Kinetics of γ-cyclodextrin nanoparticle suspension eye drops in tear fluid.
Cast your vote
You can rate an item by clicking the amount of stars they wish to award to this item.
When enough users have cast their vote on this item, the average rating will also be shown.
Your vote was cast
Thank you for your feedback
Thank you for your feedback
Moya-Ortega, Maria D
Ásgrímsdóttir, Gudrún Marta
Lund, Sigrún H
MetadataShow full item record
CitationActa Ophthalmol. 2014, 92 (6):550-6
AbstractWe have developed nanoparticle γ-cyclodextrin dexamethasone (DexNP) and dorzolamide (DorzNP) eye drops that provide sustained high drug concentrations on the eye surface. To test these characteristics, we measured dexamethasone and dorzolamide levels in tear fluid in humans following eye drop administration.
Concentration of dexamethasone was measured by mass spectrometry. One drop of DexNP was instilled into one eye. Tear fluid was sampled with microcapillary pipettes at seven time-points after drop instillation. Control eyes received Maxidex(®) (dexamethasone). The same procedure was performed for dorzolamide with DorzNP and Trusopt(®) .
Six subjects were included in each group. The peak concentration (μg/ml ± standard deviation) of dexamethasone for DexNP eye drops (636.6 ± 399.1) was up to 19-fold higher than with Maxidex(®) (39.3 ± 18.9) (p < 0.001). At 4 hr, DexNP was still 10 times higher than Maxidex(®) . In addition, DexNP resulted in about 30-fold higher concentration of dissolved dexamethasone in the tear fluid of extended time period allowing more drug to partition into the eye tissue. The overall concentration of dorzolamide was about 50% higher for DorzNP (59.5 ± 76.9) than Trusopt(®) (40.0 ± 76.7) (p < 0.05).
The results indicate high and extended concentration of dissolved dexamethasone with DexNP, which can explain the greater and longer lasting effect of dexamethasone in the cyclodextrin nanoparticle drug delivery platform. Dexamethasone seems to fit the cyclodextrin nanoparticle suspension drug delivery platform with longer duration and higher concentrations in tear fluid than available commercial drops, while dorzolamide is less suitable.
DescriptionTo access publisher's full text version of this article click on the hyperlink at the bottom of the page
RightsArchived with thanks to Acta ophthalmologica
- γ-Cyclodextrin nanoparticle eye drops with dorzolamide: effect on intraocular pressure in man.
- Authors: Gudmundsdottir BS, Petursdottir D, Asgrimsdottir GM, Gottfredsdottir MS, Hardarson SH, Jóhannesson G, Kurkov SV, Jansook P, Loftsson T, Stefánsson E
- Issue date: 2014 Feb
- Dorzolamide cyclodextrin nanoparticle suspension eye drops and Trusopt in rabbit.
- Authors: Jóhannesson G, Moya-Ortega MD, Asgrímsdóttir GM, Agnarsson BA, Lund SH, Loftsson T, Stefánsson E
- Issue date: 2014 Aug
- Topical drug delivery to the eye: dorzolamide.
- Authors: Loftsson T, Jansook P, Stefánsson E
- Issue date: 2012 Nov
- Cyclodextrin microparticles for drug delivery to the posterior segment of the eye: aqueous dexamethasone eye drops.
- Authors: Loftsson T, Hreinsdóttir D, Stefánsson E
- Issue date: 2007 May
- Cyclodextrin solubilization of carbonic anhydrase inhibitor drugs: formulation of dorzolamide eye drop microparticle suspension.
- Authors: Jansook P, Stefánsson E, Thorsteinsdóttir M, Sigurdsson BB, Kristjánsdóttir SS, Bas JF, Sigurdsson HH, Loftsson T
- Issue date: 2010 Oct