The current work aimed to enhance the oral bioavailability of water-insoluble drug Artemisinin (ART) by the inclusion of ART with hydroxypropyl-β-cyclodextrin (HP-β-CD) and then loaded with porous starch (PS). The preparation conditions of ART HP-β-CD inclusion complex loaded with PS (AHPS) were optimized according to drug loading (DL) and entrapment efficiency (EE). The properties of AHPS were characterized by optical and thermodynamic methods. ART was linked by hydrogen bond to HP-β-CD to form hydrophilic supramolecules, which are loaded into PS under the action of hydrogen bond. The maximum DL and EE of AHPS were about 16.51% and 67.26%, respectively. Then we investigated the physicochemical properties and antimalarial activity of AHPS. The solubility and bioavailability of AHPS at 48 h were higher than ART and market ART piperaquine tablets (APT), and showed better antimalarial activity in vitro and vivo. It provides a new idea for the development and application of fat-soluble drug.
Keywords: Antimalarial activity; Artemisinin; Bioavailability; Hydroxypropyl-β-cyclodextrin; Porous starch.
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