Combination of Apigenin and Melatonin with nanostructured lipid carriers as anti-inflammatory ocular treatment

Lorena Bonilla-Vidal; Marta Espina; María Luisa García; Laura Baldomà; Josefa Badia; Anna Gliszczyńska; Eliana B Souto; Elena Sánchez-López

doi:10.1016/j.ijpharm.2024.125160

Combination of Apigenin and Melatonin with nanostructured lipid carriers as anti-inflammatory ocular treatment

Int J Pharm. 2024 Dec 31:125160. doi: 10.1016/j.ijpharm.2024.125160. Online ahead of print.

Authors

Lorena Bonilla-Vidal¹, Marta Espina¹, María Luisa García¹, Laura Baldomà², Josefa Badia², Anna Gliszczyńska³, Eliana B Souto⁴, Elena Sánchez-López⁵

Affiliations

¹ Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, University of Barcelona, 08028 Barcelona, Spain; Institute of Nanoscience and Nanotechnology (IN(2)UB), University of Barcelona, 08028 Barcelona, Spain.
² Department of Biochemistry and Physiology, University of Barcelona, 08028 Barcelona, Spain; Institute of Biomedicine of the University of Barcelona (IBUB), Institute of Research of Sant Joan de Déu (IRSJD), 08950 Barcelona, Spain.
³ Department of Food Chemistry and Biocatalysis, Wrocław University of Environmental and Life Sciences, Norwida 25, 50-375 Wrocław, Poland.
⁴ UCD School of Chemical and Bioprocess Engineering, University College Dublin, Belfield D04 V1W8, Ireland.
⁵ Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, University of Barcelona, 08028 Barcelona, Spain; Institute of Nanoscience and Nanotechnology (IN(2)UB), University of Barcelona, 08028 Barcelona, Spain. Electronic address: esanchezlopez@ub.edu.

PMID: 39746583
DOI: 10.1016/j.ijpharm.2024.125160

Abstract

Ocular inflammation is a complex pathology with limited treatment options. While traditional therapies have side effects, novel approaches, such as natural compounds like Apigenin (APG) and Melatonin (MEL) offer promising solutions. APG and MEL, in combination with nanostructured lipid carriers (NLC), may provide a synergistic effect in treating ocular inflammation, potentially improving patient outcomes and reducing adverse effects. NLC could provide chemical protection of these compounds, while offering a sustained release into the ocular surface. Optimized NLC exhibited suitable physicochemical parameters, physical stability, sustained release of APG and MEL, and were biocompatible in vitro in a corneal cell line, and in ovo by using hen's egg chorioallantoic membrane test. In vitro and in vivo studies confirmed the NLCs' ability to attenuate inflammation by reducing interleukin-6 (IL-6), IL-8 and monocyte chemoattractant protein 1 (MCP-1) cytokine levels and decreasing inflammation in a rabbit model. These findings suggest that the co-encapsulation of APG and MEL into NLC could represent a promising strategy for managing ocular inflammatory conditions.

Keywords: Apigenin; Dual delivery system; Lipid nanoparticles; Melatonin; Nanostructured lipid carriers; Ocular inflammation.