Related Experiment Video
Updated: May 24, 2026
09:44
Development, Characterization, and Evaluation of CAGE-based Ionic Liquid Systems for Transdermal Delivery
Published on: September 26, 2025
Formulation and evaluation of transdermal patch of repaglinide
Shailesh T Prajapati1, Charmi G Patel, Chhagan N Patel
1Department of Pharmaceutics, Shri Sarvajanik Pharmacy College, Gujarat, Mehsana 384001, India.
ISRN Pharmaceutics
|March 6, 2012
Summary
Repaglinide transdermal patches were developed to improve drug release and patient compliance. Optimized batch F6, using HPMC K100 and 1.5% PVP, showed 92.34% drug release over 12 hours.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Materials Science
Background:
- Repaglinide exhibits short half-life (1 hour) and low bioavailability (56%) due to first-pass metabolism.
- Frequent dosing (16 mg/day) is required, impacting patient compliance.
- Transdermal drug delivery offers a potential solution for sustained release and improved bioavailability.
Purpose of the Study:
- To develop and optimize transdermal patches of Repaglinide for sustained drug release.
- To enhance drug bioavailability and improve patient compliance through a novel drug delivery system.
- To investigate the effects of hydroxypropyl methylcellulose (HPMC) grades and polyvinylpyrrolidone (PVP) K30 concentrations on patch properties and drug release kinetics.
Main Methods:
- Repaglinide transdermal patches were prepared using the solvent casting method, varying HPMC grades and PVP K30 concentrations.
- Formulations underwent comprehensive evaluation, including physical properties, drug content, and in vitro drug release/permeation studies.
- A 3(2) full factorial design was employed to analyze the impact of HPMC (X1) and PVP (X2) on tensile strength, drug release at 1 and 9 hours, and diffusion coefficient.
Main Results:
- Optimized batch F6, containing HPMC K100 and 1.5% PVP, demonstrated sustained release of 92.343% over 12 hours.
- The factorial design analysis identified significant effects of HPMC grades and PVP concentration on critical formulation parameters.
- In vitro release data analysis, using various kinetic models, elucidated the drug release mechanism.
Conclusions:
- Transdermal patches of Repaglinide are a viable approach for sustained drug delivery, potentially improving bioavailability and patient compliance.
- The optimized formulation (Batch F6) exhibited favorable release characteristics, closely matching theoretical predictions (f(2) = 69.187).
- Further investigation into in vivo performance and long-term stability is warranted.
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...
01:06Oral Hypoglycemic Agents: Glinides
Repaglinide (Prandin) and Nateglinide (Starlix), known as glinides, are oral insulin secretagogues that stimulate insulin release from pancreatic β cells by closing the ATP-sensitive potassium channels (KATP channel). Repaglinide controls insulin release from pancreatic β cells by managing potassium efflux. It shares two binding sites with sulfonylureas and also has a unique site, indicating overlapping mechanisms of action. With a rapid onset and a 4-7 hour duration, it effectively manages...
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...
01:19Modified-Release Drug Delivery Systems: Rate-Programmed II
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...
01:23Modified-Release Drug Delivery Systems: Classification
Modified-release drug delivery systems improve drug efficacy and minimize side effects by controlling the rate and location of drug release. These systems fall into three categories: rate-programmed, stimuli-activated, and site-targeted.Rate-programmed systems release drugs at a predetermined rate, maintaining consistent therapeutic levels and reducing fluctuations that could lead to toxicity or subtherapeutic effects. These systems use polymeric matrices, reservoir-based designs, or osmotic...
01:16Drug Delivery: Overview
The selection of a drug's delivery route depends upon its physicochemical properties, including lipid or water solubility and ionization, as well as the therapeutic requirement, such as immediate or sustained effect. These routes can be divided into three primary categories: enteral, parenteral, and topical.
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the gastrointestinal...
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the gastrointestinal...