Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin 150040, People's Republic of China; College of Chemistry, Chemical Engineering and Resource Utilization, Northeast Forestry University, Harbin 150040, People's Republic of China; Engineering Research Center of Forest Bio-preparation, Ministry of Education, Northeast Forestry University, Harbin 150040, People's Republic of China; Heilongjiang Provincial Key Laboratory of Ecological Utilization of Forestry-based Active Substances, Harbin 150040, People's Republic of China; National Engineering Laboratory of BioResource EcoUtilization, Harbin 150040, People's Republic of China.
Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin 150040, People's Republic of China; College of Chemistry, Chemical Engineering and Resource Utilization, Northeast Forestry University, Harbin 150040, People's Republic of China; Engineering Research Center of Forest Bio-preparation, Ministry of Education, Northeast Forestry University, Harbin 150040, People's Republic of China; Heilongjiang Provincial Key Laboratory of Ecological Utilization of Forestry-based Active Substances, Harbin 150040, People's Republic of China; National Engineering Laboratory of BioResource EcoUtilization, Harbin 150040, People's Republic of China.
Int J Biol Macromol. 2022 Jun 30;211:207-217. doi: 10.1016/j.ijbiomac.2022.04.170. Epub 2022 Apr 28.
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.
本工作旨在通过将青蒿素（ART）与羟丙基-β-环糊精（HP-β-CD）包合，然后负载多孔淀粉（PS），来提高水不溶性药物 ART 的口服生物利用度。根据载药量（DL）和包封率（EE）优化了负载 PS 的 ART HP-β-CD 包合物（AHPS）的制备条件。通过光学和热力学方法对 AHPS 的性质进行了表征。ART 通过氢键与 HP-β-CD 连接形成亲水性超分子，在氢键的作用下将其负载到 PS 中。AHPS 的最大 DL 和 EE 分别约为 16.51%和 67.26%。然后，我们研究了 AHPS 的理化性质和抗疟活性。AHPS 在 48 小时时的溶解度和生物利用度均高于 ART 和市售 ART 哌喹片（APT），并在体外和体内表现出更好的抗疟活性。为脂溶性药物的开发和应用提供了新的思路。
