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Hyaluronic Acid-Based Micelles as Ocular Platform to Modulate the Loading, Release, and Corneal Permeation of Corticosteroids.
Macromol Biosci. 2017 12; 17(12)MB

Abstract

The aim of this work is to prepare hyaluronic acid-based micelles as a platform to load corticosteroid drugs and to improve their corneal permeation after administration on the ocular surface. Three amphiphilic derivatives of hyaluronic acid (HA) are synthesized using different amounts of hexadecylamine (C16 -NH2). HAC16 a, HAC16 b, and HAC16 c derivatives are able to form micelles by the cosolvent evaporation method and to entrap corticosteroids (dexamethasone, triamcinolone, triamcinolone acetonide). HAC16 a and HAC16 b micelles show the best results in terms of drug loading and particle size. They are also able to improve drug release compared to free drug solution or suspension. In addition, HAC16 b micelles show an optimal mucoadhesion and compatibility with human corneal epithelial cells. In vitro and ex vivo permeation studies of drug-loaded HAC16 b micelles are performed to understand the ability of these micelles to act as penetration and/or permeation enhancers.

Authors+Show Affiliations

Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123, Palermo, Italy.Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123, Palermo, Italy.Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123, Palermo, Italy.Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123, Palermo, Italy. Mediterranean Center of Human Health Advanced Biotechnologies (CHAB), AteN Center, Viale delle Scienze, Edificio 18, 90128, Palermo, Italy.Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123, Palermo, Italy.Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123, Palermo, Italy. Mediterranean Center of Human Health Advanced Biotechnologies (CHAB), AteN Center, Viale delle Scienze, Edificio 18, 90128, Palermo, Italy.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

29144603

Citation

Bongiovì, Flavia, et al. "Hyaluronic Acid-Based Micelles as Ocular Platform to Modulate the Loading, Release, and Corneal Permeation of Corticosteroids." Macromolecular Bioscience, vol. 17, no. 12, 2017.
Bongiovì F, Di Prima G, Palumbo FS, et al. Hyaluronic Acid-Based Micelles as Ocular Platform to Modulate the Loading, Release, and Corneal Permeation of Corticosteroids. Macromol Biosci. 2017;17(12).
Bongiovì, F., Di Prima, G., Palumbo, F. S., Licciardi, M., Pitarresi, G., & Giammona, G. (2017). Hyaluronic Acid-Based Micelles as Ocular Platform to Modulate the Loading, Release, and Corneal Permeation of Corticosteroids. Macromolecular Bioscience, 17(12). https://doi.org/10.1002/mabi.201700261
Bongiovì F, et al. Hyaluronic Acid-Based Micelles as Ocular Platform to Modulate the Loading, Release, and Corneal Permeation of Corticosteroids. Macromol Biosci. 2017;17(12) PubMed PMID: 29144603.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Hyaluronic Acid-Based Micelles as Ocular Platform to Modulate the Loading, Release, and Corneal Permeation of Corticosteroids. AU - Bongiovì,Flavia, AU - Di Prima,Giulia, AU - Palumbo,Fabio S, AU - Licciardi,Mariano, AU - Pitarresi,Giovanna, AU - Giammona,Gaetano, Y1 - 2017/11/16/ PY - 2017/07/26/received PY - 2017/10/10/revised PY - 2017/11/17/pubmed PY - 2018/7/27/medline PY - 2017/11/17/entrez KW - corticosteroids KW - hyaluronic acid KW - ocular administration KW - polymeric micelles KW - transcorneal enhancers JF - Macromolecular bioscience JO - Macromol Biosci VL - 17 IS - 12 N2 - The aim of this work is to prepare hyaluronic acid-based micelles as a platform to load corticosteroid drugs and to improve their corneal permeation after administration on the ocular surface. Three amphiphilic derivatives of hyaluronic acid (HA) are synthesized using different amounts of hexadecylamine (C16 -NH2). HAC16 a, HAC16 b, and HAC16 c derivatives are able to form micelles by the cosolvent evaporation method and to entrap corticosteroids (dexamethasone, triamcinolone, triamcinolone acetonide). HAC16 a and HAC16 b micelles show the best results in terms of drug loading and particle size. They are also able to improve drug release compared to free drug solution or suspension. In addition, HAC16 b micelles show an optimal mucoadhesion and compatibility with human corneal epithelial cells. In vitro and ex vivo permeation studies of drug-loaded HAC16 b micelles are performed to understand the ability of these micelles to act as penetration and/or permeation enhancers. SN - 1616-5195 UR - https://www.unboundmedicine.com/medline/citation/29144603/Hyaluronic_Acid_Based_Micelles_as_Ocular_Platform_to_Modulate_the_Loading_Release_and_Corneal_Permeation_of_Corticosteroids_ L2 - https://doi.org/10.1002/mabi.201700261 DB - PRIME DP - Unbound Medicine ER -