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Development of Triamcinolone Acetonide Nanocrystals for Ocular Administration

Triamcinolone acetonide (TA) is a powerful anti-inflammatory drug used in the treatment of inflammatory ocular disorders; however, its poor aqueous solubility and ocular anatomical barriers hinder optimal treatment. The aim of this work was to obtain triamcinolone acetonide nanocrystals (TA-NC) to i...

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Autores principales: Formica, María Lina, Awde Alfonso, Hamoudi Ghassan, Paredes, Alejandro Javier, Melian, María Elisa, Camacho, Nahuel Matías, Faccio, Ricardo, Tártara, Luis Ignacio, Palma, Santiago Daniel
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9962019/
https://www.ncbi.nlm.nih.gov/pubmed/36840006
http://dx.doi.org/10.3390/pharmaceutics15020683
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author Formica, María Lina
Awde Alfonso, Hamoudi Ghassan
Paredes, Alejandro Javier
Melian, María Elisa
Camacho, Nahuel Matías
Faccio, Ricardo
Tártara, Luis Ignacio
Palma, Santiago Daniel
author_facet Formica, María Lina
Awde Alfonso, Hamoudi Ghassan
Paredes, Alejandro Javier
Melian, María Elisa
Camacho, Nahuel Matías
Faccio, Ricardo
Tártara, Luis Ignacio
Palma, Santiago Daniel
author_sort Formica, María Lina
collection PubMed
description Triamcinolone acetonide (TA) is a powerful anti-inflammatory drug used in the treatment of inflammatory ocular disorders; however, its poor aqueous solubility and ocular anatomical barriers hinder optimal treatment. The aim of this work was to obtain triamcinolone acetonide nanocrystals (TA-NC) to improve ocular corticosteroid therapy. Self-dispersible TA-NC were prepared by the bead milling technique followed by spray-drying, exhaustively characterized and then evaluated in vivo in an ocular model of endotoxin-induced uveitis (EIU). Self-dispersible TA-NC presented an average particle size of 257 ± 30 nm, a narrow size distribution and a zeta potential of −25 ± 3 mV, which remained unchanged for 120 days under storage conditions at 25 °C. In addition, SEM studies of the TA-NC showed uniform and spherical morphology, and FTIR and XRDP analyses indicated no apparent chemical and crystallinity changes. The subconjunctival administration of TA-NC in albino male white rabbits showed no clinical signs of ocular damage. In vivo studies proved that treatment with self-dispersible TA-NC alleviated the inflammatory response in the anterior chamber and iris in EUI rabbit eyes. Dispersible TA-NC are a promising approach to obtaining a novel nanometric TA formulation for ocular disorders.
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spelling pubmed-99620192023-02-26 Development of Triamcinolone Acetonide Nanocrystals for Ocular Administration Formica, María Lina Awde Alfonso, Hamoudi Ghassan Paredes, Alejandro Javier Melian, María Elisa Camacho, Nahuel Matías Faccio, Ricardo Tártara, Luis Ignacio Palma, Santiago Daniel Pharmaceutics Article Triamcinolone acetonide (TA) is a powerful anti-inflammatory drug used in the treatment of inflammatory ocular disorders; however, its poor aqueous solubility and ocular anatomical barriers hinder optimal treatment. The aim of this work was to obtain triamcinolone acetonide nanocrystals (TA-NC) to improve ocular corticosteroid therapy. Self-dispersible TA-NC were prepared by the bead milling technique followed by spray-drying, exhaustively characterized and then evaluated in vivo in an ocular model of endotoxin-induced uveitis (EIU). Self-dispersible TA-NC presented an average particle size of 257 ± 30 nm, a narrow size distribution and a zeta potential of −25 ± 3 mV, which remained unchanged for 120 days under storage conditions at 25 °C. In addition, SEM studies of the TA-NC showed uniform and spherical morphology, and FTIR and XRDP analyses indicated no apparent chemical and crystallinity changes. The subconjunctival administration of TA-NC in albino male white rabbits showed no clinical signs of ocular damage. In vivo studies proved that treatment with self-dispersible TA-NC alleviated the inflammatory response in the anterior chamber and iris in EUI rabbit eyes. Dispersible TA-NC are a promising approach to obtaining a novel nanometric TA formulation for ocular disorders. MDPI 2023-02-17 /pmc/articles/PMC9962019/ /pubmed/36840006 http://dx.doi.org/10.3390/pharmaceutics15020683 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Formica, María Lina
Awde Alfonso, Hamoudi Ghassan
Paredes, Alejandro Javier
Melian, María Elisa
Camacho, Nahuel Matías
Faccio, Ricardo
Tártara, Luis Ignacio
Palma, Santiago Daniel
Development of Triamcinolone Acetonide Nanocrystals for Ocular Administration
title Development of Triamcinolone Acetonide Nanocrystals for Ocular Administration
title_full Development of Triamcinolone Acetonide Nanocrystals for Ocular Administration
title_fullStr Development of Triamcinolone Acetonide Nanocrystals for Ocular Administration
title_full_unstemmed Development of Triamcinolone Acetonide Nanocrystals for Ocular Administration
title_short Development of Triamcinolone Acetonide Nanocrystals for Ocular Administration
title_sort development of triamcinolone acetonide nanocrystals for ocular administration
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9962019/
https://www.ncbi.nlm.nih.gov/pubmed/36840006
http://dx.doi.org/10.3390/pharmaceutics15020683
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