Abstract
In the present work calcium pectinate (Ca-pectinate) microspheres were prepared to deliver methotrexate in the environment of colon. Calcium pectinate microspheres were prepared by modified emulsification method using calcium chloride as cross linker. All the formulations were evaluated for various physicochemical parameters. Particle size of the microspheres was determined using laser diffraction particle size analyzer. Encapsulation efficiency was determined by digesting with enzyme pectinase for 24 hours and swellability by equilibrium swelling in simulated gastrointestinal fluid. The in vitro drug release studies were performed in simulated gastric fluid for 2 hours and simulated intestinal fluid for 3 hours. In vitro release rate studies were also carried out in simulated colonic fluid in presence of rat caecal contents. Moreover, release rate studies were also carried out after enzyme induction by treating the rats with 1 ml of 1% w/v aqueous dispersion of pectin for 7 days. Mean particle size of the microspheres was found to be in the range of 20.82±1.34 to 32.26±1.59 μm whereas the entrapment efficiency varied from 52.28±0.32 to 74.01±3.32%. The in vitro drug release studies in simulated gastric fluid and simulated intestinal fluid showed that only 8.15±0.49% drug was released in 5 hours whereas most of the loaded drug was released in simulated colonic fluid containing pectinase. In vitro release rate study showed release of 69.94±3.46% of drug in presence of 3% rat caecal contents, which was further increased to 94.43±4.48% when enzyme induction was carried out for 7 days. Thus, it is concluded that calcium pectinate microspheres can be used to effectively localize the release of drug in the physiological environment of colon.
Keywords: Calcium pectinate microspheres, natural polysaccharides, colon targeted drug delivery, colo-rectal cancer
Current Drug Delivery
Title: Methotrexate Bearing Calcium Pectinate Microspheres: A Platform to Achieve Colon-Specific Drug Release
Volume: 5 Issue: 3
Author(s): M. Chaurasia, M. K. Chourasia, Nitin K. Jain, A. Jain, V. Soni, Y. Gupta and S. K. Jain
Affiliation:
Keywords: Calcium pectinate microspheres, natural polysaccharides, colon targeted drug delivery, colo-rectal cancer
Abstract: In the present work calcium pectinate (Ca-pectinate) microspheres were prepared to deliver methotrexate in the environment of colon. Calcium pectinate microspheres were prepared by modified emulsification method using calcium chloride as cross linker. All the formulations were evaluated for various physicochemical parameters. Particle size of the microspheres was determined using laser diffraction particle size analyzer. Encapsulation efficiency was determined by digesting with enzyme pectinase for 24 hours and swellability by equilibrium swelling in simulated gastrointestinal fluid. The in vitro drug release studies were performed in simulated gastric fluid for 2 hours and simulated intestinal fluid for 3 hours. In vitro release rate studies were also carried out in simulated colonic fluid in presence of rat caecal contents. Moreover, release rate studies were also carried out after enzyme induction by treating the rats with 1 ml of 1% w/v aqueous dispersion of pectin for 7 days. Mean particle size of the microspheres was found to be in the range of 20.82±1.34 to 32.26±1.59 μm whereas the entrapment efficiency varied from 52.28±0.32 to 74.01±3.32%. The in vitro drug release studies in simulated gastric fluid and simulated intestinal fluid showed that only 8.15±0.49% drug was released in 5 hours whereas most of the loaded drug was released in simulated colonic fluid containing pectinase. In vitro release rate study showed release of 69.94±3.46% of drug in presence of 3% rat caecal contents, which was further increased to 94.43±4.48% when enzyme induction was carried out for 7 days. Thus, it is concluded that calcium pectinate microspheres can be used to effectively localize the release of drug in the physiological environment of colon.
