diethylenetriamine pentaacetic acid penta-ethyl ester, designated as C2E5, was successfully incorporated into a nonaqueous gel for transdermal delivery. The thermal and rheological properties of a formulation containing 40% C2E5, 20% ethyl cellulose, and 40% Miglyol 840® prepared using the solvent evaporation method demonstrated that the gel had acceptable content uniformity and flow properties. In vitro studies showed that C2E5 was steadily released from the gel at a rate suitable for transdermal delivery. Topical application of the gel at a 200 mg C2E5/kg dose level in rats achieved significantly higher plasma exposures of several active metabolites compared with neat C2E5 oil at the same dose level. The results suggest that transdermal delivery of a chelator prodrug is an effective radionuclide decorporation strategy by delivering chelators to the circulation with a pharmacokinetic profile that is more consistent with the biokinetic profile of transuranic elements in contaminated individuals.


Subject(s)
Cellulose/analogs & derivatives , Chelating Agents/administration & dosage , Diglycerides/chemistry , Drug Carriers , Pentetic Acid/analogs & derivatives , Prodrugs/administration & dosage , Administration, Cutaneous , Animals , Biotransformation , Calorimetry, Differential Scanning , Cellulose/chemistry , Chelating Agents/chemistry , Chelating Agents/pharmacokinetics , Chemistry, Pharmaceutical , Delayed-Action Preparations , Drug Compounding , Female , Gels , Pentetic Acid/administration & dosage , Pentetic Acid/blood , Pentetic Acid/chemistry , Pentetic Acid/pharmacokinetics , Prodrugs/chemistry , Prodrugs/pharmacokinetics , Rats , Rats, Sprague-Dawley , Rheology , Skin Absorption , Solubility , Technology, Pharmaceutical/methods
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