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Ex vivo rabbit cornea diffusion studies with a soluble insert of moxifloxacin

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Abstract

The objective of this research was to develop and evaluate an ocular insert for the controlled drug delivery of moxifloxacin which could perhaps be used in the treatment of corneal keratitis or even bacterial endophthalmitis. We have evaluated the ex vivo ocular diffusion of moxifloxacin through rabbit cornea, both fresh and preserved under different conditions. Histological studies were also carried out. Subsequently, drug matrix inserts were prepared using bioadhesive polymers. The inserts were evaluated for their physicochemical parameters. Ophthalmic ex vivo permeation of moxifloxacin was carried out with the most promising insert. The formulate insert was thin and provided higher ocular diffusion than commercial formulations. Ocular diffusion studies revealed significant differences between fresh and frozen corneas. Histological examinations also showed differences in the thickness of stroma between fresh and frozen corneas. The ophthalmic insert we have developed allows a larger quantity of moxifloxacin to permeate through the cornea than existing commercial formulations of the drug. Ocular delivery of moxifloxacin with this insert could be a new approach for the treatment of eye diseases.

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Abbreviations

HPMC:

Hydroxypropyl methylcellulose 4500

MOX:

Moxifloxacin

PBS:

Phosphate buffered solution

PEG:

Polyethylene glycol

PVP-K30:

Polyvinylpyrrolidone K30

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Authors and Affiliations

  1. Instituto de Ciencias Biomédicas, Departamento de Farmacia, Facultad de Ciencias de la Salud, Universidad Cardenal Herrera-CEU, CEU Universities, C/Santiago Ramón y Cajal, s/n., 46115, Alfara del Patriarca, Valencia, Spain

    María Sebastián-Morelló, María Aracely Calatayud-Pascual, Vicent Rodilla, Cristina Balaguer-Fernández & Alicia López-Castellano

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  1. María Sebastián-Morelló
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  2. María Aracely Calatayud-Pascual
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  3. Vicent Rodilla
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  4. Cristina Balaguer-Fernández
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  5. Alicia López-Castellano
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Correspondence to Alicia López-Castellano.

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Sebastián-Morelló, M., Calatayud-Pascual, M.A., Rodilla, V. et al. Ex vivo rabbit cornea diffusion studies with a soluble insert of moxifloxacin. Drug Deliv. and Transl. Res. 8, 132–139 (2018). https://doi.org/10.1007/s13346-017-0443-y

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