Related Experiment Video
Updated: May 15, 2026
11:27
A Package of Established Analytical Tools to Investigate the Solid-State Alteration of Lipid-Based Excipients
Published on: August 9, 2022
Formulation and optimization of desogestrel transdermal contraceptive patch using crystallization studies
Vishal Sachdeva1, Yun Bai, Agis Kydonieus
1Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Mercer University, Atlanta, GA 30341, USA.
International Journal of Pharmaceutics
|December 25, 2012
Summary
This study explores desogestrel for transdermal contraception, finding it more permeable than levonorgestrel. Optimized patches show potential for a 7-day contraceptive delivery system.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Dermatology
Background:
- Levonorgestrel (LNG) is the standard progestin for contraception.
- Transdermal drug delivery offers an alternative contraceptive route.
- Desogestrel's potential for transdermal application requires investigation.
Purpose of the Study:
- To evaluate desogestrel as an alternative progestin for transdermal contraceptive patches.
- To optimize formulation and adhesive selection for effective desogestrel delivery.
- To assess the feasibility of a 7-day transdermal contraceptive patch.
Main Methods:
- Saturation solubility studies of desogestrel in acrylate and polyisobutylene (PIB) adhesives.
- Formulation development using copovidone and mineral oil to enhance drug loading in PIB.
- Physical characterization including in vitro release, content uniformity, adhesion, and skin permeation studies.
- Comparison of desogestrel permeability against levonorgestrel.
Main Results:
- Desogestrel exhibited significantly higher permeability compared to LNG (p<0.05).
- Acrylate adhesives showed higher desogestrel saturation solubility than PIB.
- Optimized PIB formulations with mineral oil and copovidone improved drug loading and cosmetic properties.
- In vitro studies demonstrated potential for a uniform and reproducible 7-day patch.
Conclusions:
- Desogestrel is a promising candidate for transdermal contraceptive patches due to its enhanced permeability.
- Formulation strategies involving specific excipients and adhesives can overcome challenges in drug loading and delivery.
- The developed formulation shows potential for a novel, long-acting transdermal contraceptive system.
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...
01:21Intrauterine Drug Delivery Systems
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...
01:25Crystal Growth: Principles of Crystallization
Crystallization is a phase transformation process in which crystals are precipitated from a supersaturated solution or formed from other sources. During crystallization, atoms or molecules arrange themselves into a well-defined, rigid crystal lattice to minimize energy.
Initiating crystallization involves manipulating the concentration of the solute and the temperature of the solution. Since crystal growth occurs when the ratio of concentration and solubility of the solute in the solvent – the...
Initiating crystallization involves manipulating the concentration of the solute and the temperature of the solution. Since crystal growth occurs when the ratio of concentration and solubility of the solute in the solvent – the...
01:21Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
01:29Clinically Relevant Drug Product Specifications: Methods of Establishment
Product specifications define the acceptable quality of a pharmaceutical product by ensuring identity, purity, potency, and strength. These specifications serve as benchmarks during development, manufacturing, and post-approval quality control. Clinically relevant specifications are particularly important because they directly relate to a drug's safety and efficacy in clinical use.Dissolution studies are critical biopharmaceutic tools that link in vitro behavior to in vivo performance. They...
01:10Recrystallization: Solid–Solution Equilibria
Recrystallization is a purification technique used to separate impurities from solid compounds. In this technique, no chemical reactions occur. Instead, it exploits physical properties only, specifically, the solubility differences between the desired compound and impurities, either at a single temperature or at different temperatures, and under other selected conditions. The solid-solution equilibrium (solubility equilibrium) of each component in the solution represents a binary phase...