Transdermal nitroglycerin delivery using acrylic matrices: design, formulation, and in vitro characterization.
Houman Savoji1, Amir Mehdizadeh2, Ahmad Ramazani Saadat Abadi3
1Chemical and Petroleum Engineering Department, Sharif University of Technology, Azadi Avenue, Tehran 11365 8639, Iran ; Hakim Pharmaceutical Co., 1370 Dr. Shariati Avenue, Gholhak, Tehran 11155 4465, Iran.
ISRN Pharmaceutics
|February 11, 2014
Summary
This study optimized nitroglycerin transdermal drug delivery systems (TDDSs) using acrylic adhesives and permeation enhancers. Propylene glycol and Duro-Tak 2054 adhesive proved effective for developing nitroglycerin TDDS.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Dermal Drug Delivery
Background:
- Nitroglycerin (TNG) is a vasodilator used for angina.
- Transdermal drug delivery systems (TDDSs) offer advantages for continuous medication delivery.
- Optimizing TDDS formulations is crucial for effective drug permeation and therapeutic outcomes.
Purpose of the Study:
- To develop and optimize nitroglycerin transdermal drug delivery systems (TDDSs).
- To evaluate the impact of acrylic pressure-sensitive adhesives (PSAs) and chemical permeation enhancers (CPEs) on TNG skin permeation and release.
- To determine optimal formulation parameters for an effective monolithic TNG TDDS.
Main Methods:
- Preparation of TNG TDDSs with various acrylic PSAs and CPEs.
- In vitro evaluation of skin permeation using modified-jacketed Franz diffusion cells with excised rat skin.
- Assessment of drug release using the dissolution method.
- Measurement of adhesion properties, including 180° peel strength and probe tack.
Main Results:
- Skin permeation rate (steady state flux, Jss) was influenced by PSA viscosity, type, and CPE type.
- Duro-Tak 2516 and Duro-Tak 2054 exhibited higher Jss compared to Duro-Tak 2051.
- Propylene glycol showed the highest permeation enhancement; cetyl alcohol showed the lowest.
- Increased CPE concentration decreased PSA adhesion properties.
- An optimized formulation used 10% propylene glycol (PG) as CPE and 25% TNG in Duro-Tak 2054.
Conclusions:
- Acrylic PSA type and viscosity, along with CPE selection, significantly affect nitroglycerin transdermal permeation.
- Propylene glycol is an effective permeation enhancer for nitroglycerin TDDS.
- The optimized formulation (10% PG, 25% TNG in Duro-Tak 2054) is a promising monolithic system for nitroglycerin transdermal therapeutic systems.
More Related Videos
12:22Synthesis of Thermogelling PolyN-isopropylacrylamide-graft-chondroitin Sulfate Composites with Alginate Microparticles for Tissue Engineering
Published on: October 26, 2016
11.4K
11:32Fabrication of Biologically Derived Injectable Materials for Myocardial Tissue Engineering
Published on: December 20, 2010
14.3K
Related Concept Videos
01:18Drug Delivery: Enteral Route
2.9K
The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
2.9K
01:18Transdermal Drug Delivery Systems
233
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...
233
01:21Intrauterine Drug Delivery Systems
168
Controlled-release systems for intravaginal and intrauterine drug delivery have been developed primarily for the administration of contraceptive steroid hormones. These delivery routes circumvent first-pass hepatic metabolism, thereby enhancing bioavailability and allowing for reduced systemic dosages compared to oral administration. Such approaches contribute to improved therapeutic efficacy and patient compliance, particularly in long-term contraceptive regimens.Intravaginal Drug Delivery...
168
01:19Modified-Release Drug Delivery Systems: Rate-Programmed II
137
Rate-programmed drug delivery systems release drugs in a controlled manner to maintain therapeutic levels. Three main designs include reservoir, matrix, and hybrid systems.Reservoir systems consist of a drug core enclosed within a membrane that controls drug release. In non-swelling reservoir systems, polymers like ethyl cellulose or polymethacrylates are used. These do not hydrate in aqueous media and control release through membrane thickness, porosity, or insolubility. This type includes...
137
01:15Non-Oral Extravascular Drug Absorption Routes
724
Non-oral extravascular routes, which encompass sublingual, buccal, topical, intramuscular, and inhalation methods, primarily utilize passive diffusion to transport drugs into the systemic circulation. The absorption rates and effectiveness of these routes depend on the drug's physicochemical properties, as well as the patient's anatomical and pathophysiological state.
Lipophilic drugs that are stable at salivary pH (6) and exhibit minimal binding to the oral mucosa are absorbed more...
Lipophilic drugs that are stable at salivary pH (6) and exhibit minimal binding to the oral mucosa are absorbed more...
724
01:20Modified-Release Drug Delivery Systems: Influencing Factors
208
Modified-release drug delivery systems are designed to optimize the therapeutic effect of drugs by minimizing side effects, reducing the dosage required, and controlling drug release to align with pharmacokinetic and pharmacodynamic needs. The system depends on two key factors: the drug's release from the formulation and its movement through the body to the target site. Unlike conventional dosage forms, where absorption is the limiting step, the rate of drug release is the key determinant in...
208