Cargando…

D-α-Tocopherol-Based Micelles for Successful Encapsulation of Retinoic Acid

All-trans-retinoic acid (ATRA) represents the first-choice treatment for several skin diseases, including epithelial skin cancer and acne. However, ATRA’s cutaneous side effects, like redness and peeling, and its high instability limit its efficacy. To address these drawbacks and to improve ATRA sol...

Descripción completa

Detalles Bibliográficos
Autores principales: Zuccari, Guendalina, Baldassari, Sara, Alfei, Silvana, Marengo, Barbara, Valenti, Giulia Elda, Domenicotti, Cinzia, Ailuno, Giorgia, Villa, Carla, Marchitto, Leonardo, Caviglioli, Gabriele
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7999664/
https://www.ncbi.nlm.nih.gov/pubmed/33806321
http://dx.doi.org/10.3390/ph14030212
_version_ 1783670833506418688
author Zuccari, Guendalina
Baldassari, Sara
Alfei, Silvana
Marengo, Barbara
Valenti, Giulia Elda
Domenicotti, Cinzia
Ailuno, Giorgia
Villa, Carla
Marchitto, Leonardo
Caviglioli, Gabriele
author_facet Zuccari, Guendalina
Baldassari, Sara
Alfei, Silvana
Marengo, Barbara
Valenti, Giulia Elda
Domenicotti, Cinzia
Ailuno, Giorgia
Villa, Carla
Marchitto, Leonardo
Caviglioli, Gabriele
author_sort Zuccari, Guendalina
collection PubMed
description All-trans-retinoic acid (ATRA) represents the first-choice treatment for several skin diseases, including epithelial skin cancer and acne. However, ATRA’s cutaneous side effects, like redness and peeling, and its high instability limit its efficacy. To address these drawbacks and to improve ATRA solubilization, we prepared ATRA-loaded micelles (ATRA-TPGSs), by its encapsulation in D-α-tocopheryl-polyethylene-glycol-succinate (TPGS). First, to explore the feasibility of the project, a solubility study based on the equilibrium method was performed; then, six ATRA-TPGS formulations were prepared by the solvent-casting method using different TPGS amounts. ATRA-TPGSs showed small sizes (11–20 nm), low polydispersity, slightly negative zeta potential, and proved good encapsulation efficiency, confirmed by a chemometric-assisted Fourier transform infrared spectroscopy (FTIR) investigation. ATRA-TPGS stability was also investigated to choose the most stable formulation. Using Carbopol(®) 980 as gelling agent, ATRA-TPGS-loaded gels were obtained and analyzed for their rheological profiles. Ex vivo release studies from ATRA-TPGSs were performed by Franz cells, demonstrating a permeation after 24 h of 22 ± 4 µ cm(−2). ATRA-TPGSs showed enhanced cytotoxic effects on melanoma cells, suggesting that these formulations may represent a valid alternative to improve patient compliance and to achieve more efficacious therapeutic outcomes.
format Online
Article
Text
id pubmed-7999664
institution National Center for Biotechnology Information
language English
publishDate 2021
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-79996642021-03-28 D-α-Tocopherol-Based Micelles for Successful Encapsulation of Retinoic Acid Zuccari, Guendalina Baldassari, Sara Alfei, Silvana Marengo, Barbara Valenti, Giulia Elda Domenicotti, Cinzia Ailuno, Giorgia Villa, Carla Marchitto, Leonardo Caviglioli, Gabriele Pharmaceuticals (Basel) Article All-trans-retinoic acid (ATRA) represents the first-choice treatment for several skin diseases, including epithelial skin cancer and acne. However, ATRA’s cutaneous side effects, like redness and peeling, and its high instability limit its efficacy. To address these drawbacks and to improve ATRA solubilization, we prepared ATRA-loaded micelles (ATRA-TPGSs), by its encapsulation in D-α-tocopheryl-polyethylene-glycol-succinate (TPGS). First, to explore the feasibility of the project, a solubility study based on the equilibrium method was performed; then, six ATRA-TPGS formulations were prepared by the solvent-casting method using different TPGS amounts. ATRA-TPGSs showed small sizes (11–20 nm), low polydispersity, slightly negative zeta potential, and proved good encapsulation efficiency, confirmed by a chemometric-assisted Fourier transform infrared spectroscopy (FTIR) investigation. ATRA-TPGS stability was also investigated to choose the most stable formulation. Using Carbopol(®) 980 as gelling agent, ATRA-TPGS-loaded gels were obtained and analyzed for their rheological profiles. Ex vivo release studies from ATRA-TPGSs were performed by Franz cells, demonstrating a permeation after 24 h of 22 ± 4 µ cm(−2). ATRA-TPGSs showed enhanced cytotoxic effects on melanoma cells, suggesting that these formulations may represent a valid alternative to improve patient compliance and to achieve more efficacious therapeutic outcomes. MDPI 2021-03-04 /pmc/articles/PMC7999664/ /pubmed/33806321 http://dx.doi.org/10.3390/ph14030212 Text en © 2021 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 (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ).
spellingShingle Article
Zuccari, Guendalina
Baldassari, Sara
Alfei, Silvana
Marengo, Barbara
Valenti, Giulia Elda
Domenicotti, Cinzia
Ailuno, Giorgia
Villa, Carla
Marchitto, Leonardo
Caviglioli, Gabriele
D-α-Tocopherol-Based Micelles for Successful Encapsulation of Retinoic Acid
title D-α-Tocopherol-Based Micelles for Successful Encapsulation of Retinoic Acid
title_full D-α-Tocopherol-Based Micelles for Successful Encapsulation of Retinoic Acid
title_fullStr D-α-Tocopherol-Based Micelles for Successful Encapsulation of Retinoic Acid
title_full_unstemmed D-α-Tocopherol-Based Micelles for Successful Encapsulation of Retinoic Acid
title_short D-α-Tocopherol-Based Micelles for Successful Encapsulation of Retinoic Acid
title_sort d-α-tocopherol-based micelles for successful encapsulation of retinoic acid
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7999664/
https://www.ncbi.nlm.nih.gov/pubmed/33806321
http://dx.doi.org/10.3390/ph14030212
work_keys_str_mv AT zuccariguendalina datocopherolbasedmicellesforsuccessfulencapsulationofretinoicacid
AT baldassarisara datocopherolbasedmicellesforsuccessfulencapsulationofretinoicacid
AT alfeisilvana datocopherolbasedmicellesforsuccessfulencapsulationofretinoicacid
AT marengobarbara datocopherolbasedmicellesforsuccessfulencapsulationofretinoicacid
AT valentigiuliaelda datocopherolbasedmicellesforsuccessfulencapsulationofretinoicacid
AT domenicotticinzia datocopherolbasedmicellesforsuccessfulencapsulationofretinoicacid
AT ailunogiorgia datocopherolbasedmicellesforsuccessfulencapsulationofretinoicacid
AT villacarla datocopherolbasedmicellesforsuccessfulencapsulationofretinoicacid
AT marchittoleonardo datocopherolbasedmicellesforsuccessfulencapsulationofretinoicacid
AT caviglioligabriele datocopherolbasedmicellesforsuccessfulencapsulationofretinoicacid