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Article

Evaluation of Dissolution Enhancement of Aprepitant Drug in Ternary Pharmaceutical Solid Dispersions with Soluplus® and Poloxamer 188 Prepared by Melt Mixing

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Laboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, 54124 Thessaloniki, Region of Central Macedonia, Greece
2
Department of Pharmaceutical Technology, School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Region of Central Macedonia, Greece
3
Laboratory of General and Inorganic Chemical Technology, Department of Chemistry, Aristotle University of Thessaloniki, GR-541 24 Thessaloniki, Greece
4
Pharmathen S.A., Pharmaceutical Industry, Dervenakion Str 6, Pallini Attikis, GR-15351 Attiki, Greece
*
Author to whom correspondence should be addressed.
Received: 27 January 2019 / Accepted: 23 February 2019 / Published: 15 August 2019
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. View Full-Text
Keywords: Aprepitant; soluplus; poloxamer 188; ternary solid dispersions; hot-melt mixing; dissolution enhancement Aprepitant; soluplus; poloxamer 188; ternary solid dispersions; hot-melt mixing; dissolution enhancement
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MDPI and ACS Style

Nanaki, S.; Eleftheriou, R.M.; Barmpalexis, P.; Kostoglou, M.; Karavas, E.; Bikiaris, D. Evaluation of Dissolution Enhancement of Aprepitant Drug in Ternary Pharmaceutical Solid Dispersions with Soluplus® and Poloxamer 188 Prepared by Melt Mixing. Sci 2019, 1, 48. https://doi.org/10.3390/sci1020048

AMA Style

Nanaki S, Eleftheriou RM, Barmpalexis P, Kostoglou M, Karavas E, Bikiaris D. Evaluation of Dissolution Enhancement of Aprepitant Drug in Ternary Pharmaceutical Solid Dispersions with Soluplus® and Poloxamer 188 Prepared by Melt Mixing. Sci. 2019; 1(2):48. https://doi.org/10.3390/sci1020048

Chicago/Turabian Style

Nanaki, Stavroula, Rodanthi M. Eleftheriou, Panagiotis Barmpalexis, Margaritis Kostoglou, Evangelos Karavas, and Dimitrios Bikiaris. 2019. "Evaluation of Dissolution Enhancement of Aprepitant Drug in Ternary Pharmaceutical Solid Dispersions with Soluplus® and Poloxamer 188 Prepared by Melt Mixing" Sci 1, no. 2: 48. https://doi.org/10.3390/sci1020048

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