Celecoxib-loaded PLGA/cyclodextrin microspheres: Characterization and evaluation of anti-inflammatory activity on human chondrocyte cultures
•Celecoxib loaded-PLGA/dimethyl-β-cyclodextrin microspheres were prepared.•Dimethyl-β-cyclodextrin improves technological parameters of PLGA microspheres and modulates the release of celecoxib from the microspheres.•Celecoxib loaded-PLGA/dimethyl-β-cyclodextrin microspheres was more effective than t...
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| Veröffentlicht in: | Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2013-11, Vol.111, p.289-296 |
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| creator | Cannavà, Carmela Tommasini, Silvana Stancanelli, Rosanna Cardile, Venera Cilurzo, Felisa Giannone, Ignazio Puglisi, Giovanni Ventura, Cinzia Anna |
| description | •Celecoxib loaded-PLGA/dimethyl-β-cyclodextrin microspheres were prepared.•Dimethyl-β-cyclodextrin improves technological parameters of PLGA microspheres and modulates the release of celecoxib from the microspheres.•Celecoxib loaded-PLGA/dimethyl-β-cyclodextrin microspheres was more effective than the free drug as an anti-inflammatory agent on human chondrocyte cultures.•PLGA/dimethyl-β-cyclodextrin microspheres show good potentiality as delivery systems for the intra-articular administration of CCB.
PLGA microspheres were prepared as a sustained release system for the intra-articular administration of celecoxib (CCB). The microspheres were prepared in the presence of different concentrations of dimethyl-β-cyclodextrin (DM-β-Cyd), by the simple oil-in-water emulsion/evaporation solvent method. The microspheres were evaluated as to surface morphology, size and technological properties (such as encapsulation efficiency, drug loading capacity and drug release). Ex vivo studies on cultures of human chondrocytes were performed in order to evaluate the influence of the polymeric carriers on the pharmacological activity of CCB. All systems ranged from about 1 to 5μm in size and had a high encapsulation efficiency percentage ranging from about 80% to 90% (w/w), except for CCB-loaded-PLGA microspheres containing the highest amount of DM-β-Cyd, in which a dramatic drop in the encapsulation efficiency was observed (about 54%, w/w). FIB images evidenced the fact that the microspheres had a porous structure in the presence of the highest amount of DM-β-Cyd. The macrocycle modulated the release profiles of CCB from the microspheres, producing in some cases a zero-order kinetic release. Ex vivo biological studies demonstrated that DM-β-Cyd improved the drug's anti-inflammatory activity. Thus, CCB-loaded PLGA/cyclodextrin microspheres may have a potential therapeutic application in the treatment of osteo- and rheumatoid arthritis. |
| doi_str_mv | 10.1016/j.colsurfb.2013.06.015 |
| format | Article |
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PLGA microspheres were prepared as a sustained release system for the intra-articular administration of celecoxib (CCB). The microspheres were prepared in the presence of different concentrations of dimethyl-β-cyclodextrin (DM-β-Cyd), by the simple oil-in-water emulsion/evaporation solvent method. The microspheres were evaluated as to surface morphology, size and technological properties (such as encapsulation efficiency, drug loading capacity and drug release). Ex vivo studies on cultures of human chondrocytes were performed in order to evaluate the influence of the polymeric carriers on the pharmacological activity of CCB. All systems ranged from about 1 to 5μm in size and had a high encapsulation efficiency percentage ranging from about 80% to 90% (w/w), except for CCB-loaded-PLGA microspheres containing the highest amount of DM-β-Cyd, in which a dramatic drop in the encapsulation efficiency was observed (about 54%, w/w). FIB images evidenced the fact that the microspheres had a porous structure in the presence of the highest amount of DM-β-Cyd. The macrocycle modulated the release profiles of CCB from the microspheres, producing in some cases a zero-order kinetic release. Ex vivo biological studies demonstrated that DM-β-Cyd improved the drug's anti-inflammatory activity. Thus, CCB-loaded PLGA/cyclodextrin microspheres may have a potential therapeutic application in the treatment of osteo- and rheumatoid arthritis.