Transcorneal Permeation in a Corneal Device of Non-Steroidal Anti-Inflammatory Drugs in Drug Delivery Systems

摘要

This work is focused on the ex vivo study of corneal permeation of two anti-inflammatory drugs: diclofenac, and flurbiprofen (as a model of hydrophilic and lipophilic drug, respectively) loaded to cyclodextrins or polymeric nanoparticles in order to determine differences in their corneal permeation against free drug or commercial eye drops. These studies were carried out in a corneal device designed and developed in our laboratory. In this work the habitual conditions for the permeation studies were modified to reproduce the behaviour when eye drops were administered. For this reason a new tetracompartmental pharmacokinetic model was developed. The complex formation of diclofenac with cyclodextrins and the flurbiprofen loaded to polymeric nanoparticles has been shown as effective procedures to remarkably increase the bioavailability of the anti-inflammatory drugs. The efficiency of polymeric nanoparticles of Poly (D-L lactic-coglycolyc) acid and poly-ε-caprolacton as intraocular targeting of NSAIDs has also been proved, being the latter polymer more effective to increase the flurbiprofen corneal permeation. The apparent corneal permeability coefficient of samples has been calculated getting a low permeation values for free drugs.