Study on the Pulmonary Delivery System of Apigenin-Loaded Albumin Nanocarriers with Antioxidant Activity
Respiratory diseases are mainly derived from acute and chronic inflammation of the alveoli and bronchi. The pathophysiological mechanisms of pulmonary inflammation mainly arise from oxidative damage that could ultimately lead to acute lung injury. Apigenin (Api) is a natural polyphenol with prominen...
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| Veröffentlicht in: | Journal of aerosol medicine 2017-08, Vol.30 (4), p.274-288 |
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| creator | Pápay, Zsófia Edit Kósa, Annamária Böddi, Béla Merchant, Zahra Saleem, Imran Y Zariwala, Mohammed Gulrez Klebovich, Imre Somavarapu, Satyanarayana Antal, István |
| description | Respiratory diseases are mainly derived from acute and chronic inflammation of the alveoli and bronchi. The pathophysiological mechanisms of pulmonary inflammation mainly arise from oxidative damage that could ultimately lead to acute lung injury. Apigenin (Api) is a natural polyphenol with prominent antioxidant and anti-inflammatory properties in the lung. Inhalable formulations that consist of nanoparticles (NPs) have several advantages over other administration routes, and therefore, this study investigated the application of apigenin-loaded bovine serum albumin nanoparticles (BSA-Api-NPs) for pulmonary delivery.
Dry powder formulations of BSA-Api-NPs were prepared by spray drying and characterized by laser diffraction particle sizing, scanning electron microscopy, differential scanning calorimetry, and powder X-ray diffraction. The influence of dispersibility enhancers (lactose monohydrate and l-leucine) on the in vitro aerosol deposition using a next-generation impactor was investigated in comparison to excipient-free formulation. The dissolution of Api was determined in simulated lung fluid by using the Franz cell apparatus. The antioxidant activity was determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH
) free radical scavenging assay.
The encapsulation efficiency and the drug loading were measured to be 82.61% ± 4.56% and 7.51% ± 0.415%. The optimized spray drying conditions were suitable to produce particles with low residual moisture content. The spray-dried BSA-Api-NPs possessed good aerodynamic properties due to small and wrinkled particles with low mass median aerodynamic diameter, high emitted dose, and fine particle fraction. The aerodynamic properties were enhanced by leucine and decreased by lactose, however, the dissolution was reversely affected. The DPPH
assay confirmed that the antioxidant activity of encapsulated Api was preserved.
This study provides evidence to support that albumin nanoparticles are suitable carriers of Api and the use of traditional or novel excipients should be taken into consideration. The developed BSA-Api-NPs are a novel delivery system against lung injury with potential antioxidant activity. |
| doi_str_mv | 10.1089/jamp.2016.1316 |
| format | Article |
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Dry powder formulations of BSA-Api-NPs were prepared by spray drying and characterized by laser diffraction particle sizing, scanning electron microscopy, differential scanning calorimetry, and powder X-ray diffraction. The influence of dispersibility enhancers (lactose monohydrate and l-leucine) on the in vitro aerosol deposition using a next-generation impactor was investigated in comparison to excipient-free formulation. The dissolution of Api was determined in simulated lung fluid by using the Franz cell apparatus. The antioxidant activity was determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH
) free radical scavenging assay.
The encapsulation efficiency and the drug loading were measured to be 82.61% ± 4.56% and 7.51% ± 0.415%. The optimized spray drying conditions were suitable to produce particles with low residual moisture content. The spray-dried BSA-Api-NPs possessed good aerodynamic properties due to small and wrinkled particles with low mass median aerodynamic diameter, high emitted dose, and fine particle fraction. The aerodynamic properties were enhanced by leucine and decreased by lactose, however, the dissolution was reversely affected. The DPPH
assay confirmed that the antioxidant activity of encapsulated Api was preserved.
