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Phatsawee Jansook, Thorsteinn Loftsson, Einar Stefansson; Self-Assembled Dorzolamide/-Cyclodextrin Microparticle Eye Drops. Invest. Ophthalmol. Vis. Sci. 2011;52(14):235.
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© ARVO (1962-2015); The Authors (2016-present)
To develop novel aqueous dorzolamide eye drop formulation containing self-assembled drug/cyclodextrin (drug/CD) microparticles that enhance and prolong drug delivery to the eye.
The dorzolamide eye drop vehicle containing γCD microparticles and hydroxypropylmethylcellulose (HPMC) was developed. Physicochemical characterization and in vivo studies in rabbits were performed. The study adhered to the ARVO declaration for the use of laboratory animals in research. Ocular drug distribution was quantitative determination by UPLC-MS/MS systems.
The physicochemical properties of 3% w/v dorzolamide eye drop suspension (3%doz.) complied with the specifications of the eye drop suspension monograph of the European Pharmacopoeia. The in vivo testing of the formulation showed that the maximum dorzolamide concentration (Cmax) in aqueous humor after topical administration of 3%doz. and the commercially available 2% w/v dorzolamide eye drop solution (Trusopt®) was 5.4±3.6 and 2.2±1.5 µg/ml at tmax of 4 and 2 h, respectively (p<0.05) (Fig. 1). The dorzolamide concentration in aqueous humor at 4 and 8 h after single administration of 3%doz. was 13-fold and 45-fold higher, respectively, than that obtained after administration of Trusopt®. The eye drop suspension provided the sustained high dorzolamide concentrations for up to 24 h while the Trusopt® the dorzolamide concentration in aqueous humor was essentially zero 8 h after its administration (Fig. 1). Furthermore, this formulation delivered the drug to the posterior segment of the eye after topical administration.
The development of dorzolamide eye drop microparticle suspension containing γCD and HPMC as complexing and stabilizing agents, respectively, resulted in successful dorzolamide delivery to the aqueous humor and the posterior segment of the eye. This formulation has the potential of being developed into a once-a-day eye drop formulation leading to improve patient compliance.
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