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
Hauptverfasser: Bhattacharya, Shiv Sankar, Banerjee, Subham, Chowdhury, Purojit, Ghosh, Amitava, Hegde, Rahul Rama, Mondal, Ranjit
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container_start_page 483
container_title Colloids and surfaces, B, Biointerfaces
container_volume 112
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. 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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.</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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source MEDLINE; ScienceDirect Journals (5 years ago - present)
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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