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Development, Characterization, and Evaluation of CAGE-based Ionic Liquid Systems for Transdermal Delivery
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A Novel Eutectic-Based Transdermal Delivery System for Risperidone
Faisal Al-Akayleh1, Samer Adwan2, Mai Khanfar3
1Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy and Medical Sciences, Petra University, Amman, Jordan.
AAPS Pharmscitech
|November 22, 2020
Summary
Researchers developed novel therapeutic deep eutectic solvents (THEDES) using risperidone and fatty acids. These formulations significantly enhanced drug solubility and skin permeation, showing potential for improved drug delivery with no irritation.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Drug Delivery Systems
Background:
- Risperidone (RIS) is an antipsychotic medication with limited aqueous solubility.
- Traditional formulations may not optimize RIS delivery and efficacy.
- Deep Eutectic Solvents (DES) offer potential for enhancing drug solubility and permeation.
Purpose of the Study:
- To investigate the formation of novel room temperature therapeutic deep eutectic solvents (THEDES) of risperidone with capric acid (CA) and lauric acid (LA).
- To characterize the physicochemical properties of these THEDES.
- To evaluate the potential of THEDES for enhancing RIS skin permeation.
Main Methods:
- Preparation and characterization of RIS-fatty acid mixtures.
- Differential Scanning Calorimetry (DSC) for phase diagram construction and melting point determination.
- Freeze-drying microscopy for phase transition analysis.
- Solubility studies, skin permeation assays, rheological measurements, and in vivo skin irritation tests.
Main Results:
- Novel liquid THEDES of RIS with CA and LA were successfully formed at room temperature.
- Lowest melting points achieved were 17°C (RIS:CA, 40:60% w/w) and 22°C (RIS:LA, 30:70% w/w).
- RIS solubility increased up to 70,000-fold compared to water.
- Significant enhancement (P < 0.05) in RIS skin permeation was observed.
- THEDES formulations exhibited temperature-dependent viscosity, fitting the Arrhenius equation.
- No skin irritation or edema was observed in rat models.
Conclusions:
- Novel RIS-based THEDES with capric acid and lauric acid offer a promising platform for enhanced drug delivery.
- These formulations significantly improve RIS solubility and skin permeation.
- The developed THEDES are safe for topical application, demonstrating potential for improved risperidone therapy.
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