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Synthesis, physicochemical properties and in vitro permeation studies of new ketorolac ester derivatives

Puglia, Carmelo and Filosa, Rosanna and Peduto, Antonella and De Caprariis, Paolo and Boatto, Gianpiero and Nieddu, Maria and Santagati, Natale Alfredo and Bonina, Francesco (2007) Synthesis, physicochemical properties and in vitro permeation studies of new ketorolac ester derivatives. Current Drug Delivery, Vol. 4 (3), p. 205-210. ISSN 1567-2018. Article.

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DOI: 10.2174/156720107781023893


Six new 1-alkylazacycloalkan-2-one esters of ketorolac (1-6) were synthesized and evaluated as potential dermal prodrugs. In vitro experiments were carried out to evaluate their chemical and enzymatic stability and permeation through excised human skin. Furthermore, partition coefficients n-octanol-water of ketorolac and its esters were determined to obtain information about their lipophilicity. Esters 1-6 showed increased lipophilicity compared to the parent drug, good stability in phosphate buffer pH 7.4, and were readily hydrolyzed in human plasma. Results from in vitro percutaneous absorption studies showed that, among all esters synthesized, only for esters 2 and 4 did a higher cumulative amount of drug penetrate through the skin, compared with that obtained after topical application of ketorolac.

Item Type:Article
ID Code:4461
Uncontrolled Keywords:Ketorolac, transdermal delivery, prodrug approach, in vitro
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
Publisher:Bentham Science
Deposited On:01 Sep 2010 15:13

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