This study provides evidence to support that albumin nanoparticles are suitable carriers of Api and the use of traditional or novel excipients should be taken into consideration. The developed BSA-Api-NPs are a novel delivery system against lung injury with potential antioxidant activity.</description><identifier>ISSN: 1941-2711</identifier><identifier>EISSN: 1941-2703</identifier><identifier>DOI: 10.1089/jamp.2016.1316</identifier><identifier>PMID: 28282259</identifier><language>eng</language><publisher>United States: Mary Ann Liebert, Inc</publisher><subject>Administration, Inhalation ; Aerodynamic properties ; Aerosols ; Albumins - chemistry ; Alveoli ; Anti-inflammatory agents ; Antioxidants ; Antioxidants - administration & dosage ; Antioxidants - pharmacokinetics ; Antioxidants - pharmacology ; Apigenin - administration & dosage ; Apigenin - pharmacokinetics ; Apigenin - pharmacology ; Bovine serum albumin ; Bronchi ; Bronchus ; Calorimetry ; Calorimetry, Differential Scanning ; Chemistry, Pharmaceutical - methods ; Differential scanning calorimetry ; Diffraction ; Dispersions ; Dissolution ; Drug Carriers - chemistry ; Drug Compounding - methods ; Drug Delivery Systems ; Drug dosages ; Drug Liberation ; Drying ; Electron microscopy ; Encapsulation ; Enhancers ; Excipients ; Excipients - chemistry ; Food ; Formulations ; Free Radical Scavengers - administration & dosage ; Free Radical Scavengers - pharmacokinetics ; Free Radical Scavengers - pharmacology ; Free radicals ; Health technology assessment ; Heat measurement ; Inflammation ; Lactose ; Leucine ; Lung - metabolism ; Lungs ; Microscopy ; Microscopy, Electron, Scanning ; Moisture content ; Morphology ; Nanoparticles ; Oxidative stress ; Particle Size ; Particulates ; Permeability ; Pharmaceutical sciences ; Pharmacy ; Powder ; Respiratory diseases ; Scanning electron microscopy ; X-Ray Diffraction</subject><ispartof>Journal of aerosol medicine, 2017-08, Vol.30 (4), p.274-288</ispartof><rights>(©) Copyright 2017, Mary Ann Liebert, Inc.</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c363t-ae2d6734f6ef384c307815c8e0a0d6dcc4882ad81cd0b15389eb58c90b1487783</citedby><cites>FETCH-LOGICAL-c363t-ae2d6734f6ef384c307815c8e0a0d6dcc4882ad81cd0b15389eb58c90b1487783</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>315,781,785,27929,27930</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/28282259$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Pápay, Zsófia Edit</creatorcontrib><creatorcontrib>Kósa, Annamária</creatorcontrib><creatorcontrib>Böddi, Béla</creatorcontrib><creatorcontrib>Merchant, Zahra</creatorcontrib><creatorcontrib>Saleem, Imran Y</creatorcontrib><creatorcontrib>Zariwala, Mohammed Gulrez</creatorcontrib><creatorcontrib>Klebovich, Imre</creatorcontrib><creatorcontrib>Somavarapu, Satyanarayana</creatorcontrib><creatorcontrib>Antal, István</creatorcontrib><title>Study on the Pulmonary Delivery System of Apigenin-Loaded Albumin Nanocarriers with Antioxidant Activity</title><title>Journal of aerosol medicine</title><addtitle>J Aerosol Med Pulm Drug Deliv</addtitle><description>Respiratory diseases are mainly derived from acute and chronic inflammation of the alveoli and bronchi. The pathophysiological mechanisms of pulmonary inflammation mainly arise from oxidative damage that could ultimately lead to acute lung injury. Apigenin (Api) is a natural polyphenol with prominent antioxidant and anti-inflammatory properties in the lung. Inhalable formulations that consist of nanoparticles (NPs) have several advantages over other administration routes, and therefore, this study investigated the application of apigenin-loaded bovine serum albumin nanoparticles (BSA-Api-NPs) for pulmonary delivery.
Dry powder formulations of BSA-Api-NPs were prepared by spray drying and characterized by laser diffraction particle sizing, scanning electron microscopy, differential scanning calorimetry, and powder X-ray diffraction. The influence of dispersibility enhancers (lactose monohydrate and l-leucine) on the in vitro aerosol deposition using a next-generation impactor was investigated in comparison to excipient-free formulation. The dissolution of Api was determined in simulated lung fluid by using the Franz cell apparatus. The antioxidant activity was determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH
) free radical scavenging assay.
