Insights into the Role of Polymer-Surfactant Complexes in Drug Solubilisation/Stabilisation During Drug Release from Solid Dispersions

Research output: Contribution to journalArticleScientificpeer-review

Researchers

  • Sheng Qi
  • Steve Roser
  • Karen J. Edler
  • Claudia Pigliacelli

  • Madeleine Rogerson
  • Ilse Weuts
  • Frederic Van Dycke
  • Sigrid Stokbroekx

Research units

  • University of East Anglia
  • University of Bath
  • Johnson and Johnson Pharmaceutical Research and Development
  • SEPS Pharma

Abstract

To evaluate the role of polymer-surfactant interactions in drug solubilisation/stabilisation during the dissolution of spray-dried solid dispersions and their potential impact on in vivo drug solubilisation and absorption.

Dissolution/precipitation tests were performed on spray-dried HPMC-Etravirine solid dispersions to demonstrate the impact of different surfactants on the in vitro performance of the solid dispersions. Interactions between HPMC and bio-relevant and model anionic surfactants (bile salts and SDS respectively) were further characterised using surface tension measurements, fluorescence spectroscopy, DLS and SANS.

Fast and complete dissolution was observed in media containing anionic surfactants with no drug recrystallisation within 4 h. The CMCs of bile salts and SDS were dramatically reduced to lower CACs in the presence of HPMC and Etravirine. The maximum increases of the apparent solubility of Etravirine were with the presence of HPMC and SDS/bile salts. The SANS and DLS results indicated the formation of HPMC-SDS/bile salts complexes which encapsulated/solubilised the drug.

This study has demonstrated the impact HPMC-anionic surfactant interactions have during the dissolution of non-ionic hydrophilic polymer based solid dispersions and has highlighted the potential relevance of this to a fuller understanding of drug solubilisation/stabilisation in vivo.

Details

Original languageEnglish
Pages (from-to)290-302
Number of pages13
JournalPharmaceutical Research
Volume30
Issue number1
Publication statusPublished - Jan 2013
MoE publication typeA1 Journal article-refereed

    Research areas

  • bile salts, polymer-surfactant interaction, poorly water-soluble drugs, solid dispersions, solubilisation, SODIUM DODECYL-SULFATE, NONIONIC CELLULOSE DERIVATIVES, CHARACTERIZATION PRINCIPLES, SUPERSATURATED SOLUTIONS, ETHER C12EO6, HUMAN SKIN, IN-VITRO, POLY(VINYLPYRROLIDONE), MICROCALORIMETRY, BIOAVAILABILITY

ID: 13869856