Effects of polymer molecular weight on relative oral bioavailability of curcumin

Yin-Meng Tsai,1 Wan-Ling Chang-Liao,1 Chao-Feng Chien,1 Lie-Chwen Lin,1,2 Tung-Hu Tsai,1,31Institute of Traditional Medicine, School of Medicine, National Yang-Ming University, 2National Research Institute of Chinese Medicine, 3Department of Education and Research, Taipei City Hospital, Taipei, Taiw...

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Autores principales:	Lin LC, Chien CF, Chang-Liao WL, Tsai YM, Tsai TH
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/b76beadee5a0416a93d191f9c715dc74
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spelling	oai:doaj.org-article:b76beadee5a0416a93d191f9c715dc742021-12-02T06:34:20ZEffects of polymer molecular weight on relative oral bioavailability of curcumin1176-91141178-2013https://doaj.org/article/b76beadee5a0416a93d191f9c715dc742012-06-01T00:00:00Zhttp://www.dovepress.com/effects-of-polymer-molecular-weight-on-relative-oral-bioavailability-o-a10126https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Yin-Meng Tsai,1 Wan-Ling Chang-Liao,1 Chao-Feng Chien,1 Lie-Chwen Lin,1,2 Tung-Hu Tsai,1,31Institute of Traditional Medicine, School of Medicine, National Yang-Ming University, 2National Research Institute of Chinese Medicine, 3Department of Education and Research, Taipei City Hospital, Taipei, TaiwanBackground: Polylactic-co-glycolic acid (PLGA) nanoparticles have been used to increase the relative oral bioavailability of hydrophobic compounds and polyphenols in recent years, but the effects of the molecular weight of PLGA on bioavailability are still unknown. This study investigated the influence of polymer molecular weight on the relative oral bioavailability of curcumin, and explored the possible mechanism accounting for the outcome.Methods: Curcumin encapsulated in low (5000&ndash;15,000) and high (40,000&ndash;75,000) molecular weight PLGA (LMw-NPC and HMw-NPC, respectively) were prepared using an emulsification-solvent evaporation method. Curcumin alone and in the nanoformulations was administered orally to freely mobile rats, and blood samples were collected to evaluate the bioavailability of curcumin, LMw-NPC, and HMw-NPC. An ex vivo experimental gut absorption model was used to investigate the effects of different molecular weights of PLGA formulation on absorption of curcumin. High-performance liquid chromatography with diode array detection was used for quantification of curcumin in biosamples.Results: There were no significant differences in particle properties between LMw-NPC and HMw-NPC, but the relative bioavailability of HMw-NPC was 1.67-fold and 40-fold higher than that of LMw-NPC and conventional curcumin, respectively. In addition, the mean peak concentration (Cmax) of conventional curcumin, LMw-NPC, and HMw-NPC was 0.028, 0.042, and 0.057 &micro;g/mL, respectively. The gut absorption study further revealed that the HMw-PLGA formulation markedly increased the absorption rate of curcumin in the duodenum and resulted in excellent bioavailability compared with conventional curcumin and LMw-NPC.Conclusion: Our findings demonstrate that different molecular weights of PLGA have varying bioavailability, contributing to changes in the absorption rate at the duodenum. The results of this study provide the rationale for design of a nanomedicine delivery system to enhance the bioavailability of water-insoluble pharmaceutical compounds and functional foods.Keywords: absorption, duodenum, molecular weight, poly(lactic-co-glycolic acid), PLGA, relative oral bioavailabilityLin LCChien CFChang-Liao WLTsai YMTsai THDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 2957-2966 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Lin LC Chien CF Chang-Liao WL Tsai YM Tsai TH Effects of polymer molecular weight on relative oral bioavailability of curcumin
description	Yin-Meng Tsai,1 Wan-Ling Chang-Liao,1 Chao-Feng Chien,1 Lie-Chwen Lin,1,2 Tung-Hu Tsai,1,31Institute of Traditional Medicine, School of Medicine, National Yang-Ming University, 2National Research Institute of Chinese Medicine, 3Department of Education and Research, Taipei City Hospital, Taipei, TaiwanBackground: Polylactic-co-glycolic acid (PLGA) nanoparticles have been used to increase the relative oral bioavailability of hydrophobic compounds and polyphenols in recent years, but the effects of the molecular weight of PLGA on bioavailability are still unknown. This study investigated the influence of polymer molecular weight on the relative oral bioavailability of curcumin, and explored the possible mechanism accounting for the outcome.Methods: Curcumin encapsulated in low (5000&ndash;15,000) and high (40,000&ndash;75,000) molecular weight PLGA (LMw-NPC and HMw-NPC, respectively) were prepared using an emulsification-solvent evaporation method. Curcumin alone and in the nanoformulations was administered orally to freely mobile rats, and blood samples were collected to evaluate the bioavailability of curcumin, LMw-NPC, and HMw-NPC. An ex vivo experimental gut absorption model was used to investigate the effects of different molecular weights of PLGA formulation on absorption of curcumin. High-performance liquid chromatography with diode array detection was used for quantification of curcumin in biosamples.Results: There were no significant differences in particle properties between LMw-NPC and HMw-NPC, but the relative bioavailability of HMw-NPC was 1.67-fold and 40-fold higher than that of LMw-NPC and conventional curcumin, respectively. In addition, the mean peak concentration (Cmax) of conventional curcumin, LMw-NPC, and HMw-NPC was 0.028, 0.042, and 0.057 &micro;g/mL, respectively. The gut absorption study further revealed that the HMw-PLGA formulation markedly increased the absorption rate of curcumin in the duodenum and resulted in excellent bioavailability compared with conventional curcumin and LMw-NPC.Conclusion: Our findings demonstrate that different molecular weights of PLGA have varying bioavailability, contributing to changes in the absorption rate at the duodenum. The results of this study provide the rationale for design of a nanomedicine delivery system to enhance the bioavailability of water-insoluble pharmaceutical compounds and functional foods.Keywords: absorption, duodenum, molecular weight, poly(lactic-co-glycolic acid), PLGA, relative oral bioavailability
format	article
author	Lin LC Chien CF Chang-Liao WL Tsai YM Tsai TH
author_facet	Lin LC Chien CF Chang-Liao WL Tsai YM Tsai TH
author_sort	Lin LC
title	Effects of polymer molecular weight on relative oral bioavailability of curcumin
title_short	Effects of polymer molecular weight on relative oral bioavailability of curcumin
title_full	Effects of polymer molecular weight on relative oral bioavailability of curcumin
title_fullStr	Effects of polymer molecular weight on relative oral bioavailability of curcumin
title_full_unstemmed	Effects of polymer molecular weight on relative oral bioavailability of curcumin
title_sort	effects of polymer molecular weight on relative oral bioavailability of curcumin
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/b76beadee5a0416a93d191f9c715dc74
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_version_	1718399835011284992

Effects of polymer molecular weight on relative oral bioavailability of curcumin

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