Novel nanostructured lipid carriers loading Apigenin for anterior segment ocular pathologies
Author
Bonilla-Vidal, L.
Espina, M.
García, M.L.
Baldomà, L.
Badia, J.
González, J.A.
Delgado, L.M.
Gliszczyńska, A.
Souto, E.B.
Sánchez-López, E.
Publication date
2024ISSN
0378-5173
Abstract
Dry eye disease (DED) is a chronic multifactorial disorder of the ocular surface caused by tear film dysfunction and constitutes one of the most common ocular conditions worldwide. However, its treatment remains unsatisfactory. While artificial tears are commonly used to moisturize the ocular surface, they do not address the underlying causes of DED. Apigenin (APG) is a natural product with anti-inflammatory properties, but its low solubility and bioavailability limit its efficacy. Therefore, a novel formulation of APG loaded into biodegradable and biocompatible nanoparticles (APG-NLC) was developed to overcome the restricted APG stability, improve its therapeutic efficacy, and prolong its retention time on the ocular surface by extending its release. APG-NLC optimization, characterization, biopharmaceutical properties and therapeutic efficacy were evaluated. The optimized APG-NLC exhibited an average particle size below 200 nm, a positive surface charge, and an encapsulation efficiency over 99 %. APG-NLC exhibited sustained release of APG, and stability studies demonstrated that the formulation retained its integrity for over 25 months. In vitro and in vivo ocular tolerance studies indicated that APG-NLC did not cause any irritation, rendering them suitable for ocular topical administration. Furthermore, APG-NLC showed non-toxicity in an epithelial corneal cell line and exhibited fast cell internalization. Therapeutic benefits were demonstrated using an in vivo model of DED, where APG-NLC effectively reversed DED by reducing ocular surface cellular damage and increasing tear volume. Anti-inflammatory assays in vivo also showcased its potential to treat and prevent ocular inflammation, particularly relevant in DED patients. Hence, APG-NLC represent a promising system for the treatment and prevention of DED and its associated inflammation.
Document Type
Article
Document version
Published version
Language
English
Subject (CDU)
61 - Medical sciences
Keywords
Apigenina
Portadors de lípids nanoestructurats
Oli de rosa mosqueta
Nanopartícules lipídiques
Apigenina
Portadores de lípidos nanoestructurados
Aceite de rosa mosqueta
Nanopartículas lipídicas
Apigenin
Nanostructured lipid carriers
Rosehip oil
Lipid nanoparticles
Pages
14
Publisher
Elsevier
Collection
658
Is part of
International Journal of Pharmaceutics
Citation
Bonilla-Vidal, L.; Espina, M.; García, M.L. [et al.]. Novel nanostructured lipid carriers loading Apigenin for anterior segment ocular pathologies. International Journal of Pharmaceutics, 2024, 658, 124222. Disponible en: <https://www.sciencedirect.com/science/article/pii/S0378517324004563?via%3Dihub>. Fecha de acceso: 10 jun. 2024. DOI: 10.1016/j.ijpharm.2024.124222
This item appears in the following Collection(s)
- Ciències de la Salut [745]
Rights
Under a Creative Commons license
Except where otherwise noted, this item's license is described as https://creativecommons.org/licenses/by-nc-nd/4.0/