Abstract |
Two new sulfonamides incorporating arylsulfonylureido moieties were complexed with gamma cyclodextrin (γ-CD), hydroxypropyl-gamma cyclodextrin (HPγ-CD), hydroxypropyl-beta cyclodextrin (HPβ-CD) and hydroxyethyl- beta cyclodextrin (HEβ-CD) in order to obtain drug formulations with effective topical intraocular pressure (IOP) lowering effects, in an animal model of glaucoma. The HPγ-CD was the best solubilizing agent for the two sulfonamides and its complexes were characterized in detail and administered to rabbits with eye hypertension of 45-50 mmHg. The peak IOP lowering was observed after 1h post-administration and was of 36-37 mmHg. A low IOP pressure (of around-35 mmHg) was then maintained for the next 24h post-administration, which has not been observed before with any IOP lowering drug.
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Authors | Marco Bragagni, Murat Bozdag, Fabrizio Carta, Andrea Scozzafava, Cecilia Lanzi, Emanuela Masini, Paola Mura, Claudiu T Supuran |
Journal | Bioorganic & medicinal chemistry
(Bioorg Med Chem)
Vol. 23
Issue 18
Pg. 6223-7
(Sep 15 2015)
ISSN: 1464-3391 [Electronic] England |
PMID | 26319622
(Publication Type: Journal Article)
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Copyright | Copyright © 2015 Elsevier Ltd. All rights reserved. |
Chemical References |
- Carbonic Anhydrase Inhibitors
- Cyclodextrins
- Sulfonamides
- benzenesulfonamide
- Carbonic Anhydrases
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Topics |
- Administration, Topical
- Animals
- Carbonic Anhydrase Inhibitors
(chemistry, pharmacology, therapeutic use)
- Carbonic Anhydrases
(chemistry, metabolism)
- Chemistry, Pharmaceutical
- Cyclodextrins
(chemistry)
- Disease Models, Animal
- Glaucoma
(drug therapy)
- Humans
- Intraocular Pressure
(drug effects)
- Male
- Rabbits
- Solubility
- Sulfonamides
(chemistry, pharmacology, therapeutic use)
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