Lorenzo Veiga, BlancaDíaz Rodríguez, PatriciaÁlvarez Lorenzo, CarmenLoftsson, ThorsteinnSigurdsson, Hakon Hrafn2020-11-102020-11-102020Lorenzo-Veiga, B.; Diaz-Rodriguez, P.; Alvarez-Lorenzo, C.; Loftsson, T.; Sigurdsson, H.H. In Vitro and Ex Vivo Evaluation of Nepafenac-Based Cyclodextrin Microparticles for Treatment of Eye Inflammation. Nanomaterials 2020, 10, 709http://hdl.handle.net/10347/23634The aim of this study was to design and evaluate novel cyclodextrin (CD)-based aggregate formulations to efficiently deliver nepafenac topically to the eye structure, to treat inflammation and increase nepafenac levels in the posterior segment, thus attenuating the response of inflammatory mediators. The physicochemical properties of nine aggregate formulations containing nepafenac/γ-CD/hydroxypropyl-β (HPβ)-CD complexes as well as their rheological properties, mucoadhesion, ocular irritancy, corneal and scleral permeability, and anti-inflammatory activity were investigated in detail. The results were compared with a commercially available nepafenac suspension, Nevanac® 3 mg/mL. All formulations showed microparticles, neutral pH, and negative zeta potential (–6 to –27 mV). They were non-irritating and nontoxic and showed high permeation through bovine sclera. Formulations containing carboxymethyl cellulose (CMC) showed greater anti-inflammatory activity, even higher than the commercial formulation, Nevanac® 0.3%. The optimized formulations represent an opportunity for topical instillation of drugs to the posterior segment of the eyeeng© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/)Atribución 4.0 Internacionalhttp://creativecommons.org/licenses/by/4.0/Eye dropCyclodextrinNepafenacHET-CAMEx vivo permeation studiesOcular inflammationjournal article10.3390/nano100407092079-4991open access