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

Francesca Maestrelli, Paola Mura, Angela Casini, Francesco Mincione, Andrea Scozzafava, Claudiu T. Supuran

Research output: Contribution to journalArticlepeer-review

21 Scopus citations

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.

Original languageEnglish
Pages (from-to)2211-2219
Number of pages9
JournalJournal of Pharmaceutical Sciences
Volume91
Issue number10
DOIs
StatePublished - Oct 2002
Externally publishedYes

Keywords

  • Carbonic anhydrase
  • Cyclodextrin
  • Glaucoma
  • Intraocular pressure
  • Sulfonamide

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