Tranexamic acid loaded gellan gum-based polymeric microbeads for controlled release: In vitro and in vivo assessment
•Microbeads containing tranexamic acid for oral controlled release application.•Microbeads were prepared in complete aqueous environment thereby toxicity due to organic solvents was bypassed.•In vivo study confirmed the controlled release activity of these newly prepared microbeads.•pH sensitive dru...
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Veröffentlicht in: | Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2013-12, Vol.112, p.483-491 |
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creator | Bhattacharya, Shiv Sankar Banerjee, Subham Chowdhury, Purojit Ghosh, Amitava Hegde, Rahul Rama Mondal, Ranjit |
description | •Microbeads containing tranexamic acid for oral controlled release application.•Microbeads were prepared in complete aqueous environment thereby toxicity due to organic solvents was bypassed.•In vivo study confirmed the controlled release activity of these newly prepared microbeads.•pH sensitive drug delivery system.
Gellan gum (GG) microbeads containing tranexamic acid (TA), an anti-fibrinolytic drug were prepared by a classic sol–gel transition induced by ionic crosslinking technique using aluminum chloride (AlCl3) as cross-linking agent. The influence of different formulation variables on in vitro physico-chemical parameters and drug release studies were performed systematically. The microbeads were evaluated by scanning electron microscopy (SEM), Fourier transform infra-red (FTIR) spectroscopy, X-ray diffraction (XRD), differential scanning calorimetry (DSC) and high performance liquid chromatographic (HPLC) analysis. Particle size and swelling behavior of microbeads were also investigated. Microbeads showed improved drug encapsulation efficiency along with enhanced drug release. The in vivo studies exhibited sustained drug release in rabbits over a prolonged period after oral administration of these newly developed TA loaded GG microbeads. Based on the results of in vitro and in vivo studies in experimental animal model it was concluded that these microbeads provided intestinal specific controlled release of TA. |
doi_str_mv | 10.1016/j.colsurfb.2013.07.054 |
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Gellan gum (GG) microbeads containing tranexamic acid (TA), an anti-fibrinolytic drug were prepared by a classic sol–gel transition induced by ionic crosslinking technique using aluminum chloride (AlCl3) as cross-linking agent. The influence of different formulation variables on in vitro physico-chemical parameters and drug release studies were performed systematically. The microbeads were evaluated by scanning electron microscopy (SEM), Fourier transform infra-red (FTIR) spectroscopy, X-ray diffraction (XRD), differential scanning calorimetry (DSC) and high performance liquid chromatographic (HPLC) analysis. Particle size and swelling behavior of microbeads were also investigated. Microbeads showed improved drug encapsulation efficiency along with enhanced drug release. The in vivo studies exhibited sustained drug release in rabbits over a prolonged period after oral administration of these newly developed TA loaded GG microbeads. Based on the results of in vitro and in vivo studies in experimental animal model it was concluded that these microbeads provided intestinal specific controlled release of TA.</description><identifier>ISSN: 0927-7765</identifier><identifier>EISSN: 1873-4367</identifier><identifier>DOI: 10.1016/j.colsurfb.2013.07.054</identifier><identifier>PMID: 24183265</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>aluminum chloride ; animal models ; Animals ; Antifibrinolytic Agents - administration & dosage ; Antifibrinolytic Agents - blood ; Antifibrinolytic Agents - pharmacokinetics ; Biomedical materials ; colloids ; Controlled release ; Cross-Linking Reagents ; crosslinking ; Delayed-Action Preparations - chemistry ; differential scanning calorimetry ; Drug Carriers - chemistry ; Drug Compounding - methods ; Drug Delivery Systems ; drugs ; encapsulation ; Female ; Fourier transform infrared spectroscopy ; Gellan gum ; high performance liquid chromatography ; Hydrogels ; In vitro testing ; in vivo studies ; In vivo testing ; In vivo tests ; Male ; Mathematical models ; Microbeads ; Microscopy, Electron, Scanning ; Microspheres ; Nanoparticles ; oral administration ; Particle Size ; physicochemical properties ; Polysaccharides, Bacterial - chemistry ; Rabbits ; scanning electron microscopy ; Sol–gel transition ; Spectroscopy, Fourier Transform Infrared ; Surgical implants ; Thermodynamics ; Tranexamic acid ; Tranexamic Acid - administration & dosage ; Tranexamic Acid - blood ; Tranexamic Acid - pharmacokinetics ; X-Ray Diffraction</subject><ispartof>Colloids and surfaces, B, Biointerfaces, 2013-12, Vol.112, p.483-491</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-8247193b5ba72119b0e2d2cf529562053d81d8b82402175e6657d8011e5a1ed43</citedby><cites>FETCH-LOGICAL-c458t-8247193b5ba72119b0e2d2cf529562053d81d8b82402175e6657d8011e5a1ed43</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.2013.07.054$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3548,27923,27924,45994</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/24183265$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Bhattacharya, Shiv Sankar</creatorcontrib><creatorcontrib>Banerjee, Subham</creatorcontrib><creatorcontrib>Chowdhury, Purojit</creatorcontrib><creatorcontrib>Ghosh, Amitava</creatorcontrib><creatorcontrib>Hegde, Rahul Rama</creatorcontrib><creatorcontrib>Mondal, Ranjit</creatorcontrib><title>Tranexamic acid loaded gellan gum-based polymeric microbeads for controlled release: In vitro and in vivo assessment</title><title>Colloids and surfaces, B, Biointerfaces</title><addtitle>Colloids Surf B Biointerfaces</addtitle><description>•Microbeads containing tranexamic acid for oral controlled release application.•Microbeads were prepared in complete aqueous environment thereby toxicity due to organic solvents was bypassed.•In vivo study confirmed the controlled release activity of these newly prepared microbeads.•pH sensitive drug delivery system.
Gellan gum (GG) microbeads containing tranexamic acid (TA), an anti-fibrinolytic drug were prepared by a classic sol–gel transition induced by ionic crosslinking technique using aluminum chloride (AlCl3) as cross-linking agent. The influence of different formulation variables on in vitro physico-chemical parameters and drug release studies were performed systematically. The microbeads were evaluated by scanning electron microscopy (SEM), Fourier transform infra-red (FTIR) spectroscopy, X-ray diffraction (XRD), differential scanning calorimetry (DSC) and high performance liquid chromatographic (HPLC) analysis. Particle size and swelling behavior of microbeads were also investigated. Microbeads showed improved drug encapsulation efficiency along with enhanced drug release. The in vivo studies exhibited sustained drug release in rabbits over a prolonged period after oral administration of these newly developed TA loaded GG microbeads. Based on the results of in vitro and in vivo studies in experimental animal model it was concluded that these microbeads provided intestinal specific controlled release of TA.</description><subject>aluminum chloride</subject><subject>animal models</subject><subject>Animals</subject><subject>Antifibrinolytic Agents - administration & dosage</subject><subject>Antifibrinolytic Agents - blood</subject><subject>Antifibrinolytic Agents - pharmacokinetics</subject><subject>Biomedical materials</subject><subject>colloids</subject><subject>Controlled release</subject><subject>Cross-Linking Reagents</subject><subject>crosslinking</subject><subject>Delayed-Action Preparations - chemistry</subject><subject>differential scanning calorimetry</subject><subject>Drug Carriers - chemistry</subject><subject>Drug Compounding - methods</subject><subject>Drug Delivery Systems</subject><subject>drugs</subject><subject>encapsulation</subject><subject>Female</subject><subject>Fourier