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Lipid Nanoparticles for Enhancing the Physicochemical Stability and Topical Skin Delivery of Orobol

Orobol is one of the major soy isoflavones, and has been reported to have various pharmacological activities, including an anti-skin-aging effect. However, since it has low solubility in water and physicochemical instability, the formulation of orobol for delivery into the dermal layer of the skin c...

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Autores principales: Kim, Min-Hwan, Jeon, Yae-Eun, Kang, Soobeen, Lee, Jae-Young, Lee, Ki Won, Kim, Ki-Taek, Kim, Dae-Duk
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7560103/
https://www.ncbi.nlm.nih.gov/pubmed/32899309
http://dx.doi.org/10.3390/pharmaceutics12090845
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author Kim, Min-Hwan
Jeon, Yae-Eun
Kang, Soobeen
Lee, Jae-Young
Lee, Ki Won
Kim, Ki-Taek
Kim, Dae-Duk
author_facet Kim, Min-Hwan
Jeon, Yae-Eun
Kang, Soobeen
Lee, Jae-Young
Lee, Ki Won
Kim, Ki-Taek
Kim, Dae-Duk
author_sort Kim, Min-Hwan
collection PubMed
description Orobol is one of the major soy isoflavones, and has been reported to have various pharmacological activities, including an anti-skin-aging effect. However, since it has low solubility in water and physicochemical instability, the formulation of orobol for delivery into the dermal layer of the skin could be challenging. The objective of this study was to prepare lipid nanoparticles formulations of orobol to enhance its stability as well as its deposition into the skin. Formulations of orobol-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were characterized in terms of their mean particle size, entrapment efficiency, and morphology. The nano-sized spherical NLCs formulations maintained the stability of orobol for up to 28 days. Moreover, the NLCs formulation significantly increased the in vitro deposition of orobol into both Strat-M membranes and human cadaver skin compared with the other formulations. Additionally, the NLCs formulation did not cause significant skin irritation in clinical study. These results demonstrate that a shea butter-based NLC formulation could be a promising and safe carrier system for improving the stability of orobol and enhancing its topical skin delivery.
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spelling pubmed-75601032020-10-22 Lipid Nanoparticles for Enhancing the Physicochemical Stability and Topical Skin Delivery of Orobol Kim, Min-Hwan Jeon, Yae-Eun Kang, Soobeen Lee, Jae-Young Lee, Ki Won Kim, Ki-Taek Kim, Dae-Duk Pharmaceutics Article Orobol is one of the major soy isoflavones, and has been reported to have various pharmacological activities, including an anti-skin-aging effect. However, since it has low solubility in water and physicochemical instability, the formulation of orobol for delivery into the dermal layer of the skin could be challenging. The objective of this study was to prepare lipid nanoparticles formulations of orobol to enhance its stability as well as its deposition into the skin. Formulations of orobol-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were characterized in terms of their mean particle size, entrapment efficiency, and morphology. The nano-sized spherical NLCs formulations maintained the stability of orobol for up to 28 days. Moreover, the NLCs formulation significantly increased the in vitro deposition of orobol into both Strat-M membranes and human cadaver skin compared with the other formulations. Additionally, the NLCs formulation did not cause significant skin irritation in clinical study. These results demonstrate that a shea butter-based NLC formulation could be a promising and safe carrier system for improving the stability of orobol and enhancing its topical skin delivery. MDPI 2020-09-03 /pmc/articles/PMC7560103/ /pubmed/32899309 http://dx.doi.org/10.3390/pharmaceutics12090845 Text en © 2020 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
Kim, Min-Hwan
Jeon, Yae-Eun
Kang, Soobeen
Lee, Jae-Young
Lee, Ki Won
Kim, Ki-Taek
Kim, Dae-Duk
Lipid Nanoparticles for Enhancing the Physicochemical Stability and Topical Skin Delivery of Orobol
title Lipid Nanoparticles for Enhancing the Physicochemical Stability and Topical Skin Delivery of Orobol
title_full Lipid Nanoparticles for Enhancing the Physicochemical Stability and Topical Skin Delivery of Orobol
title_fullStr Lipid Nanoparticles for Enhancing the Physicochemical Stability and Topical Skin Delivery of Orobol
title_full_unstemmed Lipid Nanoparticles for Enhancing the Physicochemical Stability and Topical Skin Delivery of Orobol
title_short Lipid Nanoparticles for Enhancing the Physicochemical Stability and Topical Skin Delivery of Orobol
title_sort lipid nanoparticles for enhancing the physicochemical stability and topical skin delivery of orobol
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7560103/
https://www.ncbi.nlm.nih.gov/pubmed/32899309
http://dx.doi.org/10.3390/pharmaceutics12090845
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