Formulation, drug aqueous humor

The following types of mucoadhesive preparations have been evaluated for ocular drug delivery hydrogels, viscous liquids, solids (inserts), and particulate formulations [57]. Hui and Robinson [58] introduced hydrogels consisting of cross-linked polyacrylic acid for ocular delivery of progesterone in rabbits. These preparations increased progesterone concentrations in the aqueous humor four times over aqueous suspensions. 

Dorzolamide Hydrochloride is an inhibitor of human carbonic anhydrase II. The inhibition of carbonic anhydrase in the ciliary processes of the eye decreases the secretion of aqueous humor, with a resulting reduction in intraocular pressure. The drug is formulated as an ophthalmic solution, and administered topically as eyedrops. 

Cmax) of the drug in the aqueous humor of rabbits was comparable with all three formulations, whereas the time to peak concentration (tmax) occurred much later with the ointment, leading to a significantly greater total bioavailability of the drug. 

Side effects associated with use of topical tretinoin ointment include transient hyperemia, irritation, or burning. Ocular pharmacokinetic studies in rabbits show low levels of drug in the aqueous humor after topical application of [ H]-tretinoin, with major tissue uptake in the surface epithelium and the iris. Because retinoic acid has poor stability in the presence of light and oxygen and is insoluble in water, its formulations and clinical use are limited. Although it is capable of reversing squamous metaplasia and keratinization, these ocular surface changes are seen only in severe, not mild to moderate, cases of dry eye. 

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