Abstract
Glimepiride is a third generation oral antidiabetic sulphonylurea drug frequently prescribed to patients of type 2 diabetes. However, its oral therapy is encountered with bioavailability problems due to its poor solubility leading to irreproducible clinical response, in addition to adverse effects like dizziness and gastric disturbances. As a potential for convenient, safe and effective antidiabetic therapy, the rationale of this study was to develop a transdermal delivery system for glimepiride. Chitosan polymer was utilized in developing transdermal films for glimepiride. Chitosan has film forming ability, bioadhesive and absorption enhancing properties. Aiming at optimizing the drug delivery and circumventing the skin barrier function, inclusion complexation of glimepiride with beta-cyclodextrin (β-CyD) as well as the use of several conventional penetration enhancers were monitored for augmenting the drug flux. The physical and mechanical properties of the prepared films were investigated using tensile testing, IR spectroscopy and X-ray diffractometry. Release studies revealed adequate release rates from chitosan films. Permeation studies through full thickness rat abdominal skin were conducted. High flux values were obtained from films comprising a combination of the drug with limonene and ethanol as well as from films containing glimepiride-β-CyD complex. In vivo studies on diabetic rats for selected formulae revealed a marked therapeutic efficacy sustained for about 48 hours. The above-mentioned results shed light on feasibility of utilizing chitosan as an effective, safe transdermal delivery system for glimepiride characterized by increased patient compliance and better control of the disease.
Keywords: Glimepiride, transdermal, chitosan, penetration enhancers, cyclodextrins
Current Drug Delivery
Title: Design and Evaluation of Chitosan Films for Transdermal Delivery of Glimepiride
Volume: 5 Issue: 4
Author(s): H. O. Ammar, H. A. Salama, S. A. El-Nahhas and H. Elmotasem
Affiliation:
Keywords: Glimepiride, transdermal, chitosan, penetration enhancers, cyclodextrins
Abstract: Glimepiride is a third generation oral antidiabetic sulphonylurea drug frequently prescribed to patients of type 2 diabetes. However, its oral therapy is encountered with bioavailability problems due to its poor solubility leading to irreproducible clinical response, in addition to adverse effects like dizziness and gastric disturbances. As a potential for convenient, safe and effective antidiabetic therapy, the rationale of this study was to develop a transdermal delivery system for glimepiride. Chitosan polymer was utilized in developing transdermal films for glimepiride. Chitosan has film forming ability, bioadhesive and absorption enhancing properties. Aiming at optimizing the drug delivery and circumventing the skin barrier function, inclusion complexation of glimepiride with beta-cyclodextrin (β-CyD) as well as the use of several conventional penetration enhancers were monitored for augmenting the drug flux. The physical and mechanical properties of the prepared films were investigated using tensile testing, IR spectroscopy and X-ray diffractometry. Release studies revealed adequate release rates from chitosan films. Permeation studies through full thickness rat abdominal skin were conducted. High flux values were obtained from films comprising a combination of the drug with limonene and ethanol as well as from films containing glimepiride-β-CyD complex. In vivo studies on diabetic rats for selected formulae revealed a marked therapeutic efficacy sustained for about 48 hours. The above-mentioned results shed light on feasibility of utilizing chitosan as an effective, safe transdermal delivery system for glimepiride characterized by increased patient compliance and better control of the disease.
Export Options
About this article
Cite this article as:
Ammar O. H., Salama A. H., El-Nahhas A. S. and Elmotasem H., Design and Evaluation of Chitosan Films for Transdermal Delivery of Glimepiride, Current Drug Delivery 2008; 5 (4) . https://dx.doi.org/10.2174/156720108785915005
DOI https://dx.doi.org/10.2174/156720108785915005 |
Print ISSN 1567-2018 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5704 |
Call for Papers in Thematic Issues
Advancements in Robotic and AI-based Drug Discovery and Delivery for Neurological Disorders
Neurological disorders, including Alzheimer's disease, Parkinson's disease, epilepsy, and brain tumors, pose significant challenges in drug delivery due to the blood-brain barrier's intricate structure and the complexity of neuronal networks. Traditional drug delivery methods often fall short in reaching therapeutic concentrations within the central nervous system, limiting treatment efficacy and ...read more
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
- 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
-
Ethnic Disparity and Increased Prevalence of Type 2 Diabetes Among South Asians: Aetiology and Future Implications for Diabetes Prevention and Management
Current Diabetes Reviews Endometriosis and Gynecological Cancer
Current Women`s Health Reviews Von Hippel-Lindau Disease
Current Molecular Medicine Bioanalytical Applications of Au Nanoparticles
Recent Patents on Nanotechnology Adrenomedullin-RAMP2 System in Cardiovascular Development and Homeostasis
Current Hypertension Reviews Low Levels of High Density Lipoprotein Increase the Severity of Cerebral White Matter Changes:Implications for Prevention and Treatment of Cerebrovascular Diseases
Current Alzheimer Research Neuropharmacological Actions of Metformin in Stroke
Current Neuropharmacology Mitochondrial Membrane Lipids in Life and Death and their Molecular Modulation by Diet: Tuning the Furnace
Current Drug Targets Vitamin-D Receptor (VDR) Gene Polymorphisms (TaqI, FokI) in Turkish Patients with Hashimoto’s Thyroiditis: Relationship to the Levels of Vit-D and Cytokines
Endocrine, Metabolic & Immune Disorders - Drug Targets Realizing the Potential of Health-Promoting Rosehips from Dogroses (Rosa sect. Caninae)
Current Bioactive Compounds Research Strategies for Pain in Lumbar Radiculopathy Focusing on Acid-Sensing Ion Channels and Their Toxins
Current Topics in Medicinal Chemistry Disrupting Self-Assembly and Toxicity of Amyloidogenic Protein Oligomers by “ Molecular Tweezers” - from the Test Tube to Animal Models
Current Pharmaceutical Design Symptomatic Treatment of Chronic Neuropathic Pain with Gabapentin Clinical Practice and Research Prospective
Current Neuropharmacology Early Development of Symptomatic Drugs in AD: A Systematic Review of the Use of Biomarkers
CNS & Neurological Disorders - Drug Targets Primary and Secondary Hypertriglyceridaemia
Current Drug Targets SUMOylation in Neurological Diseases
Current Molecular Medicine Choice of Antihypertensive Treatment in Subjects with Pre-Diabetes. Is There a Dream After the Navigator
Current Vascular Pharmacology Expression of a Disintegrin and Metalloprotease 10 Gene Polymorphisms in a Cohort of Egyptian Patients with Hepatocellular Carcinoma
Current Cancer Therapy Reviews Novel Approaches to the Pharmacotherapy of Obesity
Current Pharmaceutical Design Wound-Associated Skin Fibrosis: Mechanisms and Treatments Based on Modulating the Inflammatory Response
Endocrine, Metabolic & Immune Disorders - Drug Targets