transform infrared spectroscopy</subject><subject>Gellan gum</subject><subject>high performance liquid chromatography</subject><subject>Hydrogels</subject><subject>In vitro testing</subject><subject>in vivo studies</subject><subject>In vivo testing</subject><subject>In vivo tests</subject><subject>Male</subject><subject>Mathematical models</subject><subject>Microbeads</subject><subject>Microscopy, Electron, Scanning</subject><subject>Microspheres</subject><subject>Nanoparticles</subject><subject>oral administration</subject><subject>Particle Size</subject><subject>physicochemical properties</subject><subject>Polysaccharides, Bacterial - chemistry</subject><subject>Rabbits</subject><subject>scanning electron microscopy</subject><subject>Sol–gel transition</subject><subject>Spectroscopy, Fourier Transform Infrared</subject><subject>Surgical implants</subject><subject>Thermodynamics</subject><subject>Tranexamic acid</subject><subject>Tranexamic Acid - administration & dosage</subject><subject>Tranexamic Acid - blood</subject><subject>Tranexamic Acid - pharmacokinetics</subject><subject>X-Ray Diffraction</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>eNqNkUtv1DAQgC0EosvCXyg-cknw2wknUMWjUiUOtGfLsScrr5x4sZNV--_xsi3Xchp79M2MPR9Cl5S0lFD1cd-6FMuax6FlhPKW6JZI8QJtaKd5I7jSL9GG9Ew3Wit5gd6UsieEMEH1a3RRQ8eZkhu03GY7w72dgsPWBY9jsh483kGMdsa7dWoGW2rikOLDBLliFc1pAOsLHlPGLs1LTjFWJkOECn_C1zM-hprFdvY4nC7Hei4FSplgXt6iV6ONBd49xi26-_b19upHc_Pz-_XVl5vGCdktTceEpj0f5GA1o7QfCDDP3ChZLxUjkvuO-m6oGGFUS1BKat8RSkFaCl7wLfpw7nvI6fcKZTFTKO7vzyCtxVAlqeCM8_4_UMEUJVx1z6NC9KxjsjbeInVG68ZKyTCaQw6TzQ-GEnPyaPbmyaM5eTREm-qxFl4-zliHCfy_sidxFXh_BkabjN3lUMzdr9pBVclcE8Er8flMQN3wMUA2xQWYHfiQwS3Gp_DcK_4ANwa6fA</recordid><startdate>20131201</startdate><enddate>20131201</enddate><creator>Bhattacharya, Shiv Sankar</creator><creator>Banerjee, Subham</creator><creator>Chowdhury, Purojit</creator><creator>Ghosh, Amitava</creator><creator>Hegde, Rahul Rama</creator><creator>Mondal, Ranjit</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>20131201</creationdate><title>Tranexamic acid loaded gellan gum-based polymeric microbeads for controlled release: In vitro and in vivo assessment</title><author>Bhattacharya, Shiv Sankar ; Banerjee, Subham ; Chowdhury, Purojit ; Ghosh, Amitava ; Hegde, Rahul Rama ; Mondal, Ranjit</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c458t-8247193b5ba72119b0e2d2cf529562053d81d8b82402175e6657d8011e5a1ed43</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2013</creationdate><topic>aluminum chloride</topic><topic>animal models</topic><topic>Animals</topic><topic>Antifibrinolytic Agents - administration & dosage</topic><topic>Antifibrinolytic Agents - blood</topic><topic>Antifibrinolytic Agents - pharmacokinetics</topic><topic>Biomedical materials</topic><topic>colloids</topic><topic>Controlled release</topic><topic>Cross-Linking Reagents</topic><topic>crosslinking</topic><topic>Delayed-Action Preparations - chemistry</topic><topic>differential scanning calorimetry</topic><topic>Drug Carriers - chemistry</topic><topic>Drug Compounding - methods</topic><topic>Drug Delivery Systems</topic><topic>drugs</topic><topic>encapsulation</topic><topic>Female</topic><topic>Fourier transform infrared spectroscopy</topic><topic>Gellan gum</topic><topic>high performance liquid chromatography</topic><topic>Hydrogels</topic><topic>In vitro testing</topic><topic>in vivo studies</topic><topic>In vivo testing</topic><topic>In vivo tests</topic><topic>Male</topic><topic>Mathematical models</topic><topic>Microbeads</topic><topic>Microscopy, Electron, Scanning</topic><topic>Microspheres</topic><topic>Nanoparticles</topic><topic>oral administration</topic><topic>Particle Size</topic><topic>physicochemical properties</topic><topic>Polysaccharides, Bacterial - chemistry</topic><topic>Rabbits</topic><topic>scanning electron microscopy</topic><topic>Sol–gel transition</topic><topic>Spectroscopy, Fourier Transform Infrared</topic><topic>Surgical implants</topic><topic>Thermodynamics</topic><topic>Tranexamic