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The Topical Nanodelivery of Vismodegib Enhances Its Skin Penetration and Performance In Vitro While Reducing Its Toxicity In Vivo
Vismodegib is a first-in-class inhibitor for advanced basal cell carcinoma treatment. Its daily oral doses present a high distribution volume and several side effects. We evaluated its skin penetration loaded in diverse nanosystems as potential strategies to reduce side effects and drug quantities....
Autores principales: | , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7912039/ https://www.ncbi.nlm.nih.gov/pubmed/33535434 http://dx.doi.org/10.3390/pharmaceutics13020186 |
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author | Calienni, Maria Natalia Maza Vega, Daniela Temprana, C. Facundo Izquierdo, María Cecilia Ybarra, David E. Bernabeu, Ezequiel Moretton, Marcela Alvira, Fernando C. Chiappetta, Diego Alonso, Silvia del Valle Prieto, María Jimena Montanari, Jorge |
author_facet | Calienni, Maria Natalia Maza Vega, Daniela Temprana, C. Facundo Izquierdo, María Cecilia Ybarra, David E. Bernabeu, Ezequiel Moretton, Marcela Alvira, Fernando C. Chiappetta, Diego Alonso, Silvia del Valle Prieto, María Jimena Montanari, Jorge |
author_sort | Calienni, Maria Natalia |
collection | PubMed |
description | Vismodegib is a first-in-class inhibitor for advanced basal cell carcinoma treatment. Its daily oral doses present a high distribution volume and several side effects. We evaluated its skin penetration loaded in diverse nanosystems as potential strategies to reduce side effects and drug quantities. Ultradeformable liposomes, ethosomes, colloidal liquid crystals, and dendrimers were able to transport Vismodegib to deep skin layers, while polymeric micelles failed at this. As lipidic systems were the most effective, we assessed the in vitro and in vivo toxicity of Vismodegib-loaded ultradeformable liposomes, apoptosis, and cellular uptake. Vismodegib emerges as a versatile drug that can be loaded in several delivery systems for topical application. These findings may be also useful for the consideration of topical delivery of other drugs with a low water solubility. |
format | Online Article Text |
id | pubmed-7912039 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-79120392021-02-28 The Topical Nanodelivery of Vismodegib Enhances Its Skin Penetration and Performance In Vitro While Reducing Its Toxicity In Vivo Calienni, Maria Natalia Maza Vega, Daniela Temprana, C. Facundo Izquierdo, María Cecilia Ybarra, David E. Bernabeu, Ezequiel Moretton, Marcela Alvira, Fernando C. Chiappetta, Diego Alonso, Silvia del Valle Prieto, María Jimena Montanari, Jorge Pharmaceutics Article Vismodegib is a first-in-class inhibitor for advanced basal cell carcinoma treatment. Its daily oral doses present a high distribution volume and several side effects. We evaluated its skin penetration loaded in diverse nanosystems as potential strategies to reduce side effects and drug quantities. Ultradeformable liposomes, ethosomes, colloidal liquid crystals, and dendrimers were able to transport Vismodegib to deep skin layers, while polymeric micelles failed at this. As lipidic systems were the most effective, we assessed the in vitro and in vivo toxicity of Vismodegib-loaded ultradeformable liposomes, apoptosis, and cellular uptake. Vismodegib emerges as a versatile drug that can be loaded in several delivery systems for topical application. These findings may be also useful for the consideration of topical delivery of other drugs with a low water solubility. MDPI 2021-02-01 /pmc/articles/PMC7912039/ /pubmed/33535434 http://dx.doi.org/10.3390/pharmaceutics13020186 Text en © 2021 by the authors. 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/). |
spellingShingle | Article Calienni, Maria Natalia Maza Vega, Daniela Temprana, C. Facundo Izquierdo, María Cecilia Ybarra, David E. Bernabeu, Ezequiel Moretton, Marcela Alvira, Fernando C. Chiappetta, Diego Alonso, Silvia del Valle Prieto, María Jimena Montanari, Jorge The Topical Nanodelivery of Vismodegib Enhances Its Skin Penetration and Performance In Vitro While Reducing Its Toxicity In Vivo |
title | The Topical Nanodelivery of Vismodegib Enhances Its Skin Penetration and Performance In Vitro While Reducing Its Toxicity In Vivo |
title_full | The Topical Nanodelivery of Vismodegib Enhances Its Skin Penetration and Performance In Vitro While Reducing Its Toxicity In Vivo |
title_fullStr | The Topical Nanodelivery of Vismodegib Enhances Its Skin Penetration and Performance In Vitro While Reducing Its Toxicity In Vivo |
title_full_unstemmed | The Topical Nanodelivery of Vismodegib Enhances Its Skin Penetration and Performance In Vitro While Reducing Its Toxicity In Vivo |
title_short | The Topical Nanodelivery of Vismodegib Enhances Its Skin Penetration and Performance In Vitro While Reducing Its Toxicity In Vivo |
title_sort | topical nanodelivery of vismodegib enhances its skin penetration and performance in vitro while reducing its toxicity in vivo |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7912039/ https://www.ncbi.nlm.nih.gov/pubmed/33535434 http://dx.doi.org/10.3390/pharmaceutics13020186 |
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