2.50
Hdl Handle:
http://hdl.handle.net/2336/21752
Title:
Dexamethasone delivery to posterior segment of the eye
Authors:
Loftsson, T; Sigurdsson, H.H; Hreinsdottir, D; Konradsdottir, F; Stefánsson, E
Citation:
Journal of Inclusion Phenomena and Macrocyclic Chemistry 2007, 57(1):585-9
Issue Date:
1-Apr-2007
Abstract:
Due to anatomic barriers and lacrimal drainage it is difficult to obtain therapeutic drug concentrations in the posterior part of the eye after topical drug administrations. Lipophilic cyclodextrins, such as randomly methylated β-cyclodextrin (RMβCD), are known to act both as solubilizers of water-insoluble drugs in aqueous solutions and as penetration enhancers that reduce the barrier function of lipophilic membranes. The purpose of this study was to investigate the effects of RMβCD on dexamethasone delivery from aqueous eye drop solution into rabbit eyes. Dexamethasone (0.5 and 1.5% w/v) drops (50 μl) were administered to the left eye of rabbits (n = 6) and the drug levels measured in different eye tissues 2 h after administration. In aqueous humor dexamethasone levels were 1,190 ± 110 and 1,670 ± 630 ng/g (mean ± SD) after administration of the 0.5 and 1.5% dexamethasone eye drops, respectively. In the retina the levels were 33 ± 7 and 66 ± 49 ng/g, and in optic nerve 41 ± 12 and 130 ± 50 ng/g, respectively. In a previous study the dexamethasone concentration in aqueous humor after topical administration of 1.3% (w/v) dexamethasone eye drops in aqueous 2-hydroxypropyl-β-cyclodextrin (HPβCD) solution was determined to be 320 ± 230 ng/g and 66 ± 20 ng/g after administration of Maxidex® eye drops. Both the hydrophilic HPβCD and the lipophilic RMβCD enhance topical dexamethasone delivery into the eye, but of the two, the lipophilic RMβCD results in higher dexamethasone concentrations.
Description:
To access publisher full text version of this article. Please click on the hyperlink in Additional Links field
Additional Links:
http://www.springerlink.com/content/e57q3nt20l23n007

Full metadata record

DC FieldValue Language
dc.contributor.authorLoftsson, T-
dc.contributor.authorSigurdsson, H.H-
dc.contributor.authorHreinsdottir, D-
dc.contributor.authorKonradsdottir, F-
dc.contributor.authorStefánsson, E-
dc.date.accessioned2008-03-27T15:51:41Z-
dc.date.available2008-03-27T15:51:41Z-
dc.date.issued2007-04-01-
dc.date.submitted2008-03-28-
dc.identifier.citationJournal of Inclusion Phenomena and Macrocyclic Chemistry 2007, 57(1):585-9en
dc.identifier.issn09230750-
dc.identifier.issn15731111-
dc.identifier.doi10.1007/s10847-006-9253-4-
dc.identifier.urihttp://hdl.handle.net/2336/21752-
dc.descriptionTo access publisher full text version of this article. Please click on the hyperlink in Additional Links fielden
dc.description.abstractDue to anatomic barriers and lacrimal drainage it is difficult to obtain therapeutic drug concentrations in the posterior part of the eye after topical drug administrations. Lipophilic cyclodextrins, such as randomly methylated β-cyclodextrin (RMβCD), are known to act both as solubilizers of water-insoluble drugs in aqueous solutions and as penetration enhancers that reduce the barrier function of lipophilic membranes. The purpose of this study was to investigate the effects of RMβCD on dexamethasone delivery from aqueous eye drop solution into rabbit eyes. Dexamethasone (0.5 and 1.5% w/v) drops (50 μl) were administered to the left eye of rabbits (n = 6) and the drug levels measured in different eye tissues 2 h after administration. In aqueous humor dexamethasone levels were 1,190 ± 110 and 1,670 ± 630 ng/g (mean ± SD) after administration of the 0.5 and 1.5% dexamethasone eye drops, respectively. In the retina the levels were 33 ± 7 and 66 ± 49 ng/g, and in optic nerve 41 ± 12 and 130 ± 50 ng/g, respectively. In a previous study the dexamethasone concentration in aqueous humor after topical administration of 1.3% (w/v) dexamethasone eye drops in aqueous 2-hydroxypropyl-β-cyclodextrin (HPβCD) solution was determined to be 320 ± 230 ng/g and 66 ± 20 ng/g after administration of Maxidex® eye drops. Both the hydrophilic HPβCD and the lipophilic RMβCD enhance topical dexamethasone delivery into the eye, but of the two, the lipophilic RMβCD results in higher dexamethasone concentrations.en
dc.language.isoenen
dc.publisherKluwer Academic Publishersen
dc.relation.urlhttp://www.springerlink.com/content/e57q3nt20l23n007en
dc.subject.meshCyclodextrinen
dc.subject.meshOphthalmic Solutionsen
dc.subject.meshSteroidsen
dc.titleDexamethasone delivery to posterior segment of the eyeen
dc.typeArticleen
dc.identifier.journalJournal of Inclusion Phenomena and Macrocyclic Chemistryen
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