</description><identifier>ISSN: 0927-7765</identifier><identifier>EISSN: 1873-4367</identifier><identifier>DOI: 10.1016/j.colsurfb.2013.06.015</identifier><identifier>PMID: 23838195</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>anti-inflammatory activity ; Anti-Inflammatory Agents - pharmacology ; Calorimetry, Differential Scanning ; Celecoxib ; Cells, Cultured ; Chondrocyte cultures ; chondrocytes ; Chondrocytes - cytology ; Chondrocytes - drug effects ; Circular Dichroism ; colloids ; Culture ; Cyclodextrins ; Cyclodextrins - chemistry ; Diclofenac - pharmacology ; Diffusion ; Dimethyl-β-cyclodextrin ; Drug delivery systems ; Drugs ; emulsions ; Encapsulation ; evaporation ; Human ; Humans ; Lactic Acid - chemistry ; Microspheres ; PLGA microspheres ; Polyglycolic Acid - chemistry ; Pyrazoles - pharmacology ; Release kinetics ; rheumatoid arthritis ; solvents ; Sulfonamides - pharmacology ; Surface chemistry</subject><ispartof>Colloids and surfaces, B, Biointerfaces, 2013-11, Vol.111, p.289-296</ispartof><rights>2013 Elsevier B.V.</rights><rights>Copyright © 2013 Elsevier B.V. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c458t-132d2e58895700a62a1b2518e6a1469d84ddc097433664f18c7441e7adfad9003</citedby><cites>FETCH-LOGICAL-c458t-132d2e58895700a62a1b2518e6a1469d84ddc097433664f18c7441e7adfad9003</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.colsurfb.2013.06.015$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/23838195$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Cannavà, Carmela</creatorcontrib><creatorcontrib>Tommasini, Silvana</creatorcontrib><creatorcontrib>Stancanelli, Rosanna</creatorcontrib><creatorcontrib>Cardile, Venera</creatorcontrib><creatorcontrib>Cilurzo, Felisa</creatorcontrib><creatorcontrib>Giannone, Ignazio</creatorcontrib><creatorcontrib>Puglisi, Giovanni</creatorcontrib><creatorcontrib>Ventura, Cinzia Anna</creatorcontrib><title>Celecoxib-loaded PLGA/cyclodextrin microspheres: Characterization and evaluation of anti-inflammatory activity on human chondrocyte cultures</title><title>Colloids and surfaces, B, Biointerfaces</title><addtitle>Colloids Surf B Biointerfaces</addtitle><description>•Celecoxib loaded-PLGA/dimethyl-β-cyclodextrin microspheres were prepared.•Dimethyl-β-cyclodextrin improves technological parameters of PLGA microspheres and modulates the release of celecoxib from the microspheres.•Celecoxib loaded-PLGA/dimethyl-β-cyclodextrin microspheres was more effective than the free drug as an anti-inflammatory agent on human chondrocyte cultures.•PLGA/dimethyl-β-cyclodextrin microspheres show good potentiality as delivery systems for the intra-articular administration of CCB.
PLGA microspheres were prepared as a sustained release system for the intra-articular administration of celecoxib (CCB). The microspheres were prepared in the presence of different concentrations of dimethyl-β-cyclodextrin (DM-β-Cyd), by the simple oil-in-water emulsion/evaporation solvent method. The microspheres were evaluated as to surface morphology, size and technological properties (such as encapsulation efficiency, drug loading capacity and drug release). Ex vivo studies on cultures of human chondrocytes were performed in order to evaluate the influence of the polymeric carriers on the pharmacological activity of CCB. All systems ranged from about 1 to 5μm in size and had a high encapsulation efficiency percentage ranging from about 80% to 90% (w/w), except for CCB-loaded-PLGA microspheres containing the highest amount of DM-β-Cyd, in which a dramatic drop in the encapsulation efficiency was observed (about 54%, w/w). FIB images evidenced the fact that the microspheres had a porous structure in the presence of the highest amount of DM-β-Cyd. The macrocycle modulated the release profiles of CCB from the microspheres, producing in some cases a zero-order kinetic release. Ex vivo biological studies demonstrated that DM-β-Cyd improved the drug's anti-inflammatory activity. Thus, CCB-loaded PLGA/cyclodextrin microspheres may have a potential therapeutic application in the treatment of osteo- and rheumatoid arthritis.