In Vitro and Ex Vivo Evaluation of Nepafenac-Based Cyclodextrin Microparticles for Treatment of Eye Inflammation
by
Blanca Lorenzo-Veiga 1
, Patricia Diaz-Rodriguez 2,3, Carmen Alvarez-Lorenzo 3, Thorsteinn Loftsson 1 and Hakon Hrafn Sigurdsson 1,*
Blanca Lorenzo-Veiga 1, Patricia Diaz-Rodriguez 2,3, Carmen Alvarez-Lorenzo 3, Thorsteinn Loftsson 1 and Hakon Hrafn Sigurdsson 1,*
1
Faculty of Pharmaceutical Sciences, University of Iceland, Hofsvallagata 53, IS-107 Reykjavik, Iceland
2
Departamento de Ingeniería Química y Tecnología Farmacéutica, Facultad de Ciencias de la Salud, Universidad de la Laguna (ULL), Campus de Anchieta, 38200 La Laguna (Tenerife), Spain
3
Departamento de Farmacología, Farmacia y Tecnología Farmacéutica, R+D Pharma Group (GI-1645), Facultad de Farmacia and Health Research Institute of Santiago de Compostela (IDIS), Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain
*
Author to whom correspondence should be addressed.
Nanomaterials 2020, 10(4), 709; https://doi.org/10.3390/nano10040709
Received: 6 March 2020 / Revised: 2 April 2020 / Accepted: 7 April 2020 / Published: 9 April 2020
(This article belongs to the Special Issue Nanoconstructs Based on Cyclodextrins)
The 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 eye.
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Keywords:
eye drop; cyclodextrin; nepafenac; HET-CAM; ex vivo permeation studies; ocular inflammation
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited
MDPI and ACS Style
Lorenzo-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, 709.
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