Dissolving polyvinylpyrrolidone-based microneedle systems for in-vitro delivery of sumatriptan succinate

Eur J Pharm Sci. 2018 Mar 1:114:84-92. doi: 10.1016/j.ejps.2017.11.031. Epub 2017 Dec 15.

Abstract

In-vitro permeation studies were conducted to assess the feasibility of fabricating dissolving-microneedle-array systems to release sumatriptan succinate. The formulations consisted mainly of the encapsulated active ingredient and a water-soluble biologically compatible polymer, polyvinylpyrrolidone (PVP), approved by the U.S. Food and Drug Administration (FDA). Tests with Franz-type diffusion cells and Göttingen minipig skins showed an increase of the transdermal flux compared to passive diffusion. A preparation, containing 30% by mass of PVP and 8.7mg sumatriptan, produced a delivery rate of 395±31μg/cm2h over a 7-hour period after a negligible lag time of approximately 39min. Theoretically, a 10.7cm2 microneedle-array patch loaded with 118.8mg of the drug would provide the required plasma concentration, 72ng/mL, for nearly 7h.

Keywords: Controlled release; Diffusion; Dissolving microneedles; Göttingen minipig; Polyvinylpyrrolidone; Sumatriptan succinate.

MeSH terms

  • Animals
  • Drug Delivery Systems / methods*
  • Female
  • Microinjections / methods*
  • Organ Culture Techniques
  • Pharmaceutic Aids / administration & dosage
  • Pharmaceutic Aids / metabolism
  • Povidone / administration & dosage
  • Povidone / metabolism*
  • Skin Absorption / drug effects
  • Skin Absorption / physiology*
  • Solubility
  • Sumatriptan / administration & dosage
  • Sumatriptan / metabolism*
  • Swine
  • Swine, Miniature
  • Vasoconstrictor Agents / administration & dosage
  • Vasoconstrictor Agents / metabolism

Substances

  • Pharmaceutic Aids
  • Vasoconstrictor Agents
  • Sumatriptan
  • Povidone