Enhanced dissolution rate of Ketoprofen by fabricating into smart nanocrystals

Pak J Pharm Sci. 2019 Nov;32(6(Supplementary)):2899-2904.

Abstract

The low bioavailability of Ketoprofen is associated with its hydrophobic nature that can be solved by nanonization. For this purpose, a polymeric solution with drug concentration of 3.5% w/w was formulated. The produced solution was milled for 60 minutes in DENA® mill which contains 0.2μ m yttrium reinforced zirconium beads. The Physicochemical properties, characterization including stability studies of the prepared nanoparticles were carried out using pharmacopeial techniques of zeta potential, PXRD, DSC, SEM and TEM. Results suggest that stable crystalline nanocrystals with a size of 169±1.98nm with PDI of 0.194±0.04 and zeta potential of -22.0±2.25mV were produced. Moreover, enhances in-vitro release rate of 78.6% for the processed Ketoprofen was achieved in first 5 min as compared to raw form and marketed drug which released only 22.9% and 33.1% of drug respectively. The 60 days stability studies at 4oC & 25°C revealed that polymers PVP-K30-HPMC-6cps-SDS were effective in stabilizing the nanocrystals. Comparatively stable ketoprofen nanocrystals were successfully produced by DENA® mill with marked enhanced dissolution rate. It proved a useful for commercialization technique due to high drug concentration and retention of distinct characteristics at large scale.

MeSH terms

  • Chemistry, Pharmaceutical / methods
  • Drug Stability
  • Ketoprofen / chemistry*
  • Methylcellulose / analogs & derivatives
  • Methylcellulose / chemistry
  • Nanoparticles / chemistry*
  • Particle Size
  • Polymers / chemistry
  • Polyvinyls / chemistry
  • Pyrrolidines / chemistry
  • Solubility / drug effects*

Substances

  • Polymers
  • Polyvinyls
  • Pyrrolidines
  • poly(N-vinylpyrrolidine)
  • Methylcellulose
  • hydroxypropyl methylcellulose phthalate
  • Ketoprofen