Nanosuspension: A New Vehicle For The Improvement Of The Delivery Of Drug To The Ocular Surface And Application To Fungal Infection In The Eye

Present limitations in the management of ophthalmic fungal infections include the inability to provide long-term extraocular drug delivery without compromising intraocular structures and/or systemic drug exposure.Nanosuspension as a new vehicle for the improvement of the delivery of drugs to the ocular mucosa and an ophthalmic penetration enhaner(Pharmasolve)and its impact on the permeability were investigated.Nanosuspension offers various advantages over conventional ocular dosage forms,including longer residence time on the corneal surface,higher drug concentrations in the infected tissue and reduction in systemic toxicity of drug.(1)Voriconazole was chosen as a model compound due to its potential usefulness.A solvent displacement technique was used to produce voriconazole–loaded nanosuspension.Characterizations of nanosuspension were evaluated.The nanosuspension had a mean size range of 138 nm and a zeta potential of +22.5 m V.Even after 6 months of stability study,results were unchanged,indicating the good potential for ocular application.(2)The oeular irritantion of a new ophthalmic penetration enhaner,pharnlasolve,and its impact on the permeability through the isolated cornea of voriconazole and its carriers were studied.The results showed that the nanosuspension as the carrier of active substance could significantly increase membrane permeability of the active substance.The liposoluble fluorescent probe was enriched and penetrated through the cornea to the eye,and has a significant penetration promoting effect.(3)The effect of different concentration of voriconazole nanosuspension on the growth of fungi was evaluated by the paper diffusion method.The results showed that nanosuspension as a carrier of voriconazole did not affect the antifungal activity of voriconazole,and it could increase the antifungal activity at lower concentration.