Development of Licorice Flavonoids Loaded Microemulsion for Transdermal Delivery Using CCD-Optimal Experimental Approach: Formulation Development and Characterization

In this research, we sought to surmount the poor dissolvability and transdermal absorption rate of licorice flavonoids (LFs) by fabricating a LFs microemulsion. LFs content was determined using high performance liquid chromatography. Initial studies such as dissolution testing, emulsification testin...

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Autores principales: Yang Xin, Shi Yun, Lu Yuhe, Mao Yinxue, Niu Shurui, Zhou Yue, Qin Kunming, Li Weidong
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Publicado: Frontiers Media S.A. 2021
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Acceso en línea:https://doaj.org/article/7e81a1d5d4024c39be4251443e5ce7cc
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spelling oai:doaj.org-article:7e81a1d5d4024c39be4251443e5ce7cc2021-11-18T09:41:16ZDevelopment of Licorice Flavonoids Loaded Microemulsion for Transdermal Delivery Using CCD-Optimal Experimental Approach: Formulation Development and Characterization2673-301310.3389/fnano.2021.748791https://doaj.org/article/7e81a1d5d4024c39be4251443e5ce7cc2021-11-01T00:00:00Zhttps://www.frontiersin.org/articles/10.3389/fnano.2021.748791/fullhttps://doaj.org/toc/2673-3013In this research, we sought to surmount the poor dissolvability and transdermal absorption rate of licorice flavonoids (LFs) by fabricating a LFs microemulsion. LFs content was determined using high performance liquid chromatography. Initial studies such as dissolution testing, emulsification testing, and pseudo ternary phase diagram generation were implemented for screening components and optimized adopting the central composite design. While the tested responses were solubility, droplet size and PDI, thirteen trials were performed using two different variables, oil percentage and optimized emulsifier and co-emulsifier ratio. Microemulsions were then characterized for droplet size, PDI, transmission electron microscopy, viscosity, electrical conductivity, pH, entrapment efficiency, drug content and stability. Additionally, skin release profile, percutaneous absorption and retention were investigated adopting Franz diffusion cell. The optimal formulation was found to compose of laureth-9 (emulsifier, 6.72 g), propylene glycol (co-emulsifier, 1.80 g), isopropyl myristate (IPM, oil, 1.48 g), LFs (1.50 g) and at least more than 85% deionized water. The optimized and storage for 3 months of microemulsion was found to clear, light yellow color without phase separation or precipitation indicated the stability of the preparation to long-term placement. The mean droplet size, PDI, entrapment efficiency and drug content were discovered as 12.68 ± 0.12 nm, 0.049 ± 0.005, 97.28 ± 0.13% and 122.67 ± 0.40 mg·g−1, respectively. Furthermore, the optimal formulation sustained release LFs, remarkably deliver more LFs through the skin layer (644.95 ± 6.73 μg cm−2) and significantly retained LFs in the skin layer (9.98 μg cm−2). The study concluded that optimized microemulsion has potential and enhanced the dissolvability and cumulative penetration amount of LFs.Yang XinShi YunLu YuheMao YinxueNiu ShuruiZhou YueQin KunmingLi WeidongFrontiers Media S.A.articlelicorice flavonoidsmicroemulsioncentral composite designpseudo ternary phase diagramformulation evaluationtransdermal deliveryChemical technologyTP1-1185ENFrontiers in Nanotechnology, Vol 3 (2021)
institution DOAJ
collection DOAJ
language EN
topic licorice flavonoids
microemulsion
central composite design
pseudo ternary phase diagram
formulation evaluation
transdermal delivery
Chemical technology
TP1-1185
spellingShingle licorice flavonoids
microemulsion
central composite design
pseudo ternary phase diagram
formulation evaluation
transdermal delivery
Chemical technology
TP1-1185
Yang Xin
Shi Yun
Lu Yuhe
Mao Yinxue
Niu Shurui
Zhou Yue
Qin Kunming
Li Weidong
Development of Licorice Flavonoids Loaded Microemulsion for Transdermal Delivery Using CCD-Optimal Experimental Approach: Formulation Development and Characterization
description In this research, we sought to surmount the poor dissolvability and transdermal absorption rate of licorice flavonoids (LFs) by fabricating a LFs microemulsion. LFs content was determined using high performance liquid chromatography. Initial studies such as dissolution testing, emulsification testing, and pseudo ternary phase diagram generation were implemented for screening components and optimized adopting the central composite design. While the tested responses were solubility, droplet size and PDI, thirteen trials were performed using two different variables, oil percentage and optimized emulsifier and co-emulsifier ratio. Microemulsions were then characterized for droplet size, PDI, transmission electron microscopy, viscosity, electrical conductivity, pH, entrapment efficiency, drug content and stability. Additionally, skin release profile, percutaneous absorption and retention were investigated adopting Franz diffusion cell. The optimal formulation was found to compose of laureth-9 (emulsifier, 6.72 g), propylene glycol (co-emulsifier, 1.80 g), isopropyl myristate (IPM, oil, 1.48 g), LFs (1.50 g) and at least more than 85% deionized water. The optimized and storage for 3 months of microemulsion was found to clear, light yellow color without phase separation or precipitation indicated the stability of the preparation to long-term placement. The mean droplet size, PDI, entrapment efficiency and drug content were discovered as 12.68 ± 0.12 nm, 0.049 ± 0.005, 97.28 ± 0.13% and 122.67 ± 0.40 mg·g−1, respectively. Furthermore, the optimal formulation sustained release LFs, remarkably deliver more LFs through the skin layer (644.95 ± 6.73 μg cm−2) and significantly retained LFs in the skin layer (9.98 μg cm−2). The study concluded that optimized microemulsion has potential and enhanced the dissolvability and cumulative penetration amount of LFs.
format article
author Yang Xin
Shi Yun
Lu Yuhe
Mao Yinxue
Niu Shurui
Zhou Yue
Qin Kunming
Li Weidong
author_facet Yang Xin
Shi Yun
Lu Yuhe
Mao Yinxue
Niu Shurui
Zhou Yue
Qin Kunming
Li Weidong
author_sort Yang Xin
title Development of Licorice Flavonoids Loaded Microemulsion for Transdermal Delivery Using CCD-Optimal Experimental Approach: Formulation Development and Characterization
title_short Development of Licorice Flavonoids Loaded Microemulsion for Transdermal Delivery Using CCD-Optimal Experimental Approach: Formulation Development and Characterization
title_full Development of Licorice Flavonoids Loaded Microemulsion for Transdermal Delivery Using CCD-Optimal Experimental Approach: Formulation Development and Characterization
title_fullStr Development of Licorice Flavonoids Loaded Microemulsion for Transdermal Delivery Using CCD-Optimal Experimental Approach: Formulation Development and Characterization
title_full_unstemmed Development of Licorice Flavonoids Loaded Microemulsion for Transdermal Delivery Using CCD-Optimal Experimental Approach: Formulation Development and Characterization
title_sort development of licorice flavonoids loaded microemulsion for transdermal delivery using ccd-optimal experimental approach: formulation development and characterization
publisher Frontiers Media S.A.
publishDate 2021
url https://doaj.org/article/7e81a1d5d4024c39be4251443e5ce7cc
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