Dissolving microarray patches for transdermal delivery of risperidone for schizophrenia management

Area of Science:

• Pharmaceutical Sciences
• Biomedical Engineering
• Drug Delivery Systems

Background:

• Schizophrenia treatment often involves risperidone (RIS), a hydrophobic drug with limitations in oral/intramuscular delivery.
• Transdermal drug delivery (TDD) offers a potential alternative for improved RIS administration.
• Developing effective TDD systems for poorly water-soluble drugs like RIS remains a challenge.

Purpose of the Study:

• To develop and characterize risperidone nanocrystals (NCs) for transdermal drug delivery.
• To incorporate RIS NCs into dissolving microneedle array patches (DMAPs) for enhanced drug delivery.
• To evaluate the in vitro, ex vivo, and in vivo performance of RIS-loaded DMAPs.

Main Methods:

• Formulation of RIS NCs using wet-media milling with poly(vinyl alcohol) (PVA) as a stabilizer.
• Fabrication of DMAPs loaded with RIS NCs.
• In vitro drug release studies over 28 days.
• Ex vivo skin permeation studies.
• In vivo pharmacokinetic studies in Sprague Dawley rats.

Main Results:

• RIS NCs with a particle size of approximately 300 nm were successfully prepared.
• Enhanced drug release of up to 80% over 28 days was observed from the NCs.
• Ex vivo studies demonstrated significantly higher RIS delivery from NC-loaded DMAPs compared to bulk RIS DMAPs.
• In vivo studies showed sustained plasma detection of RIS and its metabolite for 5 days, with a ~15-fold higher AUC compared to oral administration.

Conclusions:

• This study presents a novel approach for transdermal delivery of risperidone using dissolving microneedle array patches loaded with nanocrystals.
• RIS-loaded DMAPs significantly improve the pharmacokinetic profile compared to oral administration.
• This technology holds promise for the transdermal delivery of other poorly water-soluble drugs.