Translationale Medizin
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The Possibility of Hot Melt Extruded Decoquinate Becoming the Next Orally Dosing Drug Targeting the Liver Stage of Malaria

Hongxing Wang

Decoquinate (DQ) is a water-insoluble agent with multistage antimalarial activity. A recent report has been published that describes how the Hot Melt Extrusion (HME) approach is applied to prepare solid dispersions of DQ, an Active Pharmaceutical Ingredient (API), to improve oral bioavailability. Instead of using organic solvents to make the dispersion of DQ in polymers, DQ was melt dispersed in polymer excipients at high temperatures without alteration of the structures of all ingredients. It is impossible to suspend DQ in water or an aqueous solution prior to the conversion of DQ to amorphous solid dispersion or solid solution. However, DQ dispersion prepared by HME becomes nanosized particles readily suspended in an aqueous solution, suggesting that drug particles in such dispersion can become available in the digestive tract and accessible to the intestinal surface for absorption. It is hoped that the DQ prepared by HME can be further developed into tablet formulations. The idea is to make tablet medication available for populations in an endemic area or travelers to the area to prevent Plasmodium (P) infection or treat malaria at the early stage (liver stage) so that they can be free of symptoms caused by blood-stage infection. But will this idea work? This brief review may help us know more about DQ.