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• W1966389224 abstract "The physiological constraints imposed by the protective mechanisms of the eye lead to low absorption of drugs and a short duration of the therapeutic effect on ocular drug delivery. Upon instillation of the eye drops only 1–10% of the drug is bioavailable while the rest is drained out of the eye through lacrimal secretions [1]. To overcome this problem various approaches have been reported, such as ointments, inserts and aqueous gels, to increase the ocular residence time of topically applied medication.Controlled drug delivery to the eye offer several advantages over conventional therapies like drug solutions or suspensions as eye drops [2,3]. Ophthalmic inserts offer many advantages over conventional dosage forms, like increased ocular residence, possibility of releasing drugs at a slow and constant rate, accurate dosing, and exclusion of preservatives, increased shelf life and reduced systemic absorption [4–6]. Several reports revealed improved ocular therapy by ophthalmic inserts. Frequency of instillation of gentamycin sulfate was reduced by a long-acting ophthalmic insert [7]. O-butyryl ester prodrug of tilisolol and the O-palmitoyl ester prodrug of tilisolol were incorporated into an ophthalmic insert to control drug release [8]. Di Colo G. and co-researcher [9] observed respective contributions of diffusion and erosion to the release mechanism of drugs, namely prednisolone, oxytetracycline hydrochloride and gentamycin sulphate through erodible ophthalmic inserts based on poly(ethylene oxide).Acyclovir is a polar drug with short plasma half life of 2–3 h [10], therefore 4–5 times application is required when administered as ophthalmic ointment. Also, about 95% of the drug is drained out due to high tear turn-over via nasolacrimal drainage leading to ineffective therapy. Several approaches have been used to improve ocular bioavailabilty of acyclovir. Nanospheres of poly-d,l-lactic acid loaded with acyclovir were prepared and characterized for effect of different formulation parameters. Nanospheres showed a sustained acyclovir release, were highly tolerated by the eye and were able to increase the aqueous humor levels of acyclovir to improve the pharmacokinetic profile [11]. Fresta et al [12] prepared acyclovir-loaded polyethyl-2-cyanoacrylate (PECA) nanospheres by an emulsion polymerization process in the micellar phase and coated with polyethylene glycol (PEG). Acyclovir-loaded PEG-coated PECA nanospheres were compared with an aqueous solution of the drug for drug levels in aqueous humor. The acyclovir-loaded PEG-coated PECA nanospheres showed 25-fold increase in drug levels in aqueous humor compared with the free drug or the physical mixture.In the present investigation an attempt has been made to prepare ocular inserts of acyclovir capable of releasing drug continuously at controlled rate for 5 days." @default.
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• W1966389224 date "2008-01-25" @default.
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• W1966389224 title "Controlled Ocular Delivery of Acyclovir through Rate Controlling Ocular Insert of Eudragit: A Technical Note" @default.
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• W1966389224 doi "https://doi.org/10.1208/s12249-008-9032-1" @default.
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