Dissolving Microneedles Patch: A Promising Approach for Advancing Transdermal Delivery of Antischizophrenic Drug

J Pharm Sci. 2024 Oct;113(10):3078-3087. doi: 10.1016/j.xphs.2024.08.011. Epub 2024 Aug 16.

Abstract

Objective: Microneedles (MNs) are minimally invasive transdermal drug delivery systems capable of penetrating the stratum corneum to overcome the barrier properties. The primary objective of this research was to prepare dissolving microneedle patches (DMNP) loaded with quetiapine (QTP).

Methods: DMNP were fabricated employing the solvent casting technique, utilizing various polymer feed ratios including polyvinyl alcohol (PVA), polyvinylpyrrolidone K30 (PVP-K30), and polylactide-co-glycolide (PLGA) polymers. The loaded DMNP with QTP underwent a comprehensive characterization process encompassing assessments for compatibility, thickness, insertion potential, morphology, thermal behavior, X-ray diffraction, ex-vivo permeation, skin irritation, and histopathological changes.

Results: FTIR studies confirmed the compatibility of QTP with the microneedle patch composites. The thickness of the drug-loaded DMNP ranged from 0.67 mm to 0.97 mm. These microneedles exhibited an impressive penetration depth of 480 μm, with over 80% of the needles maintaining their original shape after piercing Parafilm-M. SEM analysis of the optimized DMNP-2 revealed the formation of sharp-tipped and uniformly surfaced needles, measuring 570 μm in length. Remarkably, the microneedles did not elicit any signs of irritation upon application of the prepared DMNP. The DMNP-2 showcased an impressive cumulative ex-vivo permeation of QTP, reaching 17.82 µg/cm2/hr. Additionally, histopathological assessment of vital organs in rabbits attested to the safety profile of the formulated microneedle patches.

Conclusions: In conclusion, the developed microneedle patch represents a promising strategy for enhancing the transdermal delivery of QTP. This innovative approach has the potential to increase patient compliance, offering a more efficient and patient-friendly method of administering QTP.

Keywords: Dissolving microneedles patch; Permeation potential; Quetiapine; Toxicity studies; Transdermal drug delivery.

MeSH terms

  • Administration, Cutaneous*
  • Animals
  • Drug Delivery Systems* / methods
  • Microinjections / instrumentation
  • Microinjections / methods
  • Needles*
  • Quetiapine Fumarate / administration & dosage
  • Quetiapine Fumarate / pharmacokinetics
  • Rabbits
  • Skin / drug effects
  • Skin / metabolism
  • Skin Absorption* / drug effects
  • Solubility
  • Transdermal Patch*

Substances

  • Quetiapine Fumarate