Transdermal drug delivery of rizatriptan using microneedles array patch: preparation, characterization and...

Area of Science:

• Pharmaceutical Sciences
• Biomaterials Engineering
• Drug Delivery Systems

Background:

• Oral rizatriptan undergoes extensive first-pass metabolism.
• Gastric stasis during migraines delays oral drug absorption.
• Transdermal delivery systems offer a promising alternative to overcome these limitations.

Purpose of the Study:

• To prepare and evaluate rizatriptan-loaded hydrogel microneedles for transdermal delivery.
• To enhance percutaneous permeation and avoid first-pass metabolism of rizatriptan.
• To assess the efficacy and bioavailability of the novel microneedle formulation.

Main Methods:

• Rizatriptan hydrogel microneedles were fabricated using a micromolding technique with varying concentrations of carboxymethyl cellulose and gelatin type A.
• Formulations were characterized for mechanical strength, encapsulation efficiency, and in vitro drug release.
• In vivo skin absorption and relative bioavailability studies were conducted in rats.

Main Results:

• Successfully prepared rizatriptan hydrogel microneedles (F1-F5) with favorable mechanical properties for skin insertion.
• In vitro studies showed high cumulative drug release (93.1-100%) within 24 hours.
• The optimized F3 formulation exhibited superior swelling, mechanical strength, controlled release, and a 179.59% relative bioavailability compared to oral rizatriptan.

Conclusions:

• Rizatriptan-loaded hydrogel microneedles provide an effective transdermal drug delivery system.
• This approach successfully bypasses first-pass metabolism and enhances rizatriptan permeation.
• The developed microneedle system holds significant potential for improved therapeutic effectiveness in migraine management.