</description><subject>anti-inflammatory activity</subject><subject>Anti-Inflammatory Agents - pharmacology</subject><subject>Calorimetry, Differential Scanning</subject><subject>Celecoxib</subject><subject>Cells, Cultured</subject><subject>Chondrocyte cultures</subject><subject>chondrocytes</subject><subject>Chondrocytes - cytology</subject><subject>Chondrocytes - drug effects</subject><subject>Circular Dichroism</subject><subject>colloids</subject><subject>Culture</subject><subject>Cyclodextrins</subject><subject>Cyclodextrins - chemistry</subject><subject>Diclofenac - pharmacology</subject><subject>Diffusion</subject><subject>Dimethyl-β-cyclodextrin</subject><subject>Drug delivery systems</subject><subject>Drugs</subject><subject>emulsions</subject><subject>Encapsulation</subject><subject>evaporation</subject><subject>Human</subject><subject>Humans</subject><subject>Lactic Acid - chemistry</subject><subject>Microspheres</subject><subject>PLGA microspheres</subject><subject>Polyglycolic Acid - chemistry</subject><subject>Pyrazoles - pharmacology</subject><subject>Release kinetics</subject><subject>rheumatoid arthritis</subject><subject>solvents</subject><subject>Sulfonamides - pharmacology</subject><subject>Surface chemistry</subject><issn>0927-7765</issn><issn>1873-4367</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2013</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqNkc1u1DAURi0EokPhFUqWbJL63wkrqhEUpJFAgq4tj33DeJTEg-2MGp6Bh8ajadnSlWXrfJ-v7kHoiuCGYCKv940NQ5pjv20oJqzBssFEPEMr0ipWcybVc7TCHVW1UlJcoFcp7THGlBP1El1Q1rKWdGKF_qxhABvu_bYegnHgqm-b25tru9ghOLjP0U_V6G0M6bCDCOl9td6ZaGyG6H-b7MNUmclVcDTDfL6GvrxkX_upH8w4mhziUpWAP_q8VAXYzaOZKrsLk4vBLhkqOw95LuWv0YveDAnePJyX6O7Txx_rz_Xm6-2X9c2mtly0uSaMOgqibTuhMDaSGrKlgrQgDeGycy13zuJOccak5D1preKcgDKuN67DmF2id-feQwy_ZkhZjz5ZGAYzQZiTJlIQTiWj5AloAYlo1RNQISmnHWWnAeQZPS02Rej1IfrRxEUTrE9-9V4_-tUnvxpLXfyW4NXDH_N2BPcv9ii0AG_PQG-CNj-jT_rue2mQRT6THVaF-HAmoGz46CHqZD1MFpyPYLN2wf9vir8vYsVB</recordid><startdate>20131101</startdate><enddate>20131101</enddate><creator>Cannavà, Carmela</creator><creator>Tommasini, Silvana</creator><creator>Stancanelli, Rosanna</creator><creator>Cardile, Venera</creator><creator>Cilurzo, Felisa</creator><creator>Giannone, Ignazio</creator><creator>Puglisi, Giovanni</creator><creator>Ventura, Cinzia Anna</creator><general>Elsevier B.V</general><scope>FBQ</scope><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>7X8</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>7SR</scope><scope>7U5</scope><scope>8BQ</scope><scope>JG9</scope><scope>L7M</scope></search><sort><creationdate>20131101</creationdate><title>Celecoxib-loaded PLGA/cyclodextrin microspheres: Characterization and evaluation of anti-inflammatory activity on human chondrocyte cultures</title><author>Cannavà, Carmela ; Tommasini, Silvana ; Stancanelli, Rosanna ; Cardile, Venera ; Cilurzo, Felisa ; Giannone, Ignazio ; Puglisi, Giovanni ; Ventura, Cinzia Anna</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c458t-132d2e58895700a62a1b2518e6a1469d84ddc097433664f18c7441e7adfad9003</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2013</creationdate><topic>anti-inflammatory activity</topic><topic>Anti-Inflammatory Agents - pharmacology</topic><topic>Calorimetry, Differential Scanning</topic><topic>Celecoxib</topic><topic>Cells, Cultured</topic><topic>Chondrocyte cultures</topic><topic>chondrocytes</topic><topic>Chondrocytes - cytology</topic><topic>Chondrocytes - drug effects</topic><topic>Circular Dichroism</topic><topic>colloids</topic><topic>Culture</topic><topic>Cyclodextrins</topic><topic>Cyclodextrins - chemistry</topic><topic>Diclofenac - pharmacology</topic><topic>Diffusion</topic><topic>Dimethyl-β-cyclodextrin</topic><topic>Drug delivery systems</topic><topic>Drugs</topic><topic>emulsions</topic><topic>Encapsulation</topic><topic>evaporation</topic><topic>Human</topic><topic>Humans</topic><topic>Lactic Acid - chemistry</topic><topic>Microspheres</topic><topic>PLGA microspheres</topic><topic>Polyglycolic Acid - chemistry</topic><topic>Pyrazoles - pharmacology</topic><topic>Release kinetics</topic><topic>rheumatoid arthritis</topic><topic>solvents</topic><topic>Sulfonamides - pharmacology</topic><topic>Surface chemistry</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Cannavà, Carmela</creatorcontrib><creatorcontrib>Tommasini, Silvana</creatorcontrib><creatorcontrib>Stancanelli, Rosanna</creatorcontrib><creatorcontrib>Cardile, Venera</creatorcontrib><creatorcontrib>Cilurzo, Felisa</creatorcontrib><creatorcontrib>Giannone, Ignazio</creatorcontrib><creatorcontrib>Puglisi, Giovanni</creatorcontrib><creatorcontrib>Ventura, Cinzia