Predicting the release profile of small molecules from within the ordered nanostructured lipidic bicontinuous cubic phase using translational diffusion coefficients determined by PFG-NMR

Abstract

The ordered nanostructured lipidic bicontinuous cubic phase has demonstrated potential as a drug release material, due to its ability to encapsulate a wide variety of compounds, which may undergo sustained, diffusion controlled release over time. Control of drug release has been shown to depend on the nanostructural parameters of the lipid mesophase. Herein, the diffusion and release of two amino acids, encapsulated within a range of different lipidic cubic mesophases are investigated. Pulsed-field gradient NMR was used to determine the diffusion coefficient of the encapsulated amino acid, which was found to be correlated with the nanoscale diameter of the water channels within the cubic mesophase. This information was used to predict the release profiles of encapsulated compounds from within the cubic mesophase, which was verified by directly measuring the release of each amino acid in vitro. Predicted release profiles tracked reasonably close to the measured release profiles, indicating that NMR determined diffusion measurements can be used to predict release profiles.