Export Options
About this article
Cite this article as:
Chaurasia M., Chourasia K. M., Jain K. Nitin, Jain A., Soni V., Gupta Y. and Jain K. S., Methotrexate Bearing Calcium Pectinate Microspheres: A Platform to Achieve Colon-Specific Drug Release, Current Drug Delivery 2008; 5 (3) . https://dx.doi.org/10.2174/156720108784911668
DOI https://dx.doi.org/10.2174/156720108784911668 |
Print ISSN 1567-2018 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5704 |
Call for Papers in Thematic Issues
Advances of natural products, bio-actives and novel drug delivery system against emerging viral infections
Due to the increasing prevalence of viral infections and the ability of these human pathogens to develop resistance to current treatment strategies, there is a great need to find and develop new compounds to combat them. These molecules must have low toxicity, specific activity and high bioavailability. The most suitable ...read more
Electrospun Fibers as Drug Delivery Systems
In recent years, electrospun fibers have attracted considerable attention as potential platforms for drug delivery due to their distinctive properties and adaptability. These fibers feature a notable surface area-to-volume ratio and can be intentionally designed with high porosity, facilitating an increased capacity for drug loading and rendering them suitable for ...read more
Emerging Nanotherapeutics for Mitigation of Neurodegenerative Disorders
Conditions affecting the central nervous system (CNS) present a significant hurdle due to limited access of both treatments and diagnostic tools for the brain. The blood-brain barrier (BBB) acts as a barrier, restricting the passage of molecules from the bloodstream into the brain. The most formidable challenge facing scientists is ...read more
Nanotechnology Based Chemotherapy for the treatment of Head & Neck Cancer
The escalating recurrence rates observed in Head and Neck cancer, particularly within the chemo-therapeutically treated cohort (50-60%), can be attributed to the non-selective nature of current anticancer drug delivery modalities. In this context, nanotechnology-based drug delivery systems emerge as a promising avenue for achieving precise localization of therapeutic agents to ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Multivariate Analysis Applied to Trace and Ultra-Trace Elements in Italian Potable Waters Determined by INAA
Current Analytical Chemistry Generalized String Pseudo-Folding Lattices in Bioinformatics: State-of-Art Review, New Model for Enzyme Sub-Classes, and Study of ESTs on Trichinella spiralis
Current Bioinformatics Design, Synthesis and Pharmacological Evaluation of Gastro- Protective Anti-inflammatory Analgesic Agents based on Dual Oxidative Stress / Cyclooxygenase Inhibition
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry The Kynurenine Pathway in the Acute and Chronic Phases of Cerebral Ischemia
Current Pharmaceutical Design Metabolism of Acrylamide: Interindividual and Interspecies Differences as Well as the Application as Biomarkers
Current Drug Metabolism Immunostimulatory Oligonucleotides
Recent Patents on Inflammation & Allergy Drug Discovery Polydivinylbenzene Hollow Nanospheres as an Effective Fluorescent Sensing Platform for DNA Detection
Current Nanoscience Electrochemical Indicators for DNA Electroanalysis
Current Analytical Chemistry Efficient Loading and Controlled Release of Benzophenone-3 Entrapped into Self-Assembling Nanogels
Current Nanoscience Diagnostic Recognition of Escherichia <i>coli</i> Septicemia in <i>In Vivo</i> Vascular Blood
Medicinal Chemistry The Interaction of Zinc Oxide/Green Tea Extract Complex Nanoparticles and its Effect on Monosodium Glutamate Toxicity in Liver of Rats
Current Pharmaceutical Biotechnology Synthesis and Anticancer Studies of Novel N-benzyl Pyridazino ne Derivatives
Letters in Drug Design & Discovery Synthesis and Biological Evaluation of 1, 3-Dihydroxyxanthone Mannich Base Derivatives as Potential Antitumor Agents
Letters in Drug Design & Discovery Hydroxytyrosol Expresses Antifungal Activity In Vitro
Current Drug Targets Design and Development of Molecular Imaging Probes
Current Topics in Medicinal Chemistry Wnt/β-catenin Antagonists: Exploring New Avenues to Trigger Old Drugs in Alleviating Glioblastoma Multiforme
Current Molecular Pharmacology The Impact of Malnutrition on the Peripheral Serotoninergic System in Anorexia Nervosa: A Systematic Review
Current Psychiatry Reviews First Synthesis of 5- and 7-Phenylethynyl-8-hydroxyquinolines by Sonogashira Reaction
Letters in Organic Chemistry Neonatal Brain Hemorrhage (NBH) of Prematurity: Translational Mechanisms of the Vascular-Neural Network
Current Medicinal Chemistry Purification and Characterization of a Laccase with Inhibitory Activity Toward HIV-1 Reverse Transcriptase and Tumor Cells from an Edible Mushroom (Pleurotus cornucopiae)
Protein & Peptide Letters