163
Thomas Mavromoustakos et al. (eds.), Supramolecules in Drug Discovery and Drug Delivery: Methods and Protocols,
Methods in Molecular Biology, vol. 2207, https://doi.org/10.1007/978-1-0716-0920-0_13,
© Springer Science+Business Media, LLC, part of Springer Nature 2021
Chapter 13
Differential Scanning Calorimetry (DSC) on Sartan/
Cyclodextrin Delivery Formulations
Nikolaos Naziris, Maria Chountoulesi, Dimitrios Ntountaniotis,
Thomas Mavromoustakos, and Costas Demetzos
Abstract
Differential scanning calorimetry (DSC) is a widely utilized method for the interactions of drug molecules
with drug delivery systems (DDSs). Herein is described a protocol for studying the interactions and
entrapment efficiency of the prototype sartan losartan and the polydynamic, structurally similar irbesartan
inside the nontoxic 2-hydroxypropyl-β-cyclodextrin (2-HP-β-CD). The thermal scan properties of both
sartan molecules have been studied when physically mixed or complexed with the cyclodextrin. The thermograms indeed showed significant differences between the mixtures and complexes, establishing DSC as
a valuable method to characterize the state of the drugs in these pharmaceutical formulations.
Key words Differential scanning calorimetry, Irbesartan, Losartan, 2-Hydroxypropyl-β-cyclodextrin,
Mixing, Lyophilization, Interactions, Complexation
1 Introduction
Thermal analysis (TA) techniques are widely used in order to study
solid, semisolid, or liquid substances. Some of the commonly studied materials are foods, electronic materials, polymers, organic or
inorganic compounds, biological organisms, and pharmaceuticals
[1]. In pharmaceutical sciences, the most frequently used TA
method is differential scanning calorimetry (DSC), where the heat
flow rate difference between a reference and a sample material is
measured. It is primarily applied on crystalline solids, solid dispersions, and polymeric dosage forms, for the characterization of
polymorphic forms, study of the effects of lyophilization, as well as
kinetics of various phenomena, such as decomposition and accelerated aging [2–4].
There is the heat-flux DSC and the power-compensation DSC,
the main difference of the two being that the first uses one furnace
heater for both samples, applying the same temperature to both
Thomas Mavromoustakos et al. (eds.), Supramolecules in Drug Discovery and Drug Delivery: Methods and Protocols,
Methods in Molecular Biology, vol. 2207, https://doi.org/10.1007/978-1-0716-0920-0_13,
© Springer Science+Business Media, LLC, part of Springer Nature 2021
Chapter 13
Differential Scanning Calorimetry (DSC) on Sartan/
Cyclodextrin Delivery Formulations
Nikolaos Naziris, Maria Chountoulesi, Dimitrios Ntountaniotis,
Thomas Mavromoustakos, and Costas Demetzos
Abstract
Differential scanning calorimetry (DSC) is a widely utilized method for the interactions of drug molecules
with drug delivery systems (DDSs). Herein is described a protocol for studying the interactions and
entrapment efficiency of the prototype sartan losartan and the polydynamic, structurally similar irbesartan
inside the nontoxic 2-hydroxypropyl-β-cyclodextrin (2-HP-β-CD). The thermal scan properties of both
sartan molecules have been studied when physically mixed or complexed with the cyclodextrin. The thermograms indeed showed significant differences between the mixtures and complexes, establishing DSC as
a valuable method to characterize the state of the drugs in these pharmaceutical formulations.
Key words Differential scanning calorimetry, Irbesartan, Losartan, 2-Hydroxypropyl-β-cyclodextrin,
Mixing, Lyophilization, Interactions, Complexation
1 Introduction
Thermal analysis (TA) techniques are widely used in order to study
solid, semisolid, or liquid substances. Some of the commonly studied materials are foods, electronic materials, polymers, organic or
inorganic compounds, biological organisms, and pharmaceuticals
[1]. In pharmaceutical sciences, the most frequently used TA
method is differential scanning calorimetry (DSC), where the heat
flow rate difference between a reference and a sample material is
measured. It is primarily applied on crystalline solids, solid dispersions, and polymeric dosage forms, for the characterization of
polymorphic forms, study of the effects of lyophilization, as well as
kinetics of various phenomena, such as decomposition and accelerated aging [2–4].
There is the heat-flux DSC and the power-compensation DSC,
the main difference of the two being that the first uses one furnace
heater for both samples, applying the same temperature to both