Levonorgestrel Microneedle Array Patch for Sustained Release Contraception: Formulation, Optimization and In Vivo Characterization

Molecules. 2022 Apr 6;27(7):2349. doi: 10.3390/molecules27072349.

Abstract

Background: The goal of this work was to develop a levonorgestrel liposome-loaded microneedle array patch for contraception.

Methods: Levonorgestrel-loaded liposome was formulated by a solvent injection technique, characterized, and studied.

Results: The formulated liposomes were characterized for particle size (147 ± 8 nm), polydispersity index (0.207 ± 0.03), zeta potential (-23 ± 4.25 mV), drug loading (18 ± 3.22%) and entrapment efficiency (85 ± 4.34%). A cryo high-resolution transmission electron microscopy and cryo field emission gun scanning electron microscopy study showed spherical shaped particles with a smooth surface. The in vitro drug release and in vivo pharmacokinetic study showed sustained behaviour of Levonorgestrel for 28 days.

Conclusion: The levonorgestrel liposome-loaded microneedle array patch showed better contraception than the drug-loaded microneedle array patch.

Keywords: contraception; drug delivery; levonorgestrel; liposomes; microneedle; nanotechnology; sustained-release.

MeSH terms

  • Contraception
  • Delayed-Action Preparations
  • Drug Delivery Systems / methods
  • Levonorgestrel*
  • Liposomes*
  • Particle Size

Substances

  • Delayed-Action Preparations
  • Liposomes
  • Levonorgestrel