Preparation and Characterization of Resveratrol Loaded Pectin/Alginate Blend Gastro-Resistant Microparticles

Background: The use of resveratrol as a dietary supplement is limited because it is easily oxidized and, after oral ingestion, it is metabolized into enterocytes and hepatocytes. Thus, new formulations are needed in order to improve its oral bioavailability. Objective: The objective of this study wa...

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Main Authors: Oihane Gartziandia, Arrate Lasa, Jose Luis Pedraz, Jonatan Miranda, Maria Puy Portillo, Manoli Igartua, Rosa Maria Hernández
Format: Article
Language:English
Published: MDPI AG 2018-07-01
Series:Molecules
Subjects:
Online Access:http://www.mdpi.com/1420-3049/23/8/1886
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spelling doaj-a0fb85a880004e25bebdf8daf7be3c802020-11-25T01:30:07ZengMDPI AGMolecules1420-30492018-07-01238188610.3390/molecules23081886molecules23081886Preparation and Characterization of Resveratrol Loaded Pectin/Alginate Blend Gastro-Resistant MicroparticlesOihane Gartziandia0Arrate Lasa1Jose Luis Pedraz2Jonatan Miranda3Maria Puy Portillo4Manoli Igartua5Rosa Maria Hernández6NanoBioCel Group, Laboratory of Pharmaceutics, School of Pharmacy, University of the Basque Country (UPV/EHU), Vitoria-Gasteiz 01006, SpainNutrition and Obesity Group, Department of Nutrition and Food Science, Faculty of Pharmacy and Lucio Lascaray Research Institute, University of País Vasco (UPV/EHU), Vitoria-Gasteiz 01006, SpainNanoBioCel Group, Laboratory of Pharmaceutics, School of Pharmacy, University of the Basque Country (UPV/EHU), Vitoria-Gasteiz 01006, SpainNutrition and Obesity Group, Department of Nutrition and Food Science, Faculty of Pharmacy and Lucio Lascaray Research Institute, University of País Vasco (UPV/EHU), Vitoria-Gasteiz 01006, SpainNutrition and Obesity Group, Department of Nutrition and Food Science, Faculty of Pharmacy and Lucio Lascaray Research Institute, University of País Vasco (UPV/EHU), Vitoria-Gasteiz 01006, SpainNanoBioCel Group, Laboratory of Pharmaceutics, School of Pharmacy, University of the Basque Country (UPV/EHU), Vitoria-Gasteiz 01006, SpainNanoBioCel Group, Laboratory of Pharmaceutics, School of Pharmacy, University of the Basque Country (UPV/EHU), Vitoria-Gasteiz 01006, SpainBackground: The use of resveratrol as a dietary supplement is limited because it is easily oxidized and, after oral ingestion, it is metabolized into enterocytes and hepatocytes. Thus, new formulations are needed in order to improve its oral bioavailability. Objective: The objective of this study was to develop and characterize a gastro-resistant formulation of resveratrol for oral administration as a dietary supplement. Method: Resveratrol was encapsulated in Eudragit-coated pectin-alginate microparticles. Results: The microparticle size was about 1450 µm, with an encapsulation efficiency of 41.72% ± 1.92%. The dissolution assay conducted, as specified in the European Pharmacopoeia for delayed-release dosage forms, revealed that our microparticles were gastro-resistant, because the resveratrol percentage released from microparticles in acid medium was less than 10%. In addition, the high-performance liquid chromatographic (HPLC) method developed for resveratrol content quantification in the microparticles was validated according to International Council for Harmonisation (ICH) Q2 (R1) guidelines. Finally, the biological activity of resveratrol was investigated in 3T3-L1 mature adipocytes, concluding that the encapsulation process does not affect the activity of resveratrol. Conclusion: In summary, the gastro-resistant microparticles developed could represent a suitable method of including resveratrol in dietary supplements and in functional foods used in obesity therapy.http://www.mdpi.com/1420-3049/23/8/1886resveratroldietary supplementgastro-resistantmicroparticlesobesityHPLC
collection DOAJ
language English
format Article
sources DOAJ
author Oihane Gartziandia
Arrate Lasa
Jose Luis Pedraz
Jonatan Miranda
Maria Puy Portillo
Manoli Igartua
Rosa Maria Hernández
spellingShingle Oihane Gartziandia
Arrate Lasa
Jose Luis Pedraz
Jonatan Miranda
Maria Puy Portillo
Manoli Igartua
Rosa Maria Hernández
Preparation and Characterization of Resveratrol Loaded Pectin/Alginate Blend Gastro-Resistant Microparticles
Molecules
resveratrol
dietary supplement
gastro-resistant
microparticles
obesity
HPLC
author_facet Oihane Gartziandia
Arrate Lasa
Jose Luis Pedraz
Jonatan Miranda
Maria Puy Portillo
Manoli Igartua
Rosa Maria Hernández
author_sort Oihane Gartziandia
title Preparation and Characterization of Resveratrol Loaded Pectin/Alginate Blend Gastro-Resistant Microparticles
title_short Preparation and Characterization of Resveratrol Loaded Pectin/Alginate Blend Gastro-Resistant Microparticles
title_full Preparation and Characterization of Resveratrol Loaded Pectin/Alginate Blend Gastro-Resistant Microparticles
title_fullStr Preparation and Characterization of Resveratrol Loaded Pectin/Alginate Blend Gastro-Resistant Microparticles
title_full_unstemmed Preparation and Characterization of Resveratrol Loaded Pectin/Alginate Blend Gastro-Resistant Microparticles
title_sort preparation and characterization of resveratrol loaded pectin/alginate blend gastro-resistant microparticles
publisher MDPI AG
series Molecules
issn 1420-3049
publishDate 2018-07-01
description Background: The use of resveratrol as a dietary supplement is limited because it is easily oxidized and, after oral ingestion, it is metabolized into enterocytes and hepatocytes. Thus, new formulations are needed in order to improve its oral bioavailability. Objective: The objective of this study was to develop and characterize a gastro-resistant formulation of resveratrol for oral administration as a dietary supplement. Method: Resveratrol was encapsulated in Eudragit-coated pectin-alginate microparticles. Results: The microparticle size was about 1450 µm, with an encapsulation efficiency of 41.72% ± 1.92%. The dissolution assay conducted, as specified in the European Pharmacopoeia for delayed-release dosage forms, revealed that our microparticles were gastro-resistant, because the resveratrol percentage released from microparticles in acid medium was less than 10%. In addition, the high-performance liquid chromatographic (HPLC) method developed for resveratrol content quantification in the microparticles was validated according to International Council for Harmonisation (ICH) Q2 (R1) guidelines. Finally, the biological activity of resveratrol was investigated in 3T3-L1 mature adipocytes, concluding that the encapsulation process does not affect the activity of resveratrol. Conclusion: In summary, the gastro-resistant microparticles developed could represent a suitable method of including resveratrol in dietary supplements and in functional foods used in obesity therapy.
topic resveratrol
dietary supplement
gastro-resistant
microparticles
obesity
HPLC
url http://www.mdpi.com/1420-3049/23/8/1886
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