Fabrication and in vitro/in vivo evaluation of amorphous andrographolide nanosuspensions stabilized by D-α-tocopheryl polyethylene glycol 1000 succinate/sodium lauryl sulfate

Fabrication and in vitro/in vivo evaluation of amorphous andrographolide nanosuspensions stabilized by D-α-tocopheryl polyethylene glycol 1000 succinate/sodium lauryl sulfate

Hongzhi Qiao,1,2,* Lihua Chen,3,* Tianqi Rui,1,2 Jingxian Wang,1,2 Ting Chen,1,2 Tingming Fu,1,2 Junsong Li,1,2 Liuqing Di1,2 1College of Pharmacy, Nanjing University of Chinese Medicine, 2Jiangsu Engineering Research Center for Efficient Delivery System of TCM, Nanjing, 3Key Laboratory of Modern P...

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Autores principales: Qiao H, Chen L, Rui T, Wang J, Chen T, Fu T, Li J, Di L
Formato: article
Lenguaje:EN
Publicado: Dove Medical Press 2017
Materias:
Andrographolide
Nanosuspensions
Box-Behnken design
D-alpha-tocopheryl polyethylene glycol 1000 succinate
Dissolution rate
Oral bioavailability
Medicine (General)
R5-920
Acceso en línea:https://doaj.org/article/6de5684afe7b4eeb9993eba303a5c87e
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spelling oai:doaj.org-article:6de5684afe7b4eeb9993eba303a5c87e2021-12-02T04:33:04ZFabrication and in vitro/in vivo evaluation of amorphous andrographolide nanosuspensions stabilized by D-α-tocopheryl polyethylene glycol 1000 succinate/sodium lauryl sulfate1178-2013https://doaj.org/article/6de5684afe7b4eeb9993eba303a5c87e2017-02-01T00:00:00Zhttps://www.dovepress.com/fabrication-and-in-vitroin-vivo--evaluation-of-amorphous-andrographoli-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Hongzhi Qiao,1,2,* Lihua Chen,3,* Tianqi Rui,1,2 Jingxian Wang,1,2 Ting Chen,1,2 Tingming Fu,1,2 Junsong Li,1,2 Liuqing Di1,2 1College of Pharmacy, Nanjing University of Chinese Medicine, 2Jiangsu Engineering Research Center for Efficient Delivery System of TCM, Nanjing, 3Key Laboratory of Modern Preparation of Traditional Chinese Medicine, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang, China *These authors contributed equally to this work Abstract: Andrographolide (ADG) is a diterpenoid isolated from Andrographis paniculata with a wide spectrum of biological activities, including anti-inflammatory, anticancer and hepatoprotective effects. However, its poor water solubility and efflux by P-glycoprotein have resulted in lower bioavailability. In this study, ADG nanosuspensions (ADG-NS) were prepared using a wet media milling technique followed by freeze drying. D-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS), a surfactant that inhibits P-glycoprotein function, and sodium lauryl sulfate were used as surface stabilizers. A Box–Behnken design was used to optimize the nanosuspension preparation. The products of these optimal preparation conditions were amorphous and possessed much faster dissolution in vitro than a coarse powder of ADG. The particle size and redispersibility index of the freeze-dried ADG-NS were 244.6±3.0 nm and 113%±1.14% (n=3), respectively. A short-term stability study indicated that the freeze-dried ADG-NS could remain highly stable as nanosuspensions during the testing period. A test of transport across a Caco-2 cell monolayer revealed that the membrane permeability (Papp) of ADG-NS was significantly higher than the permeability of the ADG coarse powder or ADG-NS without TPGS (P<0.01). Compared to the ADG coarse powder, a physical mixture, commercial dripping pills and ADG-NS without TPGS, ADG-NS exhibited significantly higher plasma exposure with significant enhancements in Cmax and area under the curve of plasma concentration versus time from zero to the last sampling time (AUC0–t) (P<0.01). An evaluation of the anti-inflammatory effect on Carr-induced paw edema demonstrated that the ADG-NS were more effective in reducing the rate of paw swelling, producing a greater increase in the serum levels of nitric oxide (NO), Interleukin-1 (IL-1) and tumor necrosis factor-α (TNF-α) (P<0.01) and an increase in superoxide dismutase activity (P<0.05) compared to the ADG coarse powder. This study indicated that nanosuspensions could act as an effective delivery device for ADG to enhance its oral bioavailability and biological efficacy. Keywords: andrographolide, nanosuspensions, Box–Behnken design, D-α-tocopheryl polyethylene glycol 1000 succinate, dissolution rate, oral bioavailabilityQiao HChen LRui TWang JChen TFu TLi JDi LDove Medical PressarticleAndrographolideNanosuspensionsBox-Behnken designD-alpha-tocopheryl polyethylene glycol 1000 succinateDissolution rateOral bioavailabilityMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 12, Pp 1033-1046 (2017)
institution DOAJ
collection DOAJ
language EN
topic Andrographolide
