AC and DC electrospinning of hydroxypropylmethylcellulose with polyethylene oxides as secondary polymer for improved drug dissolution

Int J Pharm. 2016 May 30;505(1-2):159-66. doi: 10.1016/j.ijpharm.2016.03.024. Epub 2016 Mar 17.

Abstract

Alternating current electrospinning (ACES) capable to reach multiple times higher specific productivities than widely used direct current electrospinning (DCES) was investigated and compared with DCES to prepare drug-loaded formulations based on one of the most widespread polymeric matrix used for commercialized pharmaceutical solid dispersions, hydroxypropylmethylcellulose 2910 (HPMC). In order to improve the insufficient spinnability of HPMC (both with ACES and DCES) polyethylene oxide (PEO) as secondary polymer with intense ACES activity was introduced into the electrospinning solution. Different grades of this polymer used at as low concentrations in the fibers as 0.1% or less enabled the production of high quality HPMC-based fibrous mats without altering its physicochemical properties remarkably. Increasing concentrations of higher molecular weight PEOs led to the thickening of fibers from submicronic diameters to several microns of thickness. ACES fibers loaded with the poorly water-soluble model drug spironolactone were several times thinner than drug-loaded fibers prepared with DCES in spite of the higher feeding rates applied. The amorphous HPMC-based fibers with large surface area enhanced the dissolution of spironolactone significantly, the presence of small amounts of PEO did not affect the dissolution rate. The presented results confirm the diverse applicability of ACES, a novel technique to prepare fibrous drug delivery systems.

Keywords: Dissolution enhancement; Electrospinning; Hypromellose; Nanofibers; Polyethylene oxide.

MeSH terms

  • Chemistry, Pharmaceutical / methods
  • Drug Carriers / chemistry
  • Drug Compounding / methods
  • Drug Delivery Systems*
  • Electricity
  • Hypromellose Derivatives / chemistry*
  • Molecular Weight
  • Polyethylene Glycols / chemistry*
  • Solubility
  • Spironolactone / administration & dosage*
  • Spironolactone / chemistry

Substances

  • Drug Carriers
  • Spironolactone
  • Hypromellose Derivatives
  • Polyethylene Glycols