Permeation enhancement of ascorbic acid by self-dissolving micropile array tip through rat skin
Yukako Ito1, Tomohiro Maeda, Keizo Fukushima
1Department of Pharmacokinetics, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto, Japan. yukako@mb.kyoto-phu.ac.jp
Self-dissolving micropiles (SDMP) loaded with ascorbic acid (AA) offer effective percutaneous delivery. These innovative microneedles demonstrate rapid AA release and enhanced skin permeation, suggesting their utility for transdermal AA administration.
Area of Science:
- Pharmaceutical Technology
- Dermal Drug Delivery
- Biomaterials Science
Background:
- Percutaneous administration of ascorbic acid (AA) is challenging due to skin barrier properties.
- Chondroitin sulfate-based self-dissolving micropiles (SDMP) offer a novel approach for enhanced transdermal delivery.
Purpose of the Study:
- To develop and evaluate ascorbic acid (AA) loaded self-dissolving micropiles (SDMP) for percutaneous administration.
- To assess the in vitro release, stability, and skin permeation of AA from SDMP.
Main Methods:
- SDMPs were fabricated using chondroitin sulfate, loaded with varying concentrations of AA, and characterized.
- In vitro dissolution and stability studies were conducted under controlled conditions.
- In vitro permeation studies using isolated rat skin and in vivo studies on anesthetized rat skin were performed to evaluate AA penetration.
Main Results:
- SDMPs demonstrated rapid in vitro release of AA (>90% within 5 min) and excellent stability (>99% after 1 week).
- Significant in vitro permeation of AA into receptor compartments was observed, attributed to compromised skin barrier function.
- AA permeation was dependent on both SDMP AA content and contact time, with higher permeation observed for high-content SDMPs and longer contact durations.
Conclusions:
- AA-loaded SDMP array tips are effective for percutaneous delivery of ascorbic acid.
- The developed SDMP system shows promise for enhancing transdermal AA absorption, overcoming conventional delivery limitations.
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