Dissolution rate and stability study of flavanone aglycones, naringenin and hesperetin, by drug delivery systems based on polyvinylpyrrolidone (PVP) nanodispersions

Drug Dev Ind Pharm. 2010 Mar;36(3):292-301. doi: 10.1080/03639040903140589.

Abstract

Objective: To study the dissolution behavior, the release mechanism and the stability of nanodispersion system of aglycones with PVP.

Methods: The nanodispersion system of polyvinylpyrrolidone (PVP)/naringenin-hesperetin was prepared using the solvent evaporation method. The chemical stability (compatibility) of naringenin and hesperetin in the prepared dispersions was studied under accelerated conditions for 3 months. The evaluation of physical stability was performed by X-ray diffraction analysis (XRD) and by comparing the dissolution profile before and after storage at high temperature and moisture (40 masculineC, RH 75%).

Results: The dissolution rate of naringenin and hesperetin released was dramatically increased in the nanodispersion system of PVP/naringenin-hesperetin (80/20, w/w). The release mechanism of both flavanone aglycones was better described by the diffusion model (Higuchi model). Also it was found that the rate-limiting step that controlled the release of naringenin and hesperetin in the nanodispersion system was dissolution of the carrier (PVP).

Conclusions: During accelerated degradation analysis, for 3 months at high temperature and moisture, PVP nanodispersion system showed enhanced chemical compatibility and physical stability. The physical evaluation (obtained from XRD analysis) of PVP/naringenin-hesperetin (80/20, w/w) in the selected storage conditions did not show any crystallization of flavanone aglycones in the PVP nanodispersion system or any change in their release profile.

MeSH terms

  • Capsules
  • Chemistry, Pharmaceutical
  • Diffusion
  • Drug Compounding / methods
  • Drug Delivery Systems*
  • Drug Stability
  • Excipients / chemistry
  • Flavanones / analysis
  • Flavanones / chemistry*
  • Hesperidin / analysis
  • Hesperidin / chemistry*
  • Hot Temperature / adverse effects
  • Kinetics
  • Models, Chemical
  • Nanotechnology*
  • Pharmaceutic Aids / chemistry*
  • Povidone / chemistry*
  • Solubility
  • Suspensions
  • Tablets
  • Time Factors
  • Water / adverse effects

Substances

  • Capsules
  • Excipients
  • Flavanones
  • Pharmaceutic Aids
  • Suspensions
  • Tablets
  • Water
  • Hesperidin
  • Povidone
  • naringenin
  • hesperetin