• Maria Aurora Grimaudo, Giovanni Amato, Claudia Carbone, Patricia Diaz-Rodriguez, Teresa Musumeci, Angel Concheiro, Carmen Alvarez-Lorenzo, and Giovanni Puglisi.
• Laboratory of Drug Delivery Technology, Department of Drug Sciences, University of Catania, Catania, Italy; Departamento de Farmacología, Farmacia y Tecnología Farmacéutica, I+D Farma (GI-1645), Facultad de Farmacia and Health Research Institute of Santiago de Compostela (IDIS), Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain. Electronic address: Maria.Aurora.Grimaudo@sergas.es.
• Int J Pharm. 2020 Feb 25; 576: 118986.

AbstractCorneal wound healing after a trauma or a chemical injury has been shown to correlate with antioxidant levels at the ocular surface. However, ocular bioavailability of efficient antioxidants (e.g. ferulic acid) after topical administration is limited by their poor solubility, low stability and short residence time. The aim of this work was to formulate ferulic acid in a nanocomposite platform composed of nanogels and micelles for efficient delivery to cornea. Solubility enhancement factor of ferulic acid was found to be equal to 1.9 ± 0.3 and 3.4 ± 0.3 for 50 and 100 mg/ml Pluronic® F68 micellar solutions. Hyaluronan was added to blank and ferulic acid loaded micelles, and then cross-linked with ε-polylysine. Hyaluronan nanogels showed dimensions of ~300 nm with positive zeta potential values. The formulations were characterized in terms of rheological behavior, biocompatibility, wound healing properties, ferulic acid release pattern and penetration into excised bovine corneas. In comparison to Pluronic® micelles that released ferulic acid rapidly, micelle-nanogel composites sustained the release up to 2 days. Furthermore, the micelle-nanogel formulation favored in vitro wound closure promoting fibroblasts growth and ex vivo accumulation of ferulic acid into both healthy and damaged corneas (>100 µg/cm2).Copyright © 2019 Elsevier B.V. All rights reserved.

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