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Microemulsion-based hydrogels for enhancing epidermal/dermal deposition of topically administered 20(S)-protopanaxadiol: in vitro and in vivo evaluation studies

BACKGROUND: 20(S)-Protopanaxadiol (20S-PPD) is a fully deglycosylated ginsenoside metabolite and has potent dermal antiaging activity. However, because of its low aqueous solubility and large molecular size, a suitable formulation strategy is required to improve its solubility and skin permeability,...

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Autores principales: Kim, Ki-Taek, Kim, Min-Hwan, Park, Ju-Hwan, Lee, Jae-Young, Cho, Hyun-Jong, Yoon, In-Soo, Kim, Dae-Duk
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6190503/
https://www.ncbi.nlm.nih.gov/pubmed/30337812
http://dx.doi.org/10.1016/j.jgr.2017.07.005
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author Kim, Ki-Taek
Kim, Min-Hwan
Park, Ju-Hwan
Lee, Jae-Young
Cho, Hyun-Jong
Yoon, In-Soo
Kim, Dae-Duk
author_facet Kim, Ki-Taek
Kim, Min-Hwan
Park, Ju-Hwan
Lee, Jae-Young
Cho, Hyun-Jong
Yoon, In-Soo
Kim, Dae-Duk
author_sort Kim, Ki-Taek
collection PubMed
description BACKGROUND: 20(S)-Protopanaxadiol (20S-PPD) is a fully deglycosylated ginsenoside metabolite and has potent dermal antiaging activity. However, because of its low aqueous solubility and large molecular size, a suitable formulation strategy is required to improve its solubility and skin permeability, thereby enhancing its skin deposition. Thus, we optimized microemulsion (ME)-based hydrogel (MEH) formulations for the topical delivery of 20S-PPD. METHODS: MEs and MEHs were formulated and evaluated for their particle size distribution, morphology, drug loading capacity, and stability. Then, the deposition profiles of the selected 20S-PPD-loaded MEH formulation were studied using a hairless mouse skin model and Strat-M membrane as an artificial skin model. RESULTS: A Carbopol-based MEH system of 20S-PPD was successfully prepared with a mean droplet size of 110 nm and narrow size distribution. The formulation was stable for 56 d, and its viscosity was high enough for its topical application. It significantly enhanced the in vitro and in vivo skin deposition of 20S-PPD with no influence on its systemic absorption in hairless mice. Notably, it was found that the Strat-M membrane provided skin deposition data well correlated to those obtained from the in vitro and in vivo mouse skin studies on 20S-PPD (correlation coefficient r(2) = 0.929‒0.947). CONCLUSION: The MEH formulation developed in this study could serve as an effective topical delivery system for poorly soluble ginsenosides and their deglycosylated metabolites, including 20S-PPD.
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spelling pubmed-61905032018-10-18 Microemulsion-based hydrogels for enhancing epidermal/dermal deposition of topically administered 20(S)-protopanaxadiol: in vitro and in vivo evaluation studies Kim, Ki-Taek Kim, Min-Hwan Park, Ju-Hwan Lee, Jae-Young Cho, Hyun-Jong Yoon, In-Soo Kim, Dae-Duk J Ginseng Res Research Article BACKGROUND: 20(S)-Protopanaxadiol (20S-PPD) is a fully deglycosylated ginsenoside metabolite and has potent dermal antiaging activity. However, because of its low aqueous solubility and large molecular size, a suitable formulation strategy is required to improve its solubility and skin permeability, thereby enhancing its skin deposition. Thus, we optimized microemulsion (ME)-based hydrogel (MEH) formulations for the topical delivery of 20S-PPD. METHODS: MEs and MEHs were formulated and evaluated for their particle size distribution, morphology, drug loading capacity, and stability. Then, the deposition profiles of the selected 20S-PPD-loaded MEH formulation were studied using a hairless mouse skin model and Strat-M membrane as an artificial skin model. RESULTS: A Carbopol-based MEH system of 20S-PPD was successfully prepared with a mean droplet size of 110 nm and narrow size distribution. The formulation was stable for 56 d, and its viscosity was high enough for its topical application. It significantly enhanced the in vitro and in vivo skin deposition of 20S-PPD with no influence on its systemic absorption in hairless mice. Notably, it was found that the Strat-M membrane provided skin deposition data well correlated to those obtained from the in vitro and in vivo mouse skin studies on 20S-PPD (correlation coefficient r(2) = 0.929‒0.947). CONCLUSION: The MEH formulation developed in this study could serve as an effective topical delivery system for poorly soluble ginsenosides and their deglycosylated metabolites, including 20S-PPD. Elsevier 2018-10 2017-08-18 /pmc/articles/PMC6190503/ /pubmed/30337812 http://dx.doi.org/10.1016/j.jgr.2017.07.005 Text en © 2017 The Korean Society of Ginseng, Published by Elsevier Korea LLC. http://creativecommons.org/licenses/by-nc-nd/4.0/ This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Research Article
Kim, Ki-Taek
Kim, Min-Hwan
Park, Ju-Hwan
Lee, Jae-Young
Cho, Hyun-Jong
Yoon, In-Soo
Kim, Dae-Duk
Microemulsion-based hydrogels for enhancing epidermal/dermal deposition of topically administered 20(S)-protopanaxadiol: in vitro and in vivo evaluation studies
title Microemulsion-based hydrogels for enhancing epidermal/dermal deposition of topically administered 20(S)-protopanaxadiol: in vitro and in vivo evaluation studies
title_full Microemulsion-based hydrogels for enhancing epidermal/dermal deposition of topically administered 20(S)-protopanaxadiol: in vitro and in vivo evaluation studies
title_fullStr Microemulsion-based hydrogels for enhancing epidermal/dermal deposition of topically administered 20(S)-protopanaxadiol: in vitro and in vivo evaluation studies
title_full_unstemmed Microemulsion-based hydrogels for enhancing epidermal/dermal deposition of topically administered 20(S)-protopanaxadiol: in vitro and in vivo evaluation studies
title_short Microemulsion-based hydrogels for enhancing epidermal/dermal deposition of topically administered 20(S)-protopanaxadiol: in vitro and in vivo evaluation studies
title_sort microemulsion-based hydrogels for enhancing epidermal/dermal deposition of topically administered 20(s)-protopanaxadiol: in vitro and in vivo evaluation studies
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6190503/
https://www.ncbi.nlm.nih.gov/pubmed/30337812
http://dx.doi.org/10.1016/j.jgr.2017.07.005
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