Abstract
Research on the development of dissolving microneedles (DMNs) has focused on bolus drug delivery, with little attention on sustained release. Here, we evaluated the sustained release, absorption pattern, and effective drug permeation of a novel donepezil-loaded DMN patch through an in vivo investigation on rats. The applications of DMN patches to the shaved skin of rats for 1 week and 1 h were compared with oral donepezil administration to assess their sustained release capabilities. We used a validated liquid chromatography–tandem mass spectrometry method to quantify donepezil in the plasma. We found that the microneedle arrays effectively delivered donepezil across the skin, with dissolution observed within 1 h of application. Furthermore, skin irritation test showed that the patches produced no irritation response. The DMN arrays also effectively increased drug permeation and demonstrated sustained release and absorption of donepezil from DMN patches. These patches allow extended dosing intervals, reduced gastrointestinal adverse effects, and convenient self-administration to mitigate poor drug compliance, making them beneficial for the treatment of elderly patients with Alzheimer’s disease.
Highlights
dissolving microneedles (DMNs) patches were manufactured with various additives
Our novel DMN patch is a combination of DMNs and additional drug layer, both made of biodegradable polymer, sugar, and donepezil
For the in vitro permeation study, drugs were incorporated into a soluble polymeric matrix in DMN patches in which PVP was employed as a base material, and trehalose was used as a plasticizer for improved performance
Summary
The field of microneedles is an emerging research area that combines the advantages of transdermal patches and the effectiveness of hypodermic needles for drug transport across the skin [1,2,3]. Microneedles are micron-scale needles that puncture the stratum corneum, which is the exterior surface layer of skin. They are typically 50–250 μm thick and 150–1500 μm long [4], allowing for penetration of the skin barrier without causing bleeding or stimulation of deeply located pain receptors. DMNs are a type of microneedle composed of biodegradable polymers that incorporate a target drug. Microneedles employing a potent hormonal contraceptive drug demonstrated sustained release, utilizing a patch as a backing support [7]. Drug-loaded microneedles can be self-administered with minimal training and significant tolerability [8,9,10], indicating their potential in the management of Alzheimer’s disease (AD)
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