The encapsulation efficiency and the drug loading were measured to be 82.61% ± 4.56% and 7.51% ± 0.415%. The optimized spray drying conditions were suitable to produce particles with low residual moisture content. The spray-dried BSA-Api-NPs possessed good aerodynamic properties due to small and wrinkled particles with low mass median aerodynamic diameter, high emitted dose, and fine particle fraction. The aerodynamic properties were enhanced by leucine and decreased by lactose, however, the dissolution was reversely affected. The DPPH
assay confirmed that the antioxidant activity of encapsulated Api was preserved.
This study provides evidence to support that albumin nanoparticles are suitable carriers of Api and the use of traditional or novel excipients should be taken into consideration. The developed BSA-Api-NPs are a novel delivery system against lung injury with potential antioxidant activity.</description><subject>Administration, Inhalation</subject><subject>Aerodynamic properties</subject><subject>Aerosols</subject><subject>Albumins - chemistry</subject><subject>Alveoli</subject><subject>Anti-inflammatory agents</subject><subject>Antioxidants</subject><subject>Antioxidants - administration & dosage</subject><subject>Antioxidants - pharmacokinetics</subject><subject>Antioxidants - pharmacology</subject><subject>Apigenin - administration & dosage</subject><subject>Apigenin - pharmacokinetics</subject><subject>Apigenin - pharmacology</subject><subject>Bovine serum albumin</subject><subject>Bronchi</subject><subject>Bronchus</subject><subject>Calorimetry</subject><subject>Calorimetry, Differential Scanning</subject><subject>Chemistry, Pharmaceutical - methods</subject><subject>Differential scanning calorimetry</subject><subject>Diffraction</subject><subject>Dispersions</subject><subject>Dissolution</subject><subject>Drug Carriers - chemistry</subject><subject>Drug Compounding - methods</subject><subject>Drug Delivery Systems</subject><subject>Drug dosages</subject><subject>Drug Liberation</subject><subject>Drying</subject><subject>Electron microscopy</subject><subject>Encapsulation</subject><subject>Enhancers</subject><subject>Excipients</subject><subject>Excipients - chemistry</subject><subject>Food</subject><subject>Formulations</subject><subject>Free Radical Scavengers - administration & dosage</subject><subject>Free Radical Scavengers - pharmacokinetics</subject><subject>Free Radical Scavengers - pharmacology</subject><subject>Free radicals</subject><subject>Health technology assessment</subject><subject>Heat measurement</subject><subject>Inflammation</subject><subject>Lactose</subject><subject>Leucine</subject><subject>Lung - metabolism</subject><subject>Lungs</subject><subject>Microscopy</subject><subject>Microscopy, Electron, Scanning</subject><subject>Moisture content</subject><subject>Morphology</subject><subject>Nanoparticles</subject><subject>Oxidative stress</subject><subject>Particle Size</subject><subject>Particulates</subject><subject>Permeability</subject><subject>Pharmaceutical sciences</subject><subject>Pharmacy</subject><subject>Powder</subject><subject>Respiratory diseases</subject><subject>Scanning electron microscopy</subject><subject>X-Ray Diffraction</subject><issn>1941-2711</issn><issn>1941-2703</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><recordid>eNpdkc1r3DAQxUVJadKk1xyDIJdevNVIXlk-miT9gKUtJD0LrTTOarGljSRvu_99vSTNocxh3sBvhuE9Qi6BLYCp9tPWjLsFZyAXIEC-IWfQ1lDxhomTVw1wSt7nvGVMQi3FO3LK1Vx82Z6RzX2Z3IHGQMsG6c9pGGMw6UBvcfB7nMX9IRccaexpt_OPGHyoVtE4dLQb1tPoA_1uQrQmJY8p09--bGgXio9_vDOh0M4Wv_flcEHe9mbI-OGln5Nfn-8ebr5Wqx9fvt10q8oKKUplkDvZiLqX2AtVW8EaBUurkBnmpLO2Voobp8A6toalUC2ul8q281CrplHinHx8vrtL8WnCXPTos8VhMAHjlDWoRtatVA2f0ev_0G2cUpi_09DymnEQjZipxTNlU8w5Ya93yY-zRxqYPmagjxnoYwb6mMG8cPVydlqP6F7xf6aLvzzwgrk</recordid><startdate>201708</startdate><enddate>201708</enddate><creator>Pápay, Zsófia Edit</creator><creator>Kósa, Annamária</creator><creator>Böddi, Béla</creator><creator>Merchant, Zahra</creator><creator>Saleem, Imran Y</creator><creator>Zariwala, Mohammed Gulrez</creator><creator>Klebovich, Imre</creator><creator>Somavarapu, Satyanarayana</creator><creator>Antal, István</creator><general>Mary Ann Liebert, Inc</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>3V.</scope><scope>7T5</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>BENPR</scope><scope>CCPQU</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>H94</scope><scope>K9.