Multicomponent Crystal Systems of Known Antimalarial Drug Molecules

Abstract

Potential drug molecules are often discarded due to poor physicochemical properties and pharmacokinetic profiles. As such, research into the use of multicomponent crystal systems (such as salts and co-crystals) is currently being conducted with the aim of improving the properties of the molecule, without altering the bioactivity of the drug. Although numerous studies have been performed on a wide variety of drug molecules, research with antimalarial drug molecules seems to have been neglected. With many of the current drugs becoming inactive due to resistance, there is an urgent need to find effective drugs with good pharmacokinetic profiles. The objective of this review is therefore to determine the extent to which multicomponent crystal systems have been used in antimalarial chemotherapy and whether this method provides a viable alternative to discarding potential drug candidates.

Mechanochemical synthesis insights and solid-state characterization of quininium aspirinate, a glass-forming drug–drug salt

“…The interplanar angle between adjacent quinoline planes (defined by the mean of 10 atoms) is 64.4 (1) . A similar zigzag chain packing motif involving the same functional groups of quinine has been reported for the quininium saccharinate salt in a 1:1 molar ratio (Bhatt et al, 2005;Clements et al, 2015), which also similarly crystallizes in the space group P2 1 2 1 2 1 (Z = 4), with Figure 4 (a) Hirshfeld surface of the asymmetric unit of I. Normalized contact distances (d norm ) are represented in the scale À0.3 to 0.8. Red, white, and blue colored areas represent regions where the intermolecular contacts are shorter than the sum of the van der Waals radii, at around those values, and longer than them, respectively.…”

Solubility Enhancement of Antidiabetic Drugs Using a Co‐Crystallization Approach

“…Despite these challenges, a lot of research effort has focussed on preparing pharmaceutical co‐crystals of APIs, and this research is summarized in several reviews. [ 12 , 13 , 14 , 15 , 16 , 17 ]…”

“…In addition, the inability to predict the structure of a co‐crystal from its building blocks remains the greatest challenge of the co‐crystal approach and crystal engineering in general. Despite these challenges, a lot of research effort has focussed on preparing pharmaceutical co‐crystals of APIs, and this research is summarized in several reviews [12–17] …”

“…Despite these challenges, a lot of research effort has focussed on preparing pharmaceutical co-crystals of APIs, and this research is summarized in several reviews. [12][13][14][15][16][17] There are a variety of techniques that can be used for the synthesis of co-crystals. These techniques can be divided into solution-based and solid-based methods.…”

Investigation into the Structures and Properties of Multicomponent Crystals Formed from a Series of 7-Chloroquinolines and Aromatic Acids

“…This has led researchers to pursue the formation of salts and cocrystals using a number of drug molecules to determine the effect that this has on some of the physicochemical properties of the drug, such as solubility, thermal stability, bioavailability, and, ultimately, its pharmacokinetic profile. − Despite these results, the use of this method in an attempt to improve some of the physicochemical properties of antimalarial compounds has received little attention …”