Abstract
Inadequate skin permeability is the main challenge encountered in the transdermal drug delivery and to solve this crisis physical and chemical enhancement techniques are being developed. The aim of the present investigation was to study the combined effect of two such techniques, iontophoresis and esterification, on the transdermal delivery of atenolol. A series of ester prodrugs of atenolol were synthesized, characterized and studied for physicochemical properties and stability. In vitro permeation studies were carried out for atenolol and prodrugs at different donor concentrations (5, 10, and 20 mM) by passive process and iontophoresis (0.5 mA/cm ). Evaluation of the physicochemical parameters showed significant increase in lipophilicity and slight reduction in pK value in the ester prodrugs compared to parent drug. Stability studies revealed higher stability at pH 4 than pH 6. Prodrugs significantly enhanced the transdermal flux of atenolol in passive process while in iontophoresis the enhancement ranged from 1.4 to 2.7 fold compared to atenolol. In the prodrug series, permeation rate increased with increase in the length of alkyl side chain up to the addition of 5 carbon units, but thereafter no specific pattern was recorded in both passive and iontophoretic process. The steady state flux was highest in atenolol valerate (1.48 μmol/cm h), which shows the promise of meeting the desired permeation rate (3.0- 31.0 μmol/ h) for maintenance of the therapeutic level in a 70 kg human.
Keywords: Transdermal, prodrugs, atenolol, stability, iontophoresis
Current Drug Delivery
Title: Transdermal Delivery of Atenolol: Effect of Prodrugs and Iontophoresis
Volume: 6 Issue: 3
Author(s): B. Anroop, B. Ghosh, V. Parcha and J. Khanam
Affiliation:
Keywords: Transdermal, prodrugs, atenolol, stability, iontophoresis
Abstract: Inadequate skin permeability is the main challenge encountered in the transdermal drug delivery and to solve this crisis physical and chemical enhancement techniques are being developed. The aim of the present investigation was to study the combined effect of two such techniques, iontophoresis and esterification, on the transdermal delivery of atenolol. A series of ester prodrugs of atenolol were synthesized, characterized and studied for physicochemical properties and stability. In vitro permeation studies were carried out for atenolol and prodrugs at different donor concentrations (5, 10, and 20 mM) by passive process and iontophoresis (0.5 mA/cm ). Evaluation of the physicochemical parameters showed significant increase in lipophilicity and slight reduction in pK value in the ester prodrugs compared to parent drug. Stability studies revealed higher stability at pH 4 than pH 6. Prodrugs significantly enhanced the transdermal flux of atenolol in passive process while in iontophoresis the enhancement ranged from 1.4 to 2.7 fold compared to atenolol. In the prodrug series, permeation rate increased with increase in the length of alkyl side chain up to the addition of 5 carbon units, but thereafter no specific pattern was recorded in both passive and iontophoretic process. The steady state flux was highest in atenolol valerate (1.48 μmol/cm h), which shows the promise of meeting the desired permeation rate (3.0- 31.0 μmol/ h) for maintenance of the therapeutic level in a 70 kg human.
Export Options
About this article
Cite this article as:
Anroop B., Ghosh B., Parcha V. and Khanam J., Transdermal Delivery of Atenolol: Effect of Prodrugs and Iontophoresis, Current Drug Delivery 2009; 6 (3) . https://dx.doi.org/10.2174/156720109788680895
DOI https://dx.doi.org/10.2174/156720109788680895 |
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
-
Extracellular Vesicles Isolated from Mesenchymal Stromal Cells Primed with Hypoxia: Novel Strategy in Regenerative Medicine
Current Stem Cell Research & Therapy Phospholipid Transfer Protein in Diabetes, Metabolic Syndrome and Obesity
Cardiovascular & Hematological Disorders-Drug Targets Personalizing HER2-Targeted Therapy in Metastatic Breast Cancer Beyond HER2 Status: What We Have Learned from Clinical Specimens
Current Pharmacogenomics and Personalized Medicine Therapeutic Potential of Modulating MicroRNA in Peripheral Artery Disease
Current Vascular Pharmacology Association between Paraoxonase 1(PON1) Gene Polymorphisms and PON1 Enzyme Activity in Indian Patients with Coronary Artery Disease (CAD)
Current Pharmacogenomics and Personalized Medicine N-3 (Omega-3) Fatty Acids: Effects on Brain Dopamine Systems and Potential Role in the Etiology and Treatment of Neuropsychiatric Disorders
CNS & Neurological Disorders - Drug Targets Neuroprotective and Preventative Effects of Molecular Hydrogen
Current Pharmaceutical Design Vitamin D Deficiency May Be Associated with a More Rapid Decline in CD4 Cell Count to <350 Cells/µL in Untreated HIV-Infected Adults
Current HIV Research Risk Factors of Alzheimers Disease Among Iranian Population
Current Alzheimer Research Majra Honey Abrogated the Normal and Cancer Cells Proliferation Inhibition by Juniperus procera Extract and Extract/Honey Generated AgNPs
Anti-Cancer Agents in Medicinal Chemistry Strategies for Overcoming Inherent and Acquired Resistance to EGFR Inhibitors by Targeting Downstream Effectors in the RAS/PI3K Pathway
Current Cancer Drug Targets Biochemical Markers of Cardiovascular Damage from Tobacco Smoke
Current Pharmaceutical Design A Review of Eugenol-based Nanomedicine: Recent Advancements
Current Bioactive Compounds Phycobilins and Phycobiliproteins Used in Food Industry and Medicine
Mini-Reviews in Medicinal Chemistry Subject Index to Volume 2
Current Pharmacogenomics Atypical Presentation of Tardive Dyskinesia Associated with Risperidone Long-Acting Injection as Maintenance Treatment in Bipolar Affective Disorder: A Case Report
Current Drug Safety Dabigatran - A New Chapter in Anticoagulation
Cardiovascular & Hematological Agents in Medicinal Chemistry Mechanisms of Incretin Effects on Plasma Lipids and Implications for the Cardiovascular System
Cardiovascular & Hematological Agents in Medicinal Chemistry New Target Molecules in the Drug Control of Blood Pressure and Circulation
Current Drug Targets - Cardiovascular & Hematological Disorders Evaluation of Anticancer, Antibacterial and Antioxidant Properties of a Medicinally Treasured Fern Tectaria coadunata with its Phytoconstituents Analysis by HR-LCMS
Anti-Cancer Agents in Medicinal Chemistry