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    Mucoadhesive Nanoparticles as Carrier Systems for Prolonged Ocular Delivery of Gatifloxacin/Prednisolone Bitherapy
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    Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Eini Street, Cairo 11562, Egypt, and Department of Pharmaceutics, Faculty of Pharmacy, Helwan University, Ain Helwan, Helwan, Cairo 11795, Egypt
    * Corresponding author. Mailing address: Cairo University, Faculty of Pharmacy, Department of Pharmaceutics and Industrial Pharmacy, Kasr El-Eini Street, Cairo 11562, Egypt. Tel: (+2) 0111344459. Fax: (+2) 27001060. E-mail: [email protected]
    †Cairo University.
    ‡Helwan University.
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    Molecular Pharmaceutics

    Cite this: Mol. Pharmaceutics 2010, 7, 2, 576–585
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    https://doi.org/10.1021/mp900279c
    Published February 17, 2010
    Copyright © 2010 American Chemical Society
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    A fluoroquinolone/glucocorticoid combination for the treatment of bacterial keratitis in the form of mucoadhesive nanoparticle suspensions was developed to prolong the release and improve patient compliance. Gatifloxacin/prednisolone loaded nanoparticles were prepared using Eudragit RS 100 and RL 100 and coated with the bioadhesive polymer, hyaluronic acid. FT-IR and DSC studies revealed no interaction between gatifloxacin and prednisolone. The effects of the drug:polymer ratio (D:P) and the RS/RL ratio were studied. The obtained nanoparticles were distinct and spherical with a solid dense structure. They have average particle size range of 315.2 to 973.65 nm. Increasing the D:P ratio significantly lowered the entrapment efficiency for both drugs (p < 0.05). The nanoparticle suspensions revealed significantly prolonged drug release comparing to the free drugs (p < 0.05) with no burst effect. Increasing the polymer concentration and the Eudragit RS ratio significantly decreased the release efficiency values. Gatifloxacin showed anomalous release (n = 0.4943) from 1:1 D:P ratio nanoparticle suspension and Fickian diffusion mechanism (n < 0.45) from formulas prepared at higher D:P ratios. Gatifloxacin showed better bioavailability and sustained action in aqueous humor and corneal tissue from the nanoparticles compared to the commercial eye drops. The resulting nanoparticle suspension is promising in reducing dose frequency and improving patient compliance.

    Copyright © 2010 American Chemical Society

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    Cite this: Mol. Pharmaceutics 2010, 7, 2, 576–585
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    https://doi.org/10.1021/mp900279c
    Published February 17, 2010
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