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Mixed Polymeric Micelles for Rapamycin Skin Delivery
Facial angiofibromas (FA) are one of the most obvious cutaneous manifestations of tuberous sclerosis complex. Topical rapamycin for angiofibromas has been reported as a promising treatment. Several types of vehicles have been used hitherto, but polymeric micelles and especially those made of d-α-toc...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8948846/ https://www.ncbi.nlm.nih.gov/pubmed/35335945 http://dx.doi.org/10.3390/pharmaceutics14030569 |
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author | Le Guyader, Guillaume Do, Bernard Rietveld, Ivo B. Coric, Pascale Bouaziz, Serge Guigner, Jean-Michel Secretan, Philippe-Henri Andrieux, Karine Paul, Muriel |
author_facet | Le Guyader, Guillaume Do, Bernard Rietveld, Ivo B. Coric, Pascale Bouaziz, Serge Guigner, Jean-Michel Secretan, Philippe-Henri Andrieux, Karine Paul, Muriel |
author_sort | Le Guyader, Guillaume |
collection | PubMed |
description | Facial angiofibromas (FA) are one of the most obvious cutaneous manifestations of tuberous sclerosis complex. Topical rapamycin for angiofibromas has been reported as a promising treatment. Several types of vehicles have been used hitherto, but polymeric micelles and especially those made of d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) seem to have shown better skin bioavailability of rapamycin than the so far commonly used ointments. To better understand the influence of polymeric micelles on the behavior of rapamycin, we explored it through mixed polymeric micelles combining TPGS and poloxamer, evaluating stability and skin bioavailability to define an optimized formulation to effectively treat FA. Our studies have shown that TPGS improves the physicochemical behavior of rapamycin, i.e., its solubility and stability, due to a strong inclusion in micelles, while poloxamer P123 has a more significant influence on skin bioavailability. Accordingly, we formulated mixed-micelle hydrogels containing 0.1% rapamycin, and the optimized formulation was found to be stable for up to 3 months at 2–8 °C. In addition, compared to hydroalcoholic gel formulations, the studied system allows for better biodistribution on human skin. |
format | Online Article Text |
id | pubmed-8948846 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-89488462022-03-26 Mixed Polymeric Micelles for Rapamycin Skin Delivery Le Guyader, Guillaume Do, Bernard Rietveld, Ivo B. Coric, Pascale Bouaziz, Serge Guigner, Jean-Michel Secretan, Philippe-Henri Andrieux, Karine Paul, Muriel Pharmaceutics Article Facial angiofibromas (FA) are one of the most obvious cutaneous manifestations of tuberous sclerosis complex. Topical rapamycin for angiofibromas has been reported as a promising treatment. Several types of vehicles have been used hitherto, but polymeric micelles and especially those made of d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) seem to have shown better skin bioavailability of rapamycin than the so far commonly used ointments. To better understand the influence of polymeric micelles on the behavior of rapamycin, we explored it through mixed polymeric micelles combining TPGS and poloxamer, evaluating stability and skin bioavailability to define an optimized formulation to effectively treat FA. Our studies have shown that TPGS improves the physicochemical behavior of rapamycin, i.e., its solubility and stability, due to a strong inclusion in micelles, while poloxamer P123 has a more significant influence on skin bioavailability. Accordingly, we formulated mixed-micelle hydrogels containing 0.1% rapamycin, and the optimized formulation was found to be stable for up to 3 months at 2–8 °C. In addition, compared to hydroalcoholic gel formulations, the studied system allows for better biodistribution on human skin. MDPI 2022-03-04 /pmc/articles/PMC8948846/ /pubmed/35335945 http://dx.doi.org/10.3390/pharmaceutics14030569 Text en © 2022 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 Le Guyader, Guillaume Do, Bernard Rietveld, Ivo B. Coric, Pascale Bouaziz, Serge Guigner, Jean-Michel Secretan, Philippe-Henri Andrieux, Karine Paul, Muriel Mixed Polymeric Micelles for Rapamycin Skin Delivery |
title | Mixed Polymeric Micelles for Rapamycin Skin Delivery |
title_full | Mixed Polymeric Micelles for Rapamycin Skin Delivery |
title_fullStr | Mixed Polymeric Micelles for Rapamycin Skin Delivery |
title_full_unstemmed | Mixed Polymeric Micelles for Rapamycin Skin Delivery |
title_short | Mixed Polymeric Micelles for Rapamycin Skin Delivery |
title_sort | mixed polymeric micelles for rapamycin skin delivery |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8948846/ https://www.ncbi.nlm.nih.gov/pubmed/35335945 http://dx.doi.org/10.3390/pharmaceutics14030569 |
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