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Cyclodextrin complexes of sulfonamide carbonic anhydrase inhibitors as long-lasting topically acting antiglaucoma agents

Maestrelli, F., Mura, P., Casini, Angela, Mincione, F., Scozzafava, A. and Supuran, C.T. 2002. Cyclodextrin complexes of sulfonamide carbonic anhydrase inhibitors as long-lasting topically acting antiglaucoma agents. Journal of Pharmaceutical Sciences 91 (10) , pp. 2211-2219. 10.1002/jps.10215

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Abstract

Complexes of several 1,3,4-thiadiazole-2-sulfonamide derivatives possessing strong carbonic anhydrase (CA) inhibitory properties with β-cyclodextrin and hydroxypropyl-β-cyclodextrin were obtained and characterized. Although the investigated CA inhibitors possessed very powerful inhibitory properties against the two CA isozymes involved in aqueous humor production within the eye, i.e., CA II and CA IV, these compounds were topically ineffective as intraocular pressure (IOP) lowering agents in normotensive/hypertensive rabbits, due to their very low water solubility. On the contrary, the cyclodextrin–sulfonamide complexes proved to be effective and long-lasting IOP lowering agents in the two animal models of glaucoma mentioned above. © 2002 Wiley-Liss Inc. and the American Pharmaceutical Association J Pharm Sci 91:2211–2219, 2002

Item Type: Article
Date Type: Publication
Status: Published
Schools: Chemistry
Subjects: Q Science > QD Chemistry
Publisher: Wiley
ISSN: 1520-6017
Date of Acceptance: 7 May 2002
Last Modified: 04 Jun 2017 08:49
URI: http://orca.cf.ac.uk/id/eprint/85553

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Cited 14 times in Web of Science. View in Web of Science.

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