Related Experiment Video
Updated: Jun 9, 2025
07:49
Slow-release Drug Delivery through Elvax 40W to the Rat Retina: Implications for the Treatment of Chronic Conditions
Published on: September 17, 2014
11.5K
Combining ion-pair strategy and percutaneous permeation enhancers to develop sustained-release paliperidone patch
Yafang Xu1, Shuai Zhang1, Cong Li1
1Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning 110016, China.
International Journal of Pharmaceutics
|October 23, 2024
Summary
A novel sustained-release paliperidone (PAL) patch was developed using ion-pairing and permeation enhancers. This transdermal patch offers improved drug utilization and controlled release, enhancing therapeutic potential.
Area of Science:
- * Pharmaceutical Sciences
- * Drug Delivery Systems
Background:
- * Paliperidone (PAL) is an antipsychotic medication requiring improved delivery methods.
- * Transdermal patches offer a promising alternative to oral administration for sustained drug release.
- * Challenges in transdermal drug delivery include poor drug solubility and skin barrier penetration.
Purpose of the Study:
- * To develop a sustained-release paliperidone transdermal patch.
- * To enhance drug-adhesive miscibility and control drug release using an ion-pair strategy.
- * To improve skin permeation of paliperidone via percutaneous permeation enhancers (PPEs).
Main Methods:
- * Development of a paliperidone patch utilizing ion-pair strategy and PPEs.
- * Optimization of patch formulation (55 μm thickness, 7% PAL-LA, 9.7% POCC) via Box-Behnken design and in vitro permeation studies.
- * Pharmacokinetic evaluation and mechanism studies to assess sustained release and drug utilization.
Main Results:
- * Optimized patch demonstrated sustained release with a longer mean residence time (MRT₀-t) of 18.35 ± 3.11 h and higher bioavailability (BA) of 63.14%.
- * The developed patch showed comparable Cmax to oral gavage but with significantly prolonged drug release.
- * Ion-pair formation effectively improved drug miscibility and controlled release characteristics.
Conclusions:
- * A sustained-release paliperidone transdermal patch was successfully developed.
- * The combination of ion-pairing and PPEs provides an effective strategy for enhancing transdermal drug delivery.
- * The developed patch exhibits favorable properties for sustained drug release, good drug-polymer miscibility, and efficient drug utilization.
Related Concept Videos
01:17Pore Transport and Ion-Pair Transport
377
Pore transport and ion-pair formation are critical mechanisms for the absorption and distribution of drugs in the body.
Pore transport, also known as convective transport, is a process where small molecules like urea, water, and sugars rapidly cross cell membranes as though there were channels or pores in the membrane. Although direct microscopic evidence is limited but the concept of pores or channels is widely accepted based on physiological evidence. Despite the lack of direct...
Pore transport, also known as convective transport, is a process where small molecules like urea, water, and sugars rapidly cross cell membranes as though there were channels or pores in the membrane. Although direct microscopic evidence is limited but the concept of pores or channels is widely accepted based on physiological evidence. Despite the lack of direct...
377
01:29Drug Delivery: Parenteral Route
434
The parenteral route is a critical method of drug administration. It delivers compounds directly into the systemic circulation and bypasses the gastrointestinal tract. This approach is particularly advantageous for drugs that exhibit poor absorption or instability when administered orally.
There are three primary parenteral routes: intravenous (IV), intramuscular (IM), and subcutaneous (SC). The IV route introduces the drug directly into the bloodstream, ensuring immediate action. The IM route...
There are three primary parenteral routes: intravenous (IV), intramuscular (IM), and subcutaneous (SC). The IV route introduces the drug directly into the bloodstream, ensuring immediate action. The IM route...
434
01:22Drug Delivery: Miscellaneous Routes
329
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...
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...
329
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
121
Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
121
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
179
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
179
01:25Routes of Drug Administration: Parenteral
1.9K
The administration of drugs via parenteral routes allows for direct drug introduction into the systemic circulation, resulting in high bioavailability because the medication bypasses the harsh conditions of the gastrointestinal tract and hepatic metabolism.
The intravenous route (IV) of drug administration can be further categorized into two types. The bolus injection administers the entire dose rapidly, while an intravenous infusion slowly delivers smaller doses steadily.
The IV route is often...
The intravenous route (IV) of drug administration can be further categorized into two types. The bolus injection administers the entire dose rapidly, while an intravenous infusion slowly delivers smaller doses steadily.
The IV route is often...
1.9K