Galactosylated PLGA nanoparticles for the oral delivery of resveratrol: enhanced bioavailability and in vitro anti-inflammatory activity

Frederick YK Siu,1–3 Shaotang Ye,1–3 Hui Lin,1–3 Shoujun Li1–3 1College of Veterinary Medicine, South China Agricultural University, Guangzhou, People’s Republic of China; 2Guangdong Provincial Key Laboratory of Prevention and Control for Severe Cli...

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Autores principales: Siu FYK, Ye S, Lin H, Li S
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Publicado: Dove Medical Press 2018
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spelling oai:doaj.org-article:afe0ebb3a3d24e0ba717d657e91409872021-12-02T08:50:03ZGalactosylated PLGA nanoparticles for the oral delivery of resveratrol: enhanced bioavailability and in vitro anti-inflammatory activity1178-2013https://doaj.org/article/afe0ebb3a3d24e0ba717d657e91409872018-07-01T00:00:00Zhttps://www.dovepress.com/galactosylated-plga-nanoparticles-for-the-oral-delivery-of-resveratrol-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Frederick YK Siu,1–3 Shaotang Ye,1–3 Hui Lin,1–3 Shoujun Li1–3 1College of Veterinary Medicine, South China Agricultural University, Guangzhou, People’s Republic of China; 2Guangdong Provincial Key Laboratory of Prevention and Control for Severe Clinical Animal Diseases, Guangzhou, People’s Republic of China; 3Guangdong Technological Engineering Research Center for Pet, Guangzhou, People’s Republic of China Background: Resveratrol (RES) is a natural anti-inflammatory and antioxidant compound with poor water solubility and oral bioavailability. The present study takes the advantages of nanocarriers combined with a ligand (galactose) anchoring to orally deliver RES in an attempt to improve its bioavailability and pharmacological activity. Methods: RES-loaded galactosylated nanoparticles (RES-GNPs) were prepared by solvent diffusion technique using poly(lactic-co-glycolic acid), synthesized N-oleoyl-d-galactosamine and Tween 80. RES-GNPs were characterized by particle size, morphology, entrapment efficiency (EE) and in vitro release. Oral bioavailability and in vitro anti-inflammatory activity were investigated in rats and lipopolysaccharides-induced RAW 264.7 cells, respectively. Results: The resulting RES-GNPs were 108.4 nm around in particle size with a polydispersity index of 0.217. Furthermore, RES-GNPs possessed a high EE and a slow drug release in water. After oral administration, RES-GNPs significantly enhanced the oral bioavailability of RES, up to 335.7% relative to RES suspensions. In situ single-pass intestinal perfusion and cellular uptake experiments showed that GNPs could improve the intestinal permeability and transcellular transport of RES. Moreover, the anti-inflammatory efficacy of RES-GNPs in RAW 264.7 cells model was superior to free RES and RES-GNPs. Conclusion: The results indicate that RES-GNPs can effectively promote the intestinal absorption of RES and strengthen its bioactivity, which may be a promising system for the treatment of inflammatory diseases. Keywords: resveratrol, polymeric nanoparticles, galactosylation, oral bioavailability, anti-inflammationSiu FYKYe SLin HLi SDove Medical Pressarticleresveratrolpolymeric nanoparticlesgalactosylationoral bioavailabilityanti-inflammationMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 13, Pp 4133-4144 (2018)
institution DOAJ
collection DOAJ
language EN
topic resveratrol
polymeric nanoparticles
galactosylation
oral bioavailability
anti-inflammation
Medicine (General)
R5-920
spellingShingle resveratrol
polymeric nanoparticles
galactosylation
oral bioavailability
anti-inflammation
Medicine (General)
R5-920
Siu FYK
Ye S
Lin H
Li S
Galactosylated PLGA nanoparticles for the oral delivery of resveratrol: enhanced bioavailability and in vitro anti-inflammatory activity
description Frederick YK Siu,1–3 Shaotang Ye,1–3 Hui Lin,1–3 Shoujun Li1–3 1College of Veterinary Medicine, South China Agricultural University, Guangzhou, People’s Republic of China; 2Guangdong Provincial Key Laboratory of Prevention and Control for Severe Clinical Animal Diseases, Guangzhou, People’s Republic of China; 3Guangdong Technological Engineering Research Center for Pet, Guangzhou, People’s Republic of China Background: Resveratrol (RES) is a natural anti-inflammatory and antioxidant compound with poor water solubility and oral bioavailability. The present study takes the advantages of nanocarriers combined with a ligand (galactose) anchoring to orally deliver RES in an attempt to improve its bioavailability and pharmacological activity. Methods: RES-loaded galactosylated nanoparticles (RES-GNPs) were prepared by solvent diffusion technique using poly(lactic-co-glycolic acid), synthesized N-oleoyl-d-galactosamine and Tween 80. RES-GNPs were characterized by particle size, morphology, entrapment efficiency (EE) and in vitro release. Oral bioavailability and in vitro anti-inflammatory activity were investigated in rats and lipopolysaccharides-induced RAW 264.7 cells, respectively. Results: The resulting RES-GNPs were 108.4 nm around in particle size with a polydispersity index of 0.217. Furthermore, RES-GNPs possessed a high EE and a slow drug release in water. After oral administration, RES-GNPs significantly enhanced the oral bioavailability of RES, up to 335.7% relative to RES suspensions. In situ single-pass intestinal perfusion and cellular uptake experiments showed that GNPs could improve the intestinal permeability and transcellular transport of RES. Moreover, the anti-inflammatory efficacy of RES-GNPs in RAW 264.7 cells model was superior to free RES and RES-GNPs. Conclusion: The results indicate that RES-GNPs can effectively promote the intestinal absorption of RES and strengthen its bioactivity, which may be a promising system for the treatment of inflammatory diseases. Keywords: resveratrol, polymeric nanoparticles, galactosylation, oral bioavailability, anti-inflammation
format article
author Siu FYK
Ye S
Lin H
Li S
author_facet Siu FYK
Ye S
Lin H
Li S
author_sort Siu FYK
title Galactosylated PLGA nanoparticles for the oral delivery of resveratrol: enhanced bioavailability and in vitro anti-inflammatory activity
title_short Galactosylated PLGA nanoparticles for the oral delivery of resveratrol: enhanced bioavailability and in vitro anti-inflammatory activity
title_full Galactosylated PLGA nanoparticles for the oral delivery of resveratrol: enhanced bioavailability and in vitro anti-inflammatory activity
title_fullStr Galactosylated PLGA nanoparticles for the oral delivery of resveratrol: enhanced bioavailability and in vitro anti-inflammatory activity
title_full_unstemmed Galactosylated PLGA nanoparticles for the oral delivery of resveratrol: enhanced bioavailability and in vitro anti-inflammatory activity
title_sort galactosylated plga nanoparticles for the oral delivery of resveratrol: enhanced bioavailability and in vitro anti-inflammatory activity
publisher Dove Medical Press
publishDate 2018
url https://doaj.org/article/afe0ebb3a3d24e0ba717d657e9140987
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AT yes galactosylatedplgananoparticlesfortheoraldeliveryofresveratrolenhancedbioavailabilityandinvitroantiinflammatoryactivity
AT linh galactosylatedplgananoparticlesfortheoraldeliveryofresveratrolenhancedbioavailabilityandinvitroantiinflammatoryactivity
AT lis galactosylatedplgananoparticlesfortheoraldeliveryofresveratrolenhancedbioavailabilityandinvitroantiinflammatoryactivity
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