Nanosuspensions
Box-Behnken design
D-alpha-tocopheryl polyethylene glycol 1000 succinate
Dissolution rate
Oral bioavailability
Medicine (General)
R5-920
spellingShingle Andrographolide
Nanosuspensions
Box-Behnken design
D-alpha-tocopheryl polyethylene glycol 1000 succinate
Dissolution rate
Oral bioavailability
Medicine (General)
R5-920
Qiao H
Chen L
Rui T
Wang J
Chen T
Fu T
Li J
Di L
Fabrication and in vitro/in vivo evaluation of amorphous andrographolide nanosuspensions stabilized by D-α-tocopheryl polyethylene glycol 1000 succinate/sodium lauryl sulfate
description Hongzhi Qiao,1,2,* Lihua Chen,3,* Tianqi Rui,1,2 Jingxian Wang,1,2 Ting Chen,1,2 Tingming Fu,1,2 Junsong Li,1,2 Liuqing Di1,2 1College of Pharmacy, Nanjing University of Chinese Medicine, 2Jiangsu Engineering Research Center for Efficient Delivery System of TCM, Nanjing, 3Key Laboratory of Modern Preparation of Traditional Chinese Medicine, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang, China *These authors contributed equally to this work Abstract: Andrographolide (ADG) is a diterpenoid isolated from Andrographis paniculata with a wide spectrum of biological activities, including anti-inflammatory, anticancer and hepatoprotective effects. However, its poor water solubility and efflux by P-glycoprotein have resulted in lower bioavailability. In this study, ADG nanosuspensions (ADG-NS) were prepared using a wet media milling technique followed by freeze drying. D-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS), a surfactant that inhibits P-glycoprotein function, and sodium lauryl sulfate were used as surface stabilizers. A Box–Behnken design was used to optimize the nanosuspension preparation. The products of these optimal preparation conditions were amorphous and possessed much faster dissolution in vitro than a coarse powder of ADG. The particle size and redispersibility index of the freeze-dried ADG-NS were 244.6±3.0 nm and 113%±1.14% (n=3), respectively. A short-term stability study indicated that the freeze-dried ADG-NS could remain highly stable as nanosuspensions during the testing period. A test of transport across a Caco-2 cell monolayer revealed that the membrane permeability (Papp) of ADG-NS was significantly higher than the permeability of the ADG coarse powder or ADG-NS without TPGS (P<0.01). Compared to the ADG coarse powder, a physical mixture, commercial dripping pills and ADG-NS without TPGS, ADG-NS exhibited significantly higher plasma exposure with significant enhancements in Cmax and area under the curve of plasma concentration versus time from zero to the last sampling time (AUC0–t) (P<0.01). An evaluation of the anti-inflammatory effect on Carr-induced paw edema demonstrated that the ADG-NS were more effective in reducing the rate of paw swelling, producing a greater increase in the serum levels of nitric oxide (NO), Interleukin-1 (IL-1) and tumor necrosis factor-α (TNF-α) (P<0.01) and an increase in superoxide dismutase activity (P<0.05) compared to the ADG coarse powder. This study indicated that nanosuspensions could act as an effective delivery device for ADG to enhance its oral bioavailability and biological efficacy. Keywords: andrographolide, nanosuspensions, Box–Behnken design, D-α-tocopheryl polyethylene glycol 1000 succinate, dissolution rate, oral bioavailability
format article
author Qiao H
Chen L
Rui T
Wang J
Chen T
Fu T
Li J
Di L
author_facet Qiao H
Chen L
Rui T
Wang J
Chen T
Fu T
Li J
Di L
author_sort Qiao H
title Fabrication and in vitro/in vivo evaluation of amorphous andrographolide nanosuspensions stabilized by D-α-tocopheryl polyethylene glycol 1000 succinate/sodium lauryl sulfate
title_short Fabrication and in vitro/in vivo evaluation of amorphous andrographolide nanosuspensions stabilized by D-α-tocopheryl polyethylene glycol 1000 succinate/sodium lauryl sulfate
title_full Fabrication and in vitro/in vivo evaluation of amorphous andrographolide nanosuspensions stabilized by D-α-tocopheryl polyethylene glycol 1000 succinate/sodium lauryl sulfate
title_fullStr Fabrication and in vitro/in vivo evaluation of amorphous andrographolide nanosuspensions stabilized by D-α-tocopheryl polyethylene glycol 1000 succinate/sodium lauryl sulfate
title_full_unstemmed Fabrication and in vitro/in vivo evaluation of amorphous andrographolide nanosuspensions stabilized by D-α-tocopheryl polyethylene glycol 1000 succinate/sodium lauryl sulfate
title_sort fabrication and in vitro/in vivo evaluation of amorphous andrographolide nanosuspensions stabilized by d-α-tocopheryl polyethylene glycol 1000 succinate/sodium lauryl sulfate
publisher Dove Medical Press
publishDate 2017
url https://doaj.org/article/6de5684afe7b4eeb9993eba303a5c87e
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