Anna</creatorcontrib><collection>AGRIS</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>Engineered Materials Abstracts</collection><collection>Solid State and Superconductivity Abstracts</collection><collection>METADEX</collection><collection>Materials Research Database</collection><collection>Advanced Technologies Database with Aerospace</collection><jtitle>Colloids and surfaces, B, Biointerfaces</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Cannavà, Carmela</au><au>Tommasini, Silvana</au><au>Stancanelli, Rosanna</au><au>Cardile, Venera</au><au>Cilurzo, Felisa</au><au>Giannone, Ignazio</au><au>Puglisi, Giovanni</au><au>Ventura, Cinzia Anna</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Celecoxib-loaded PLGA/cyclodextrin microspheres: Characterization and evaluation of anti-inflammatory activity on human chondrocyte cultures</atitle><jtitle>Colloids and surfaces, B, Biointerfaces</jtitle><addtitle>Colloids Surf B Biointerfaces</addtitle><date>2013-11-01</date><risdate>2013</risdate><volume>111</volume><spage>289</spage><epage>296</epage><pages>289-296</pages><issn>0927-7765</issn><eissn>1873-4367</eissn><abstract>•Celecoxib loaded-PLGA/dimethyl-β-cyclodextrin microspheres were prepared.•Dimethyl-β-cyclodextrin improves technological parameters of PLGA microspheres and modulates the release of celecoxib from the microspheres.•Celecoxib loaded-PLGA/dimethyl-β-cyclodextrin microspheres was more effective than the free drug as an anti-inflammatory agent on human chondrocyte cultures.•PLGA/dimethyl-β-cyclodextrin microspheres show good potentiality as delivery systems for the intra-articular administration of CCB.
PLGA microspheres were prepared as a sustained release system for the intra-articular administration of celecoxib (CCB). The microspheres were prepared in the presence of different concentrations of dimethyl-β-cyclodextrin (DM-β-Cyd), by the simple oil-in-water emulsion/evaporation solvent method. The microspheres were evaluated as to surface morphology, size and technological properties (such as encapsulation efficiency, drug loading capacity and drug release). Ex vivo studies on cultures of human chondrocytes were performed in order to evaluate the influence of the polymeric carriers on the pharmacological activity of CCB. All systems ranged from about 1 to 5μm in size and had a high encapsulation efficiency percentage ranging from about 80% to 90% (w/w), except for CCB-loaded-PLGA microspheres containing the highest amount of DM-β-Cyd, in which a dramatic drop in the encapsulation efficiency was observed (about 54%, w/w). FIB images evidenced the fact that the microspheres had a porous structure in the presence of the highest amount of DM-β-Cyd. The macrocycle modulated the release profiles of CCB from the microspheres, producing in some cases a zero-order kinetic release. Ex vivo biological studies demonstrated that DM-β-Cyd improved the drug's anti-inflammatory activity. Thus, CCB-loaded PLGA/cyclodextrin microspheres may have a potential therapeutic application in the treatment of osteo- and rheumatoid arthritis.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>23838195</pmid><doi>10.1016/j.colsurfb.2013.06.015</doi><tpages>8</tpages></addata></record> |
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| subjects | anti-inflammatory activity Anti-Inflammatory Agents - pharmacology Calorimetry, Differential Scanning Celecoxib Cells, Cultured Chondrocyte cultures chondrocytes Chondrocytes - cytology Chondrocytes - drug effects Circular Dichroism colloids Culture Cyclodextrins Cyclodextrins - chemistry Diclofenac - pharmacology Diffusion Dimethyl-β-cyclodextrin Drug delivery systems Drugs emulsions Encapsulation evaporation Human Humans Lactic Acid - chemistry Microspheres PLGA microspheres Polyglycolic Acid - chemistry Pyrazoles - pharmacology Release kinetics rheumatoid arthritis solvents Sulfonamides - pharmacology Surface chemistry |
| title | Celecoxib-loaded PLGA/cyclodextrin microspheres: Characterization and evaluation of anti-inflammatory activity on human chondrocyte cultures |
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