</scope><scope>M0S</scope><scope>M1P</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>7X8</scope></search><sort><creationdate>201708</creationdate><title>Study on the Pulmonary Delivery System of Apigenin-Loaded Albumin Nanocarriers with Antioxidant Activity</title><author>Pápay, Zsófia Edit ; Kósa, Annamária ; Böddi, Béla ; Merchant, Zahra ; Saleem, Imran Y ; Zariwala, Mohammed Gulrez ; Klebovich, Imre ; Somavarapu, Satyanarayana ; Antal, István</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c363t-ae2d6734f6ef384c307815c8e0a0d6dcc4882ad81cd0b15389eb58c90b1487783</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2017</creationdate><topic>Administration, Inhalation</topic><topic>Aerodynamic properties</topic><topic>Aerosols</topic><topic>Albumins - chemistry</topic><topic>Alveoli</topic><topic>Anti-inflammatory agents</topic><topic>Antioxidants</topic><topic>Antioxidants - administration & dosage</topic><topic>Antioxidants - pharmacokinetics</topic><topic>Antioxidants - pharmacology</topic><topic>Apigenin - administration & dosage</topic><topic>Apigenin - pharmacokinetics</topic><topic>Apigenin - pharmacology</topic><topic>Bovine serum albumin</topic><topic>Bronchi</topic><topic>Bronchus</topic><topic>Calorimetry</topic><topic>Calorimetry, Differential Scanning</topic><topic>Chemistry, Pharmaceutical - methods</topic><topic>Differential scanning calorimetry</topic><topic>Diffraction</topic><topic>Dispersions</topic><topic>Dissolution</topic><topic>Drug Carriers - chemistry</topic><topic>Drug Compounding - methods</topic><topic>Drug Delivery Systems</topic><topic>Drug dosages</topic><topic>Drug Liberation</topic><topic>Drying</topic><topic>Electron microscopy</topic><topic>Encapsulation</topic><topic>Enhancers</topic><topic>Excipients</topic><topic>Excipients - chemistry</topic><topic>Food</topic><topic>Formulations</topic><topic>Free Radical Scavengers - administration & dosage</topic><topic>Free Radical Scavengers - pharmacokinetics</topic><topic>Free Radical Scavengers - pharmacology</topic><topic>Free radicals</topic><topic>Health technology assessment</topic><topic>Heat measurement</topic><topic>Inflammation</topic><topic>Lactose</topic><topic>Leucine</topic><topic>Lung - metabolism</topic><topic>Lungs</topic><topic>Microscopy</topic><topic>Microscopy, Electron, Scanning</topic><topic>Moisture content</topic><topic>Morphology</topic><topic>Nanoparticles</topic><topic>Oxidative stress</topic><topic>Particle Size</topic><topic>Particulates</topic><topic>Permeability</topic><topic>Pharmaceutical sciences</topic><topic>Pharmacy</topic><topic>Powder</topic><topic>Respiratory diseases</topic><topic>Scanning electron microscopy</topic><topic>X-Ray Diffraction</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Pápay, Zsófia Edit</creatorcontrib><creatorcontrib>Kósa, Annamária</creatorcontrib><creatorcontrib>Böddi, Béla</creatorcontrib><creatorcontrib>Merchant, Zahra</creatorcontrib><creatorcontrib>Saleem, Imran Y</creatorcontrib><creatorcontrib>Zariwala, Mohammed Gulrez</creatorcontrib><creatorcontrib>Klebovich, Imre</creatorcontrib><creatorcontrib>Somavarapu, Satyanarayana</creatorcontrib><creatorcontrib>Antal, István</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>ProQuest Central (Corporate)</collection><collection>Immunology Abstracts</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Medical Database (Alumni Edition)</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central</collection><collection>ProQuest One Community College</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of aerosol medicine</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Pápay, Zsófia Edit</au><au>Kósa, Annamária</au><au>Böddi, Béla</au><au>Merchant, Zahra</au><au>Saleem, Imran Y</au><au>Zariwala, Mohammed Gulrez</au><au>Klebovich, Imre</au><au>Somavarapu, Satyanarayana</au><au>Antal, István</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Study on the Pulmonary Delivery System of Apigenin-Loaded Albumin Nanocarriers with Antioxidant Activity</atitle><jtitle>Journal of aerosol medicine</jtitle><addtitle>J Aerosol Med Pulm Drug Deliv</addtitle><date>2017-08</date><risdate>2017</risdate><volume>30</volume><issue>4</issue><spage>274</spage><epage>288</epage><pages>274-288</pages><issn>1941-2711</issn><eissn>1941-2703</eissn><abstract>Respiratory diseases are mainly derived from acute and chronic inflammation of the alveoli and bronchi. The pathophysiological mechanisms of pulmonary inflammation mainly arise from oxidative damage that could ultimately lead to acute lung injury. Apigenin (Api) is a natural polyphenol with prominent antioxidant and anti-inflammatory properties in the lung. Inhalable formulations that consist of nanoparticles (NPs) have several advantages over other administration routes, and therefore, this study investigated the application of apigenin-loaded bovine serum albumin nanoparticles (BSA-Api-NPs) for pulmonary delivery.
