Formulation and characterization of nanoparticle-based ethinyl estradiol transdermal drug delivery system for contraception and menopausal disorders

Pak J Pharm Sci. 2023 Sep;36(5):1543-1552.

Abstract

Nanoparticles based TDDS was employed to overcome the adverse effects of oral contraceptives. A transdermal patch of Ethinyl Estradiol (EE) nanoparticles was aimed to provide sustained release of the drug and lower dosage frequency. The patch was designed with Eudragit-based polymeric films or EE-loaded chitosan nanoparticles poured onto a polyvinyl alcohol backing membrane, with a non-ionic surfactant (span-20) and a plasticizer (n-butyl phthalate) using solvent evaporation method. Nanoparticles were analyzed for their size, morphology, yield and entrapment efficiency. The patches were analyzed for their folding endurance, thickness, weight, drug content, in vitro release pattern, FTIR and DSC. All patches were transparent, having a uniform, smooth surface. The folding endurance of all the patches indicated optimum flexibility. In vitro, release and Ex-Vivo permeation studies showed that F1 containing nanoparticles exhibited the most optimum drug release in 72h (97.6%). The release pattern demonstrated was diffusion controlled. FTIR, DSC studies indicated no interaction between drug and excipients. The accelerated stability studies were performed at 40C and 70% relative humidity for six months. The product was found stable. The developed patches of EE nanoparticles were expected to improve patient compliance by reducing dose frequency and provide optimum therapy by sustained drug release for contraception.

MeSH terms

  • Administration, Cutaneous
  • Contraception
  • Drug Delivery Systems / methods
  • Ethinyl Estradiol
  • Humans
  • Menopause
  • Nanoparticle Drug Delivery System
  • Nanoparticles*
  • Skin Absorption*
  • Transdermal Patch

Substances

  • Ethinyl Estradiol
  • Nanoparticle Drug Delivery System