Drug Delivery · 2022 · 54 citations · 27 references
PharmacyOphthalmologyPharmaceuticsBiomaterialsDrug DeliveryOphthalmic Drug DeliveryCorneal Drug DeliveryIn Situ Ocular GelsMucoadhesive Ocular DeliveryOphthalmic FormulationsOphthalmic GelsTopical Ocular Drug DeliveryChitosanConjunctival IrritationCorneal MucoadhesionGelationHybrid Drug Delivery SystemsMucoadhesive In Situ GelsMucoadhesive Ophthalmic FormulationsMucoadhesive Ophthalmic Gels
PURPOSE: gels have been around for decades but only a few have been translated into ophthalmic pharmaceuticals. The aim of this study was to combine the thermo-gelling polymer poloxamer 407 and mucoadhesive polymers chitosan (CS) and methyl cellulose (MC) for developing effective and long-acting ophthalmic delivery systems for L-carnosine (a natural dipeptide drug) for corneal wound healing. METHODS: permeation were studied. Healing of corneal epithelium ulcers was investigated in a rabbit's eye model. RESULTS: Both gelation time and temperature were significantly dependent on the concentrations of poloxamer 407 and additive polymers (chitosan and methyl cellulose), where it ranged from <10 s to several minutes. Mechanical properties investigated through texture analysis (hardness, adhesiveness, and cohesiveness) were dependent on composition. Promising spreading-ability, mucoadhesion, transcorneal permeation of L-carnosine, high ocular tolerability, and enhanced corneal epithelium wound healing were recorded for poloxamer 407/chitosan systems. CONCLUSION: gelling systems comprising combinations of poloxamer-chitosan exhibited superior gelation time and temperature, mucoadhesion, and rheological characteristics suitable for effective long-acting drug delivery systems for corneal wounds.
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Taís Gratieri, Guilherme M. Gelfuso, Osvaldo de Freitas et al. · European Journal of Pharmaceutics and Biopharmaceutics · 2011 · 173 citations · Full text