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Atypical effects of incorporated surfactants on stability and dissolution properties of amorphous polymeric dispersions

Research output: Contribution to journalArticle

Hisham Al-Obaidi, M. Jayne Lawrence, Graham Buckton

Original languageEnglish
Pages (from-to)1373-1383
Number of pages11
JournalJournal of Pharmacy and Pharmacology
Volume68
Issue number11
Early online date2 Oct 2016
DOIs
Publication statusPublished - 1 Nov 2016

King's Authors

Abstract

Objectives: To understand the impact of ionic and non-ionic surfactants on the dissolution and stability properties of amorphous polymeric dispersions using griseofulvin (GF) as a model for poorly soluble drugs. Methods: Solid dispersions of the poorly water-soluble drug, griseofulvin (GF) and the polymers, poly(vinylpyrrolidone) (PVP) and poly(2-hydroxypropyl methacrylate) (PHPMA), have been prepared by spray drying and bead milling and the effect of the ionic and non-ionic surfactants, namely sodium dodecyl sulphate (SDS) and Tween-80, on the physico-chemical properties of the solid dispersions studied. Key findings: The X-ray powder diffraction data and hot-stage microscopy showed a fast re-crystallisation of GF. While dynamic vapour sorption (DVS) measurements indicated an increased water uptake, slow dissolution rates were observed for the solid dispersions incorporating surfactants. The order by which surfactants free dispersions were prepared seemed critical as indicated by DVS and thermal analysis. Dispersions prepared by milling with SDS showed significantly better stability than spray-dried dispersions (drug remained amorphous for more than 6 months) as well as improved dissolution profile. Conclusions: We suggest that surfactants can hinder the dissolution by promoting aggregation of polymeric chains, however that effect depends mainly on how the particles were prepared.

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