Fast dissolving paracetamol/caffeine nanofibers prepared by electrospinning

Int J Pharm. 2014 Dec 30;477(1-2):369-79. doi: 10.1016/j.ijpharm.2014.10.036. Epub 2014 Oct 17.

Abstract

A series of polyvinylpyrrolidone fibers loaded with paracetamol (PCM) and caffeine (CAF) was fabricated by electrospinning and explored as potential oral fast-dissolving films. The fibers take the form of uniform cylinders with smooth surfaces, and contain the drugs in the amorphous form. Drug-polymer intermolecular interactions were evidenced by infrared spectroscopy and molecular modeling. The properties of the fiber mats were found to be highly appropriate for the preparation of oral fast dissolving films: their thickness is around 120-130 μm, and the pH after dissolution in deionized water lies in the range of 6.7-7.2. Except at the highest drug loading, the folding endurance of the fibers was found to be >20 times. A flavoring agent can easily be incorporated into the formulation. The fiber mats are all seen to disintegrate completely within 0.5s when added to simulated saliva solution. They release their drug cargo within around 150s in a dissolution test, and to undergo much more rapid dissolution than is seen for the pure drugs. The data reported herein clearly demonstrate that electrospun PCM/CAF fibers comprise excellent candidates for oral fast-dissolving films, which could be particularly useful for children and patients with swallowing difficulties.

Keywords: Caffeine; Caffeine (PubChem CID: 2519); Electrospinning; Fast-dissolving drug delivery system; Nanofiber; Paracetamol; Paracetamol (PubChem CID: 1983); Polyvinylpyrrolidone (PubChem CID: 6917).

MeSH terms

  • Acetaminophen / administration & dosage*
  • Acetaminophen / chemistry
  • Administration, Sublingual
  • Caffeine / administration & dosage*
  • Caffeine / chemistry
  • Drug Combinations
  • Drug Delivery Systems*
  • Drug Liberation
  • Hydrogen-Ion Concentration
  • Microscopy, Electron, Scanning
  • Molecular Structure
  • Nanofibers / chemistry*
  • Solubility
  • Surface Properties
  • Technology, Pharmaceutical / methods*
  • Time Factors

Substances

  • Drug Combinations
  • Acetaminophen
  • Caffeine