Thermal Stability of Amorphous Solid Dispersions

Abstract

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.

Synergistic Antimicrobial Activities of Limonene with Mineral Carriers in LDPE Films for Active Packaging Application

“…In this sense, mineral carriers capable of retaining bioactive molecules by physical and chemical adsorption or interaction with them are promising materials for techniques in which high-temperatures are needed [27,28]. Different release behavior and mass transfer mechanisms can be obtained because of the interactions between the volatile additive, carrier, and polymer.…”

Characterization and Antibacterial Evaluation of Biodegradable Mannose-Conjugated Fe-MIL-88NH2 Composites Containing Vancomycin against Methicillin-Resistant Staphylococcus aureus Strains

“…Powder XRD is the most effective technique for elucidating the structure of nanomaterials. XRD patterns can reveal an abundance of information, from phase composition to crystallite size, and from lattice strain to crystallographic orientation [57]. The main crystalline peaks of the prepared Fe-MIL-88NH 2 were observed at 9.05 • , 10.6 • , 16.9 • , 17.7 • , and 18.9 • , which revealed that the crystal structure of the prepared MOFs was almost consistent with the structure, as reported previously in the literature.…”

Thermal Stability Kinetics and Shelf Life Estimation of the Redox‐Active Therapeutic and Mimic of Superoxide Dismutase Enzyme, Mn(III) meso‐Tetrakis(N‐ethylpyridinium‐2‐yl)porphyrin Chloride (MnTE‐2‐PyPCl5, BMX‐010)

“…Despite the large number of studies dedicated to unravelling the biological and clinical aspects of MnTE-2-PyPCl 5 both in vitro and in vivo [1,[16][17][18]22], studies on the stability of this class of compounds are still somewhat limited [28][29][30]. It is worth noting, however, that information on MnTE-2-PyPCl 5 stability may shed light on the stability of other MnP analogues [28] and likely support protocols on purification, handling, storage, formulation, expiration date, and general use of these compounds [31][32][33][34].…”

“…Thermogravimetric (TG) analyses are important for the evaluation and/or comparison of thermal stabilities of pharmaceutical materials, the study of drug-excipient compatibility in drug products, and the determination of kinetic parameters associated with thermal processes (such as activation energies, frequency factor, and reaction order) [ 31 – 34 , 39 , 40 ]. Overall, this information is useful for the development of pharmaceutical products and quality control [ 32 , 34 , 39 , 41 ]. Studies on the kinetics of thermal degradation are recommended to evaluate the thermal stability of active pharmaceutical ingredients (API) and/or their solid-state pharmaceutic formulations [ 31 – 34 , 39 , 41 , 42 ].…”