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Pharmaceutics 2018, 10(3), 89; https://doi.org/10.3390/pharmaceutics10030089

Hot Melt Extrusion: Highlighting Physicochemical Factors to Be Investigated While Designing and Optimizing a Hot Melt Extrusion Process

School of Pharmacy, University of Camerino, Via S. Agostino, 62032 Camerino, Italy
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Received: 7 May 2018 / Revised: 22 June 2018 / Accepted: 9 July 2018 / Published: 11 July 2018
(This article belongs to the Special Issue Pharmaceutical Applications of Hot-melt Extrusion)
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Abstract

Hot-melt extrusion (HME) is a well-accepted and extensively studied method for preparing numerous types of drug delivery systems and dosage forms. It offers several advantages: no solvents are required, it is easy to scale up and employ on the industrial level, and, in particular, it offers the possibility of improving drug bioavailability. HME involves the mixing of a drug with one or more excipients, in general polymers and even plasticizers, which can melt, often forming a solid dispersion of the drug in the polymer. The molten mass is extruded and cooled, giving rise to a solid material with designed properties. This process, which can be realized using different kinds of special equipment, may involve modifications in the drug physicochemical properties, such as chemical, thermal and mechanical characteristics thus affecting the drug physicochemical stability and bioavailability. During process optimization, the evaluation of the drug solid state and stability is thus of paramount importance to guarantee stable drug properties for the duration of the drug product shelf life. This manuscript reviews the most important physicochemical factors that should be investigated while designing and optimizing a hot melt extrusion process, and by extension, during the different pre-formulation, formulation and process, and post-formulation phases. It offers a comprehensive evaluation of the chemical and thermal stability of extrudates, the solid physical state of extrudates, possible drug-polymer interactions, the miscibility/solubility of the drug-polymer system, the rheological properties of extrudates, the physicomechanical properties of films produced by hot melt extrusion, and drug particle dissolution from extrudates. It draws upon the last ten years of research, extending inquiry as broadly as possible. View Full-Text
Keywords: hot-melt extrusion; solid state stability; solid dispersion; thermal methods; X-ray powder diffractometry; spectroscopic techniques; microscopic methods; mechanical analyses; dissolution testing hot-melt extrusion; solid state stability; solid dispersion; thermal methods; X-ray powder diffractometry; spectroscopic techniques; microscopic methods; mechanical analyses; dissolution testing
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Censi, R.; Gigliobianco, M.R.; Casadidio, C.; Di Martino, P. Hot Melt Extrusion: Highlighting Physicochemical Factors to Be Investigated While Designing and Optimizing a Hot Melt Extrusion Process. Pharmaceutics 2018, 10, 89.

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