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Design of Ionic Liquid Formulations with Azone-Mimic Structures for Enhanced Drug Skin Permeation
Takeshi Oshizaka1, Aki Yamamoto1, Hikaru Tanaka1
1Faculty of Pharmaceutical Sciences, Josai International University, 1 Gumyo, Togane, Chiba 283-8555, Japan.
Journal of Pharmaceutical Sciences
|December 16, 2023
Summary
A novel ionic liquid, IL-Azone, enhances drug skin permeation more effectively than Azone when formulated with white petrolatum. This formulation minimizes IL-Azone degradation, leading to rapid and pronounced drug delivery.
Area of Science:
- Pharmaceutical Sciences
- Dermal Drug Delivery
- Materials Science
Background:
- Laurocapram (Azone) is a potent skin permeation enhancer but causes significant skin irritation.
- Ionic liquids (ILs) offer potential as less irritating alternatives for drug delivery.
- An Azone-mimic ionic liquid (IL-Azone) was developed using less irritating components: cationic ε-caprolactam and anionic myristic acid.
Purpose of the Study:
- To identify a suitable formulation for the developed IL-Azone.
- To evaluate the skin permeation enhancement of IL-Azone compared to Azone.
- To investigate the influence of formulation water content on IL-Azone stability and efficacy.
Main Methods:
- Formulations containing 5% Azone or IL-Azone with the model drug antipyrine were prepared.
- Skin permeation experiments were conducted using various formulations.
- The effect of white petrolatum's low water content on IL-Azone stability and permeation enhancement was assessed.
Main Results:
- IL-Azone demonstrated minimal skin permeation enhancement with most tested formulations.
- A significant and rapid enhancement in skin permeation was observed when IL-Azone was combined with white petrolatum.
- IL-Azone in white petrolatum showed more pronounced and faster permeation enhancement than Azone, attributed to its degradation at the stratum corneum-epidermis interface.
Conclusions:
- White petrolatum is a suitable vehicle for IL-Azone, preventing its premature degradation due to minimal water content.
- IL-Azone in white petrolatum offers superior and faster drug skin permeation compared to Azone.
- This optimized formulation holds promise for enhanced dermal drug delivery applications.
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