Enhanced Topical Delivery of Methotrexate via Transferosome-Loaded Microneedle Array Patch: Formulation,...

Area of Science:

• Dermatology and Pharmaceutical Sciences
• Nanotechnology for Drug Delivery
• Biomaterials and Drug Formulation

Background:

• Conventional psoriasis treatments, including methotrexate (MTX), present complications and patient compliance issues due to systemic side effects.
• There is a critical need for innovative topical drug delivery systems to enhance skin permeation and therapeutic efficacy for psoriasis management.
• Microneedle (MN) technology offers a promising avenue for transdermal drug delivery, potentially overcoming limitations of traditional topical formulations.

Purpose of the Study:

• To develop and optimize a novel topical delivery system for methotrexate (MTX) using transferosome-loaded microneedles (MNs) for psoriasis treatment.
• To evaluate the enhanced skin permeation, sustained release, and therapeutic efficacy of the MTX-loaded MN array patch.
• To assess the safety profile by comparing systemic exposure of MTX from the MN patch versus conventional formulations.

Main Methods:

• Fabrication and optimization of transferosomes loaded with methotrexate (MTX) using a design of experiment approach.
• Incorporation of optimized transferosomes into a dissolving microneedle (MN) array patch.
• In vitro, ex vivo, and in vivo evaluation of the MTX-loaded MN array patch, including drug diffusion, release kinetics, skin permeation, and systemic exposure.

Main Results:

• Optimized transferosomes exhibited a mean vesicle diameter of 169.4 nm and an entrapment efficiency of 69%.
• The transferosome-loaded dissolving MN array patch demonstrated significantly enhanced MTX diffusion and sustained release over 24 hours compared to MTX patch and gel.
• In vivo studies showed higher drug accumulation at the application site and reduced systemic MTX exposure with the MN array patch, confirmed by histological assessments of epidermal penetration.

Conclusions:

• Transferosome-loaded microneedles represent a viable and effective strategy for topical methotrexate delivery in psoriasis.
• This novel MN system provides prolonged drug release and enhanced localized therapeutic efficacy while significantly reducing systemic toxicity.
• The developed transferosome-loaded MN array patch offers a promising innovative approach for improved psoriasis management.