acid</topic><topic>Tranexamic Acid - administration & dosage</topic><topic>Tranexamic Acid - blood</topic><topic>Tranexamic Acid - pharmacokinetics</topic><topic>X-Ray Diffraction</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Bhattacharya, Shiv Sankar</creatorcontrib><creatorcontrib>Banerjee, Subham</creatorcontrib><creatorcontrib>Chowdhury, Purojit</creatorcontrib><creatorcontrib>Ghosh, Amitava</creatorcontrib><creatorcontrib>Hegde, Rahul Rama</creatorcontrib><creatorcontrib>Mondal, Ranjit</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>Bhattacharya, Shiv Sankar</au><au>Banerjee, Subham</au><au>Chowdhury, Purojit</au><au>Ghosh, Amitava</au><au>Hegde, Rahul Rama</au><au>Mondal, Ranjit</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Tranexamic acid loaded gellan gum-based polymeric microbeads for controlled release: In vitro and in vivo assessment</atitle><jtitle>Colloids and surfaces, B, Biointerfaces</jtitle><addtitle>Colloids Surf B Biointerfaces</addtitle><date>2013-12-01</date><risdate>2013</risdate><volume>112</volume><spage>483</spage><epage>491</epage><pages>483-491</pages><issn>0927-7765</issn><eissn>1873-4367</eissn><abstract>•Microbeads containing tranexamic acid for oral controlled release application.•Microbeads were prepared in complete aqueous environment thereby toxicity due to organic solvents was bypassed.•In vivo study confirmed the controlled release activity of these newly prepared microbeads.•pH sensitive drug delivery system.
Gellan gum (GG) microbeads containing tranexamic acid (TA), an anti-fibrinolytic drug were prepared by a classic sol–gel transition induced by ionic crosslinking technique using aluminum chloride (AlCl3) as cross-linking agent. The influence of different formulation variables on in vitro physico-chemical parameters and drug release studies were performed systematically. The microbeads were evaluated by scanning electron microscopy (SEM), Fourier transform infra-red (FTIR) spectroscopy, X-ray diffraction (XRD), differential scanning calorimetry (DSC) and high performance liquid chromatographic (HPLC) analysis. Particle size and swelling behavior of microbeads were also investigated. Microbeads showed improved drug encapsulation efficiency along with enhanced drug release. The in vivo studies exhibited sustained drug release in rabbits over a prolonged period after oral administration of these newly developed TA loaded GG microbeads. Based on the results of in vitro and in vivo studies in experimental animal model it was concluded that these microbeads provided intestinal specific controlled release of TA.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>24183265</pmid><doi>10.1016/j.colsurfb.2013.07.054</doi><tpages>9</tpages></addata></record> |
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subjects | aluminum chloride animal models Animals Antifibrinolytic Agents - administration & dosage Antifibrinolytic Agents - blood Antifibrinolytic Agents - pharmacokinetics Biomedical materials colloids Controlled release Cross-Linking Reagents crosslinking Delayed-Action Preparations - chemistry differential scanning calorimetry Drug Carriers - chemistry Drug Compounding - methods Drug Delivery Systems drugs encapsulation Female Fourier transform infrared spectroscopy Gellan gum high performance liquid chromatography Hydrogels In vitro testing in vivo studies In vivo testing In vivo tests Male Mathematical models Microbeads Microscopy, Electron, Scanning Microspheres Nanoparticles oral administration Particle Size physicochemical properties Polysaccharides, Bacterial - chemistry Rabbits scanning electron microscopy Sol–gel transition Spectroscopy, Fourier Transform Infrared Surgical implants Thermodynamics Tranexamic acid Tranexamic Acid - administration & dosage Tranexamic Acid - blood Tranexamic Acid - pharmacokinetics X-Ray Diffraction |
title | Tranexamic acid loaded gellan gum-based polymeric microbeads for controlled release: In vitro and in vivo assessment |
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