Abstract
Mortality rate due to heart diseases increases dramatically with age. Captopril is an angiotensin converting enzyme inhibitor (ACE) used effectively for the management of hypertension. Due to short elimination half-life of captopril the oral dose is very high. Captopril is prone to oxidation and it has been reported that the oxidation rate of captopril in skin tissues is considerably low when compared to intestinal tissues. All these factors make captopril an ideal drug candidate for transdermal delivery. In this research work an effort was made to formulate transdermal films of captopril by utilizing polyvinylpyrrolidone (PVP) and polyvinyl alcohol (PVA) as film formers and polyethylene glycol 400 (PEG400) as a plasticizer. Dimethyl sulfoxide (DMSO) and dimethylformamide (DMF) were used as permeation enhancers. Physicochemical parameters of the films such as appearance, thickness, weight variation and drug content were evaluated. The invitro permeation studies were carried out through excised human cadaver skin using Franz diffusion cells. The in-vitro permeation studies demonstrated that the film (P4) having the polymer ratio (PVP:PVA = 80:20) with DMSO (10%) resulted a promising drug release of 79.58% at 24 hours with a flux of 70.0 µg/cm2/hr. No signs of erythema or oedema were observed on the rabbit skin as a result of skin irritation study by Draize test. Based on the stability report it was confirmed that the films were physically and chemically stable, hence the prepared films are very well suited for transdermal application.
Keywords: Transdermal, captopril, dimethyl formamide, dimethylsulfoxide, polyvinyl alcohol, polyvinylpyrrolidone.
Current Drug Delivery
Title:Permeation Studies of Captopril Transdermal Films Through Human Cadaver Skin
Volume: 12 Issue: 5
Author(s): Rajesh Sreedharan Nair and Sujith Nair
Affiliation:
Keywords: Transdermal, captopril, dimethyl formamide, dimethylsulfoxide, polyvinyl alcohol, polyvinylpyrrolidone.
Abstract: Mortality rate due to heart diseases increases dramatically with age. Captopril is an angiotensin converting enzyme inhibitor (ACE) used effectively for the management of hypertension. Due to short elimination half-life of captopril the oral dose is very high. Captopril is prone to oxidation and it has been reported that the oxidation rate of captopril in skin tissues is considerably low when compared to intestinal tissues. All these factors make captopril an ideal drug candidate for transdermal delivery. In this research work an effort was made to formulate transdermal films of captopril by utilizing polyvinylpyrrolidone (PVP) and polyvinyl alcohol (PVA) as film formers and polyethylene glycol 400 (PEG400) as a plasticizer. Dimethyl sulfoxide (DMSO) and dimethylformamide (DMF) were used as permeation enhancers. Physicochemical parameters of the films such as appearance, thickness, weight variation and drug content were evaluated. The invitro permeation studies were carried out through excised human cadaver skin using Franz diffusion cells. The in-vitro permeation studies demonstrated that the film (P4) having the polymer ratio (PVP:PVA = 80:20) with DMSO (10%) resulted a promising drug release of 79.58% at 24 hours with a flux of 70.0 µg/cm2/hr. No signs of erythema or oedema were observed on the rabbit skin as a result of skin irritation study by Draize test. Based on the stability report it was confirmed that the films were physically and chemically stable, hence the prepared films are very well suited for transdermal application.
Export Options
About this article
Cite this article as:
Nair Sreedharan Rajesh and Nair Sujith, Permeation Studies of Captopril Transdermal Films Through Human Cadaver Skin, Current Drug Delivery 2015; 12 (5) . https://dx.doi.org/10.2174/1567201812666150212124508
DOI https://dx.doi.org/10.2174/1567201812666150212124508 |
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
-
Preface [Hot Topic: The Roller Coaster of Antioxidant Therapy (Guest Editor: Francesco Visioli)]
Current Medicinal Chemistry Aliphatic and Aromatic Oxidations, Epoxidation and S-Oxidation of Prodrugs that Yield Active Drug Metabolites
Current Medicinal Chemistry Biomimetic Approaches for Targeted Nanomedicine: Current Status and Future Perspectives
Current Drug Therapy Antithrombotic Therapy in Cardiac Embolism
Current Cardiology Reviews Supplementation of Creatine and Ribose Prevents Apoptosis and Right Ventricle Hypertrophy in Hypoxic Hearts
Current Pharmaceutical Design Serum Uric Acid and Diabetes: From Pathophysiology to Cardiovascular Disease
Current Pharmaceutical Design High Density Lipoprotein Associated Paraoxonase1 Activity in Relation to Oxidative Stress in CAD Patients
Current Cardiology Reviews Novel Molecules Targeting Dyslipidemia and Atherosclerosis
Current Medicinal Chemistry Natural Polyphenols and Cardioprotection
Mini-Reviews in Medicinal Chemistry Structural and Functional Diversity of Estrogen Receptor Ligands
Current Topics in Medicinal Chemistry L-Dopa Related Hyperhomocysteinemia: A Possible Mediator of Toxicity?
Letters in Drug Design & Discovery Complications of the Type 2 Diabetes Mellitus
Current Cardiology Reviews Asymptomatic Primary Hyperparathyroidism: Management and Implications
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Influence of Leptin on Immunity
Current Immunology Reviews (Discontinued) Cell Microencapsulation Implants into the Central Nervous System
Recent Patents on Nanomedicine Cell-Penetrating Peptides as a Potential Drug Delivery System for Effective Treatment of Diabetes
Current Pharmaceutical Design The Impact of Diabetes on Mortality Among Elderly Patients Admitted for Treatment at a Hospital for Cardiovascular Disease in Southern Brazil
Current Diabetes Reviews Pharmacotherapy in Neonatal and Pediatric Extracorporeal Membrane Oxygenation (ECMO)
Current Drug Metabolism Psoriatic Arthritis – Review of the Immunologic, Clinic and Therapeutic Aspects of an Inflammatory Systemic Disease
Current Rheumatology Reviews Virus Vasculopathy and Stroke: An Under-Recognized Cause and Treatment Target
Infectious Disorders - Drug Targets