Journal
COLLOIDS AND SURFACES B-BIOINTERFACES
Volume 145, Issue -, Pages 241-250Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.colsurfb.2016.04.054
Keywords
Nanospheres; Dexibuprofen; PLGA; PEG; Inflammation; Drug delivery
Funding
- Spanish Ministry of Science and Innovation [MAT 2014-59134-R]
- Spanish Ministry for the PhD scholarship FPI-MICINN [BES-2012-056083]
- FCT Portuguese Foundation for Science and Technology [UID/AGR/04033/2013]
- FCT/MEC [UID/QUI/50006/2013]
- FEDER [PT2020]
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Dexibuprofen-loaded PEGylated PLGA nanospheres have been developed to improve the biopharmaceutical profile of the anti-inflammatory drug for ocular administration. Dexibuprofen is the active enantiomer of ibuprofen and therefore lower doses may be applied to achieve the same therapeutic level. According to this, two batches of nanospheres of different drug concentrations, 0.5 and 1.0 mg/m1 respectively, have been developed (the latter corresponding to the therapeutic ibuprofen concentration for inflammatory eye diseases). Both batches were composed of negatively charged nanospheres (-14.1 and -15.9 mV), with a mean particle size below 200nm, and a high encapsulation efficiency (99%). X-ray, FTIR, and DSC analyses confirmed that the drug was dispersed inside the matrix of the nanospheres. While the in vitro release profile was sustained up to 12 h, the ex vivo corneal and scleral permeation profile demonstrated higher drug retention and permeation in the corneal tissue rather than in the sclera. These results were also confirmed by the quantification of dexibuprofen in ocular tissues after the in vivo administration of drug-loaded nanospheres. Cell viability studies confirmed that PEGylated-PLGA nanospheres were less cytotoxic than free dexibuprofen in the majority of the tested concentrations. Ocular in vitro (HET-CAM test) and in vivo (Draize test) tolerance assays demonstrated the non-irritant character of both nanosphere batches. In vivo anti-inflammatory effects were evaluated in albino rabbits before and after inflammation induction. Both batches confirmed to be effective to treat and prevent ocular inflammation. (C) 2016 Elsevier B.V. All rights reserved.
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