Abstract
The purpose of the present study was to design a membrane-moderated transdermal therapeutic system (TTS) of nimodipine using 2%w / w hydroxypropyl methylcellulose (HPMC) gel as a reservoir system containing menthol as penetration enhancer and 60%v / v ethanol-water as solvent system. The flux of nimodipine was markedly increased from 35.51 μg / cm2 / h to 167.53±3.69 μg / cm2 / h with the addition of 8%w / w menthol to HPMC drug reservoir. There was an increase in the flux of nimodipine through ethylene vinyl acetate (EVA) copolymer membrane with an increase in vinyl acetate content (9 to 28%w / w) of the copolymer. The permeability flux of nimodipine from the chosen EVA 2825 (with 28%w / w vinyl acetate content) was 152.05±2.68 μg / cm2 / h, and this flux decreased to 132.69±1.45 μg / cm2 / h on application of a water-based acrylic adhesive (TACKWHITE A 4MED®) coat. However, the transdermal flux of nimodipine across EVA 2825 membrane coated with TACKWHITE A 4MEDa / rat skin composite was found to be 116.05±2.39 μg / cm2 / h, which is about 1.4 times greater than the required flux. Thus a new transdermal therapeutic system for nimodipine was designed using EVA 2825 membrane coated with a pressure-sensitive adhesive TACKWHITE 4A MED®, and 2%w / w HPMC gel as reservoir containing 8%w / w of menthol as a penetration enhancer. The in vivo evaluation of nimodipine TTS patch was carried out to find the ability of the fabricated mentholbased TTS patch in providing the predetermined plasma concentration of the drug in human volunteers. The results showed that the menthol-based TTS patch of nimodipine provided steady plasma concentration of the drug with minimal fluctuations with improved bioavailability in comparison with the immediate release tablet dosage form.
Keywords: transdermal delivery, nimodipine, menthol, membrane-moderated, bioavailability, human volunteers.
Current Drug Delivery
Title: Studies on the Transdermal Delivery of Nimodipine from a Menthol-based TTS in Human Volunteers
Volume: 1 Issue: 2
Author(s): Y. S.R. Krishnaiah and P. Bhaskar
Affiliation:
Keywords: transdermal delivery, nimodipine, menthol, membrane-moderated, bioavailability, human volunteers.
Abstract: The purpose of the present study was to design a membrane-moderated transdermal therapeutic system (TTS) of nimodipine using 2%w / w hydroxypropyl methylcellulose (HPMC) gel as a reservoir system containing menthol as penetration enhancer and 60%v / v ethanol-water as solvent system. The flux of nimodipine was markedly increased from 35.51 μg / cm2 / h to 167.53±3.69 μg / cm2 / h with the addition of 8%w / w menthol to HPMC drug reservoir. There was an increase in the flux of nimodipine through ethylene vinyl acetate (EVA) copolymer membrane with an increase in vinyl acetate content (9 to 28%w / w) of the copolymer. The permeability flux of nimodipine from the chosen EVA 2825 (with 28%w / w vinyl acetate content) was 152.05±2.68 μg / cm2 / h, and this flux decreased to 132.69±1.45 μg / cm2 / h on application of a water-based acrylic adhesive (TACKWHITE A 4MED®) coat. However, the transdermal flux of nimodipine across EVA 2825 membrane coated with TACKWHITE A 4MEDa / rat skin composite was found to be 116.05±2.39 μg / cm2 / h, which is about 1.4 times greater than the required flux. Thus a new transdermal therapeutic system for nimodipine was designed using EVA 2825 membrane coated with a pressure-sensitive adhesive TACKWHITE 4A MED®, and 2%w / w HPMC gel as reservoir containing 8%w / w of menthol as a penetration enhancer. The in vivo evaluation of nimodipine TTS patch was carried out to find the ability of the fabricated mentholbased TTS patch in providing the predetermined plasma concentration of the drug in human volunteers. The results showed that the menthol-based TTS patch of nimodipine provided steady plasma concentration of the drug with minimal fluctuations with improved bioavailability in comparison with the immediate release tablet dosage form.
Export Options
About this article
Cite this article as:
Krishnaiah S.R. Y. and Bhaskar P., Studies on the Transdermal Delivery of Nimodipine from a Menthol-based TTS in Human Volunteers, Current Drug Delivery 2004; 1 (2) . https://dx.doi.org/10.2174/1567201043479966
DOI https://dx.doi.org/10.2174/1567201043479966 |
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
-
Innate Inflammatory Responses in Stroke: Mechanisms and Potential Therapeutic Targets
Current Medicinal Chemistry Novel Hybrid Anticonvulsants Derived from Pyrrolidine-2,5-dione Scaffold with Broad Spectrum of Activity in the Preclinical Studies
Current Topics in Medicinal Chemistry Novel Drug Targets for the Treatment of Cardiac Diseases
Current Pharmacogenomics and Personalized Medicine The Relationship Between Inflammation, Platelet Activation and Antiplatelet Resistance
Inflammation & Allergy - Drug Targets (Discontinued) Clopidogrel in Secondary Ischemic Stroke Prevention
Recent Patents on Cardiovascular Drug Discovery Role of the Blood-Brain Barrier in the Pathogenesis of Alzheimers Disease
Current Alzheimer Research Dyslipidemia, Vascular Atheroma and Statins
Current Vascular Pharmacology Mechanisms of Neuronal Damage and Neuroprotection Underlying Ischemia/Reperfusion Injury after Physical Exercise
Current Drug Targets Diabetes Mellitus and Vascular Endothelial Dysfunction: Current Perspectives
Current Vascular Pharmacology Dietary Melatonin Protects Against Behavioural, Metabolic, Oxidative, and Organ Morphological Changes in Mice that are Fed High-Fat, High- Sugar Diet
Endocrine, Metabolic & Immune Disorders - Drug Targets Stem Cells: An Overview of the Current Status of Therapies for Central and Peripheral Nervous System Diseases
Current Medicinal Chemistry Catatonia Due to a General Medical Condition (Organic Catatonia)
Current Psychiatry Reviews The Role of Venous Abnormalities in Neurological Disease
Reviews on Recent Clinical Trials Cellular Membrane Microparticles: Potential Targets of Combinational Therapy for Vascular Disease
Current Vascular Pharmacology The Neuropathology of Vascular Disease in the Medical Research Council Cognitive Function and Ageing Study (MRC CFAS)
Current Alzheimer Research Is Age of 80 Years a Threshold for Carotid Revascularization?
Current Cardiology Reviews HPTLC Analysis with the Effect of <i>Bacopa monnieri, Evolvulus alsinoides</i> and <i>Tinospora cordifolia</i> against Scopolamine-Induced Amnesic Rats
Drug Delivery Letters Spinal Microvascular Expression of PV-1 is Associated with Inflammation, Perivascular Astrocyte Loss, and Diminished EC Glucose Transport Potential in Acute SCI
Current Neurovascular Research Nanocarriers for Tracking and Treating Diseases
Current Medicinal Chemistry The Multimodal Treatment of Acromegaly: Current Status and Future Perspectives
Endocrine, Metabolic & Immune Disorders - Drug Targets