Effect of PVP K-25 on the formation of the naproxen:beta-ciclodextrin complex

Int J Pharm. 2003 Mar 6;253(1-2):97-110. doi: 10.1016/s0378-5173(02)00664-6.

Abstract

The aim of this study was to investigate the effects of the presence of the water-soluble polymer polyvinylpyrrolidone K-25 (MW=24000g/mol) on the complexation of the AINE naproxen, in its sodium salt form, with the beta-cyclodextrin. The data revealed that the polyvinylpyrrolidone K-25 interacts with the drug as well as with the drug:beta-cyclodextrin inclusion complex. The polymer shows more affinity for the inclusion complex, K=(6.67+/-0.292) x 10(-5)M(-1) than for the free drug, (2.08+/-0.208) x 10(-5)M(-1). The presence of different proportions of polymer, in a range 0-1% (w/w) of polyvinylpyrrolidone, does not increase the ability of drug-cyclodextrin complexation but important changes in the driving force of complex formation were detected, depending on the percentage of polyvinylpyrrolidone K-25 present. At low polymer concentrations, the complexation process is driven entropically, while at higher PVP proportions it is enthalpically favored. In the ternary system, polyvinylpyrrolidone K-25 partially or totally coats the drug:beta-cyclodextrin inclusion complex interacting with the beta-cyclodextrin (through hydrogen bonds), and with the naproxen.

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / chemistry*
  • Cyclodextrins / chemistry*
  • Drug Carriers
  • Excipients / chemistry
  • Naproxen / chemistry*
  • Normal Distribution
  • Povidone / chemistry*
  • Solubility
  • Solutions
  • Spectrometry, Fluorescence
  • Spectrophotometry, Ultraviolet
  • Spectroscopy, Fourier Transform Infrared
  • Water
  • beta-Cyclodextrins*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Cyclodextrins
  • Drug Carriers
  • Excipients
  • Solutions
  • beta-Cyclodextrins
  • Water
  • Naproxen
  • Povidone
  • betadex