Nanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide

Ching-Chi Yen,1 Yi-Chen Chen,1 Ming-Tsang Wu,2 Chia-Chi Wang,1,3 Yu-Tse Wu1,4 1School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan; 2Chinese Medicine Department, Ditmanson Medical Foundation, Chiayi Christian Hospital, Chiayi City, Taiwan; 3PhD Program in Toxico...

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Autores principales:	Yen CC, Chen YC, Wu MT, Wang CC, Wu YT
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2018
Materias:	andrographolide nanoemulsion intestinal permeability oral bioavailability Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/6ecb56919ca64506a6b7c6cd7a30c0ea
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spelling	oai:doaj.org-article:6ecb56919ca64506a6b7c6cd7a30c0ea2021-12-02T05:09:47ZNanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide1178-2013https://doaj.org/article/6ecb56919ca64506a6b7c6cd7a30c0ea2018-01-01T00:00:00Zhttps://www.dovepress.com/nanoemulsion-as-a-strategy-for-improving-the-oral-bioavailability-and--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Ching-Chi Yen,1 Yi-Chen Chen,1 Ming-Tsang Wu,2 Chia-Chi Wang,1,3 Yu-Tse Wu1,4 1School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan; 2Chinese Medicine Department, Ditmanson Medical Foundation, Chiayi Christian Hospital, Chiayi City, Taiwan; 3PhD Program in Toxicology, College of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan; 4Department of Medical Research, Kaohsiung Medical University Hospital, Kaohsiung, Taiwan Background: Andrographolide (AG), a compound with low water solubility, possesses various pharmacological activities, particularly anti-inflammatory activity. However, its low oral bioavailability is a major obstacle to its potential use. This study developed and optimized an AG-loaded nanoemulsion (AG-NE) formulation to improve AG oral bioavailability and its protective effects against inflammatory bowel disease. Methods: A high-pressure homogenization technique was used to prepare the AG-NE and solubility, viscosity, and droplet size tests were conducted to develop the optimized AG-NE composed of α-tocopherol, ethanol, Cremophor EL, and water. The permeability was assessed using everted rat gut sac method and in vivo absorption and anti-inflammatory effect in rats was also evaluated. The plasma concentration of AG was determined using our validated high performance liquid chromatography method, which was used to generate a linear calibration curve over the concentration range of 0.1–25 µg/mL in rat plasma (R2>0.999).Results: The optimized AG-NE had a droplet size of 122±11 nm confirmed using transmission electron microscopy and a viscosity of 28 centipoise (cps). It was stable at 4 and 25°C for 90 days. An ex vitro intestinal permeability study indicated that the jejunum was the optimal site for AG absorption from the optimized AG-NE, which was 8.21 and 1.40 times higher than that from an AG suspension and AG ethanol solution, respectively. The pharmacokinetic results indicate that the absorption of AG from AG-NE was significantly enhanced in comparison with that from the AG suspension, with a relative bioavailability of 594.3%. Moreover, the ulcer index and histological damage score of mice with indomethacin-induced intestinal lesions were significantly reduced by AG-NE pretreatment. Conclusion: We conclude that the developed AG-NE not only enhanced the oral bioavailability of AG in this study but may also prove to be an effective formulation of AG for preventing gastrointestinal inflammatory disorders. Keywords: andrographolide, nanoemulsion, intestinal permeability, oral bioavailabilityYen CCChen YCWu MTWang CCWu YTDove Medical Pressarticleandrographolidenanoemulsionintestinal permeabilityoral bioavailabilityMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 13, Pp 669-680 (2018)
institution	DOAJ
collection	DOAJ
language	EN
topic	andrographolide nanoemulsion intestinal permeability oral bioavailability Medicine (General) R5-920
spellingShingle	andrographolide nanoemulsion intestinal permeability oral bioavailability Medicine (General) R5-920 Yen CC Chen YC Wu MT Wang CC Wu YT Nanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide
description	Ching-Chi Yen,1 Yi-Chen Chen,1 Ming-Tsang Wu,2 Chia-Chi Wang,1,3 Yu-Tse Wu1,4 1School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan; 2Chinese Medicine Department, Ditmanson Medical Foundation, Chiayi Christian Hospital, Chiayi City, Taiwan; 3PhD Program in Toxicology, College of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan; 4Department of Medical Research, Kaohsiung Medical University Hospital, Kaohsiung, Taiwan Background: Andrographolide (AG), a compound with low water solubility, possesses various pharmacological activities, particularly anti-inflammatory activity. However, its low oral bioavailability is a major obstacle to its potential use. This study developed and optimized an AG-loaded nanoemulsion (AG-NE) formulation to improve AG oral bioavailability and its protective effects against inflammatory bowel disease. Methods: A high-pressure homogenization technique was used to prepare the AG-NE and solubility, viscosity, and droplet size tests were conducted to develop the optimized AG-NE composed of α-tocopherol, ethanol, Cremophor EL, and water. The permeability was assessed using everted rat gut sac method and in vivo absorption and anti-inflammatory effect in rats was also evaluated. The plasma concentration of AG was determined using our validated high performance liquid chromatography method, which was used to generate a linear calibration curve over the concentration range of 0.1–25 µg/mL in rat plasma (R2>0.999).Results: The optimized AG-NE had a droplet size of 122±11 nm confirmed using transmission electron microscopy and a viscosity of 28 centipoise (cps). It was stable at 4 and 25°C for 90 days. An ex vitro intestinal permeability study indicated that the jejunum was the optimal site for AG absorption from the optimized AG-NE, which was 8.21 and 1.40 times higher than that from an AG suspension and AG ethanol solution, respectively. The pharmacokinetic results indicate that the absorption of AG from AG-NE was significantly enhanced in comparison with that from the AG suspension, with a relative bioavailability of 594.3%. Moreover, the ulcer index and histological damage score of mice with indomethacin-induced intestinal lesions were significantly reduced by AG-NE pretreatment. Conclusion: We conclude that the developed AG-NE not only enhanced the oral bioavailability of AG in this study but may also prove to be an effective formulation of AG for preventing gastrointestinal inflammatory disorders. Keywords: andrographolide, nanoemulsion, intestinal permeability, oral bioavailability
format	article
author	Yen CC Chen YC Wu MT Wang CC Wu YT
author_facet	Yen CC Chen YC Wu MT Wang CC Wu YT
author_sort	Yen CC
title	Nanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide
title_short	Nanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide
title_full	Nanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide
title_fullStr	Nanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide
title_full_unstemmed	Nanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide
title_sort	nanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide
publisher	Dove Medical Press
publishDate	2018
url	https://doaj.org/article/6ecb56919ca64506a6b7c6cd7a30c0ea
work_keys_str_mv	AT yencc nanoemulsionasastrategyforimprovingtheoralbioavailabilityandantiinflammatoryactivityofandrographolide AT chenyc nanoemulsionasastrategyforimprovingtheoralbioavailabilityandantiinflammatoryactivityofandrographolide AT wumt nanoemulsionasastrategyforimprovingtheoralbioavailabilityandantiinflammatoryactivityofandrographolide AT wangcc nanoemulsionasastrategyforimprovingtheoralbioavailabilityandantiinflammatoryactivityofandrographolide AT wuyt nanoemulsionasastrategyforimprovingtheoralbioavailabilityandantiinflammatoryactivityofandrographolide
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Nanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide

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