Wormlike micellar aggregates of saponins from Ilex paraguariensis A. St. Hil. (mate): a characterisation by cryo-TEM, rheology, light scattering and small-angle neutron scattering

J Pharm Sci. 2011 Feb;100(2):536-46. doi: 10.1002/jps.22283. Epub 2010 Nov 2.

Abstract

This work reports the physico-chemical characterisation of the micellar structures formed by a saponin fraction obtained from an important South American species, Ilex paraguariensis (mate). The mate saponin-enriched fraction (MSF) mainly comprises triterpenic glycosides and was obtained from mate green fruits through solid-phase extraction. The physico-chemical studies focused on the determination of the critical micellar concentration (CMC), the size and shape of the micelles, using conventional transmission electronic microscopy (TEM), as well as Cryo-TEM, light scattering and small-angle neutron scattering. The rheological behaviour of the solutions up to 4 wt% was also determined using a controlled-strain rheometer. Finally, the MSF ability to solubilise poorly water-soluble drugs was assayed using carbamazepine and flurbiprofen as basic and weak acidic drug models. Small spherical micelles of around 20 Å radius were observed in the presence of elongated structures with lengths of more than 500 nm, possessing a well-defined CMC of 0.41 g/L. MSF solutions ranging from 0.25 to 4% (w/v) demonstrated a viscoelastic behaviour independent of the concentration. MSF could improve the solubility of carbamazepine in the range of 0.13 to 1.5% (w/v).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cryoelectron Microscopy
  • Fruit / chemistry
  • Ilex paraguariensis / chemistry*
  • Micelles*
  • Microscopy, Electron, Transmission
  • Neutron Diffraction
  • Rheology
  • Saponins / chemistry*
  • Saponins / isolation & purification
  • Scattering, Small Angle
  • Solubility
  • Surface-Active Agents / chemistry*
  • Surface-Active Agents / isolation & purification

Substances

  • Micelles
  • Saponins
  • Surface-Active Agents