Related Experiment Video
Updated: Jun 22, 2026
10:04
Local Application of Drugs to Study Nicotinic Acetylcholine Receptor Function in Mouse Brain Slices
Published on: October 29, 2012
Nortriptyline for smoking cessation: release and human skin diffusion from patches
A Melero1, T M Garrigues, M Alós
1Department of Pharmacy and Pharmaceutics, Faculty of Pharmacy, University of Valencia, Av. Vicente Andrés Estellés, s/n, 46100-Burjassot, Valencia, Spain.
International Journal of Pharmaceutics
|June 9, 2009
Summary
This study developed a novel transdermal Nortriptyline Hydrochloride (NTH) patch for smoking cessation. The NTH patches demonstrated controlled release and effective skin permeation, offering a promising alternative for nicotine dependence treatment.
Area of Science:
- Pharmaceutical Sciences
- Dermatology
- Drug Delivery Systems
Background:
- Smoking cessation therapy often relies on methods with variable efficacy and adherence.
- Transdermal drug delivery offers a potential alternative for consistent therapeutic dosing.
- Nortriptyline Hydrochloride (NTH) is an established medication for smoking cessation support.
Purpose of the Study:
- To develop a simple, cost-effective transdermal formulation of Nortriptyline Hydrochloride (NTH).
- To evaluate the release kinetics and skin permeation of NTH from developed patches.
- To assess the potential of the NTH patches for delivering therapeutic doses for smoking cessation support.
Main Methods:
- Formulation of transdermal patches using Hydroxypropyl-methyl-cellulose and selected enhancers.
- Characterization of patches: appearance, thickness, NTH content uniformity, release, and skin permeation.
- In vitro diffusion studies using human heat separated epidermis (HHSE) and Franz Diffusion Cells (FDC).
- Confocal Laser Scanning Microscopy (CLSM) to evaluate skin integrity post-application.
Main Results:
- Four formulations exhibited controlled NTH release.
- NTH flux through HHSE ranged from 20.39 to 256.19 microg/(cm(2) h).
- NTH penetration into stratum corneum and deeper skin layers was quantified.
- Confocal microscopy showed no evidence of skin damage.
Conclusions:
- Developed NTH transdermal patches offer controlled release and effective permeation.
- The highest flux achieved supports delivering recommended daily doses (25-75 mg) with practical patch sizes.
- These NTH patches represent a viable, non-damaging option for smoking cessation support therapy.
Related Concept Videos
01:18Transdermal Drug Delivery Systems
Transdermal drug delivery systems (TDDS) enable the controlled release of drugs across the skin into systemic circulation. They are particularly advantageous for drugs with short half-lives or narrow therapeutic indices, as they maintain consistent plasma concentrations and reduce the risk of subtherapeutic or toxic levels.TDDS are categorized into monolithic, reservoir, and mixed systems. Monolithic systems embed the drug in a polymer matrix, where diffusion governs release. Reservoir systems...
01:23Drugs Acting on Autonomic Ganglia: Stimulants
Ganglionic stimulants activate NM nicotinic receptors in autonomic ganglia, falling into two categories: nicotine mimetics [e.g., lobeline, dimethylpiperazine, tetramethylammonium] and muscarinic receptor agonists [e.g., muscarine, methacholine]. The first category's action is rapid and blocked by nicotinic receptor antagonists, while the second category's action is delayed and blocked by atropine-like agents. Nicotine, an alkaloid, affects the heart rate by stimulating sympathetic or...
01:22Drug Delivery: Miscellaneous Routes
Drug delivery methods like oral inhalation, nasal sprays, transdermal patches, eye drops, intravitreal injection, and rectal administration provide localized effects with reduced toxicity.
Oral inhalation and nasal sprays swiftly transfer drugs across the respiratory epithelium's mucosal layer. Inhaled glucocorticoids and bronchodilators directly target lung conditions such as asthma, while fluticasone nasal spray mitigates allergic rhinitis.
Transdermal patches transport drugs through the...
Oral inhalation and nasal sprays swiftly transfer drugs across the respiratory epithelium's mucosal layer. Inhaled glucocorticoids and bronchodilators directly target lung conditions such as asthma, while fluticasone nasal spray mitigates allergic rhinitis.
Transdermal patches transport drugs through the...
01:26Oral Drug Delivery Systems: Continuous-Release Systems
Continuous-release drug delivery systems offer a strategic approach to maintaining therapeutic drug levels over extended periods following oral administration. By modulating the release rate of active pharmaceutical ingredients, these systems minimize fluctuations in plasma concentrations, which enhances clinical efficacy and reduces the need for frequent dosing. Such characteristics make them particularly advantageous in managing chronic diseases where patient adherence and stable drug...
01:27CNS Depressants: Alcohol and Nicotine
Ethanol, a clear colorless alcohol, has been consumed by humans for millennia, but its effects on the body are far from benign. At lower doses, it induces decreased inhibitions and loquaciousness, leading to its social appeal. However, it can cause severe consequences at higher doses, such as coma and respiratory depression, due to its zero-order elimination kinetics. Chronic ethanol abuse wreaks havoc on multiple organ systems, particularly the CNS and the liver. Abrupt cessation of ethanol...
01:23Antidepressant Drugs: MAOIs and Other Agents
Atypical antidepressants, including bupropion (Wellbutrin), mirtazapine (Remeron), nefazodone (Serzone), trazodone (Desyrel), and vilazodone (Viibryd), offer unique mechanisms of action. Bupropion weakly inhibits dopamine and norepinephrine reuptake, aiding depression treatment and smoking cessation, with a low risk of sexual dysfunction. Mirtazapine enhances serotonin and norepinephrine neurotransmission, leading to sedation, increased appetite, and weight gain. As a result, it helps treat...