Congruent Release of Drug and Polymer from Amorphous Solid Dispersions: Insights into the Role of Drug-Polymer Hydrogen Bonding, Surface Crystallization, and Glass Transition.

Molecular Pharmaceutics
Sugandha SabooLynne S Taylor

Abstract

Drug loading is an important parameter known to impact the release rate of a poorly soluble drug from an amorphous solid dispersion (ASD). Recent studies have shown that small increases in drug loading can dramatically reduce the drug release rate from ASDs prepared with poly(vinylpyrrolidone-co-vinyl acetate) (PVPVA). However, the link between drug physicochemical properties and the drug loading where the release is abruptly compromised is not well understood. This study probes the role of different factors on the relative dissolution rates of drug and polymer from PVPVA-based ASDs as a function of drug loading: (1) the impact of drug-polymer hydrogen bonding interactions on the initial dissolution rate of ASDs, investigated using two structural analogues, indomethacin (IND) and indomethacin methyl ester (INDester), (2) the influence of surface drug crystallization, observed for INDester ASDs, and (3) by changing temperature, the impact of the "wet" glass transition temperature (Tg). Scanning electron microscopy (SEM), with or without energy dispersive X-ray (EDX) analysis, Fourier transform infrared spectroscopy (FTIR), and powder X-ray diffraction (PXRD) were utilized to study the solid-state phase behavior and/or drug enric...Continue Reading

References

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Citations

Dec 22, 2020·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Esther S BochmannBernd Liepold
Jan 8, 2021·International Journal of Pharmaceutics: X·Christian LuebbertGabriele Sadowski
Apr 19, 2021·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Maria C PaisanaAna Mafalda Paiva
Jun 27, 2021·Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy·R SilvaP F Façanha Filho
Sep 16, 2020·Molecular Pharmaceutics·Na LiLynne S Taylor
Dec 18, 2020·Molecular Pharmaceutics·Kweku K Amponsah-EfahRaj Suryanarayanan
Sep 28, 2021·Molecular Pharmaceutics·Mohammad Atif Faiz AfzalJohn C Shelley

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