Dry powder formulations of BSA-Api-NPs were prepared by spray drying and characterized by laser diffraction particle sizing, scanning electron microscopy, differential scanning calorimetry, and powder X-ray diffraction. The influence of dispersibility enhancers (lactose monohydrate and l-leucine) on the in vitro aerosol deposition using a next-generation impactor was investigated in comparison to excipient-free formulation. The dissolution of Api was determined in simulated lung fluid by using the Franz cell apparatus. The antioxidant activity was determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH
) free radical scavenging assay.
The encapsulation efficiency and the drug loading were measured to be 82.61% ± 4.56% and 7.51% ± 0.415%. The optimized spray drying conditions were suitable to produce particles with low residual moisture content. The spray-dried BSA-Api-NPs possessed good aerodynamic properties due to small and wrinkled particles with low mass median aerodynamic diameter, high emitted dose, and fine particle fraction. The aerodynamic properties were enhanced by leucine and decreased by lactose, however, the dissolution was reversely affected. The DPPH
assay confirmed that the antioxidant activity of encapsulated Api was preserved.
This study provides evidence to support that albumin nanoparticles are suitable carriers of Api and the use of traditional or novel excipients should be taken into consideration. The developed BSA-Api-NPs are a novel delivery system against lung injury with potential antioxidant activity.</abstract><cop>United States</cop><pub>Mary Ann Liebert, Inc</pub><pmid>28282259</pmid><doi>10.1089/jamp.2016.1316</doi><tpages>15</tpages><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
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| ispartof | Journal of aerosol medicine, 2017-08, Vol.30 (4), p.274-288 |
| issn | 1941-2711 1941-2703 |
| language | eng |
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| source | MEDLINE; Alma/SFX Local Collection |
| subjects | Administration, Inhalation Aerodynamic properties Aerosols Albumins - chemistry Alveoli Anti-inflammatory agents Antioxidants Antioxidants - administration & dosage Antioxidants - pharmacokinetics Antioxidants - pharmacology Apigenin - administration & dosage Apigenin - pharmacokinetics Apigenin - pharmacology Bovine serum albumin Bronchi Bronchus Calorimetry Calorimetry, Differential Scanning Chemistry, Pharmaceutical - methods Differential scanning calorimetry Diffraction Dispersions Dissolution Drug Carriers - chemistry Drug Compounding - methods Drug Delivery Systems Drug dosages Drug Liberation Drying Electron microscopy Encapsulation Enhancers Excipients Excipients - chemistry Food Formulations Free Radical Scavengers - administration & dosage Free Radical Scavengers - pharmacokinetics Free Radical Scavengers - pharmacology Free radicals Health technology assessment Heat measurement Inflammation Lactose Leucine Lung - metabolism Lungs Microscopy Microscopy, Electron, Scanning Moisture content Morphology Nanoparticles Oxidative stress Particle Size Particulates Permeability Pharmaceutical sciences Pharmacy Powder Respiratory diseases Scanning electron microscopy X-Ray Diffraction |
| title | Study on the Pulmonary Delivery System of Apigenin-Loaded Albumin Nanocarriers with Antioxidant Activity |
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