Thermal Stability of Amorphous Solid Dispersions

Amorphous solid dispersion drug delivery systems (ASD DDS) were proved to be efficient for the enhancement of solubility and bioavailability of poorly water-soluble drugs. One of the major keys for successful preparation of ASD is the selection of appropriate excipients, mostly polymers, which have a crucial role in improving drug solubility and its physical stability. Even though, excipients should be chemically inert, there is some evidence that polymers can affect the thermal stability of active pharmaceutical ingredients (API). The thermal stability of a drug is closely related to the shelf-life of pharmaceutical products and therefore it is a matter of high pharmaceutical relevance. An overview of thermal stability of amorphous solids is provided in this paper. Evaluation of thermal stability of amorphous solid dispersion is perceived from the physicochemical perspective, from a kinetic (motions) and thermodynamic (energy) point of view, focusing on activation energy and fragility, as well all other relevant parameters for ASD design, with a glance on computational kinetic analysis of solid-state decomposition.

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or continue reading here: Jelić, D. Thermal Stability of Amorphous Solid Dispersions. Molecules 2021, 26, 238.

Keywords: amorphous solid dispersion of drug; thermal stability; polymers; kinetics; kinetic analysis

ConclusionsStability of amorphous solid dispersions is one of the most intriguing and investigating topic in the field of the drug development. An overview of thermal stability provided here highlights its intrinsic characteristic connected with drug stability, both chemical and physical. Overall, thermal stability is important for the thermal behavior of drug, thermal decomposition of drug and its products, compatibility/incompatibility between API and excipients, and solubility potential and its shelf-life, which are the most important challenges in the drug development. Furthermore, one should not take for granted that the drug-polymer interaction does not affect the thermal stability of drug. This review aimed to put an applicative feature of solid-state kinetics, which might give quantified predictions of stability of ASD via kinetic and thermodynamic contributions, since activation energy and fragility can be used as successful indicators for poor stability of ASD.

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