Open AccessAprepitant Drug in Ternary Pharmaceutical Solid Dispersions with Soluplus® and Poloxamer 188 Prepared by Melt Mixing
Author(s) -
Stavroula Nanaki,
Rodanthi Maria Eleftheriou,
Panagiotis Barmpalexis,
Margaritis Kostoglou,
Evangelos Karavas,
Dimitrios N. Bikiaris
Publication year - 2019
Publication title -
sci
Language(s) - English
Resource type - Journals
ISSN - 2413-4155
DOI - 10.3390/sci1010029
Subject(s) - poloxamer , differential scanning calorimetry , materials science , dissolution , ternary operation , chromatography , chemical engineering , fourier transform infrared spectroscopy , poloxamer 407 , scanning electron microscope , polarized light microscopy , chemistry , nuclear chemistry , polymer , organic chemistry , copolymer , composite material , physics , computer science , engineering , thermodynamics , programming language , optics
In the present study Aprepitant (APT) ternary solid dispersions (SDs) were developed and evaluated for the first time. Specifically, ternary SDs of APT with Poloxamer 188 and Soluplus® (SOL) were prepared via melt mixing and compared to binary APT/Poloxamer 188 and APT/SOL SDs. Initially, combined thermo-gravimetric and hot-stage polarized light microscopy studies indicated that all tested compounds were thermally stable up to 280 °C, while Poloxamer 188 acted as a plasticizer to SOL by significantly reducing the temperature required to fully solubilize the API during SD preparation. Differential scanning calorimetry combined with wide angle X-ray diffraction studies showed that crystalline API was dispersed in both binary and ternary SDs, while Fourier transformation-infrared spectroscopy studies revealed no molecular interactions among the components. Scanning electron microscopy combined with EDAX element analysis showed that the API was dispersed in nano-scale within the polymer matrices, while increasing APT content led to increasing API nano-crystals within the SDs. Finally, dissolution studies showed that the prepared formulations enhanced dissolution of Aprepitant and its mechanism analysis was further studied. A mathematical model was also investigated to evaluate the drug release mechanism