Microneedle-mediated transdermal delivery of azelaic acid loaded nanostructured lipid carriers for alopecia

Title : Microneedle-mediated transdermal delivery of azelaic acid loaded nanostructured lipid carriers for alopecia

Abstract:

Objective: Alopecia, particularly androgenetic alopecia, leads to progressive hair loss and negatively affects self-esteem and quality of life. Azelaic Acid, with known anti-inflammatory and antiandrogenic properties, suffers from poor skin permeability and instability, limiting its efficacy. The present study aimed to develop and optimize a microneedle-mediated transdermal delivery system of Azelaic Acid-loaded nanostructured lipid carriers (NLCs) to enhance follicular targeting, drug stability, and therapeutic potential.

Methods: NLCs were prepared using glyceryl monostearate and olive oil as solid and liquid lipids, with Tween 80 as the surfactant, employing a hot high-pressure homogenization technique followed by sonication. The formulation was optimized using Box-Behnken Design with three variables: olive oil concentration, homogenization speed, and surfactant amount. Optimized NLCs were incorporated into dissolving microneedle patches fabricated from poly(methyl vinyl ether/maleic acid) and Sylgard® 184 silicone elastomer. The formulations were evaluated for particle size, PDI, zeta potential, entrapment efficiency, in vitro drug release, mechanical strength, insertion capability, and stability under ICH conditions.

Results: Optimized NLCs demonstrated a particle size of ~11.41 nm with uniform distribution (PDI < 0.3) and entrapment efficiency >95%. DSC and FTIR confirmed the absence of drug–excipient interaction. Microneedle patches exhibited excellent mechanical strength (up to 1.2 N), a sharp geometry (height: ~822.69 μm, tip diameter: ~1.23 μm), and rapid dissolution within 9 minutes. In vitro studies showed biphasic drug release over 7 hours. Ex vivo permeation and in vivo studies in Wistar rats confirmed enhanced drug delivery and superior hair regrowth compared to conventional treatments.

Conclusion: The developed microneedle-assisted NLC system effectively enhanced azelaic acid delivery, offering a promising and stable transdermal platform for alopecia management.

Keywords: azelaic acid, nanostructured lipid carriers, Box–Behnken design, Microneedle patch

Biography:

Dr. Saloni Dalwadi is an Assistant Professor in the Department of Pharmaceutics at Anand Pharmacy College, Gujarat, India. She holds a B.Pharm, M.Pharm in Pharmaceutics, and a Ph.D. in Pharmacy from Gujarat Technological University. Her research interests focus on advanced and patient-centric drug delivery systems, nanoparticle drug delivery systems, transdermal drug delivery, microneedles, 3D printing pharmaceuticals, and innovative pharmaceutical formulations. Her doctoral research involved the development and characterization of patient-centric drug delivery systems with an emphasis on transdermal and microneedle-based approaches. She has published research articles in international indexed journals and actively contributes to pharmaceutical research, innovation, teaching, and academic development.