Abstract

A model was previously derived to predict in vitro dissolution of drug into surfactant solution and showed good predictability for pharmaceutical surfactants, where surfactant-mediated enhanced drug dissolution was several fold less than enhanced solubility (about 3-fold or less) due to drug-loaded micelles exhibiting slower diffusivity than free drug. The present objective was to quantitatively assess the contributions of biorelevant media-mediated solubility and diffusivity on enhanced drug dissolution in FeSSGF and FeSSIF-V2. Three poorly water soluble drugs were subjected to dissolution into FeSSGF and FeSSIF-V2, as well as their corresponding “surfactant-free” media. Solubility and laser diffraction analysis of drug in FeSSGF and dynamic light-scattering studies (DLS) of drug in FeSSIF-V2 were conducted. Results showed drug-saturated FeSSGF globules and FeSSIF-V2 mixed micelles were large and slow diffusing (diffusivities of about 1×10−9 and 7×10−8 cm2/s, respectively), compared to free drug (about 7×10−6 cm2/s) and drug-bound micelles from pharmaceutical surfactants (about 0.5-1×10−6 cm2/s). Of the three drugs, griseofulvin exhibited the greatest biorelevant media-enhanced solubility and dissolution (652-fold and 6.23-fold respectively in FeSSGF, and 190-fold and 12.7-fold respectively in FeSSIF-V2), but slow colloid diffusivity markedly attenuated large solubility benefits, particularly in FeSSGF.

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