Wei Wei, Zhang Qihong, Su Weike
Department of Pharmacology, Ningxia Medical University, Yinchuan 750004, China.
National Engineering Research Center for Process Development of Active Pharmaceutical Ingredients, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, China.
Pharmaceuticals (Basel). 2025 May 18;18(5):743. doi: 10.3390/ph18050743.
This study was performed to simultaneously improve the solubility, permeability, and pharmacological activity of decoquinate (DQ). A ternary DQ solid dispersion with hydroxypropyl--cyclodextrin (HP--CD) and tea saponin (TS) was mechanochemically prepared to enhance the efficacy of DQ. The encapsulation efficiency of the ternary complex reached 93.51%, and the drug loading was 9.48%. The mean particle size was 90.88 ± 0.44 nm. The polydispersity index was 0.244 ± 0.004, and the zeta potential was -38.81 ± 0.75 mV. The sugar ring moiety formed multiple hydrogen bonds with the surface of HP--CD, creating favorable conditions for the development of a stable ternary complex through sophisticated molecular interactions that facilitated its assembly. In vivo studies demonstrated that the DQ/HP--CD/TS ternary complex drinking water demonstrated superior anticoccidial activity compared to pure DQ and commercial feed formulations against . This innovative mechanochemically synthesized ternary complex demonstrates remarkable promise for improving DQ-based formulations, as it simultaneously boosts aqueous solubility, permeability, and therapeutic efficacy. These synergistic enhancements position the compound as a strong candidate for pharmaceutical development.
本研究旨在同时提高地克珠利(DQ)的溶解度、渗透性和药理活性。通过机械化学法制备了地克珠利与羟丙基-β-环糊精(HP-β-CD)和茶皂素(TS)的三元固体分散体,以增强地克珠利的疗效。三元复合物的包封率达到93.51%,载药量为9.48%。平均粒径为90.88±0.44nm。多分散指数为0.244±0.004,ζ电位为-38.81±0.75mV。糖环部分与HP-β-CD表面形成多个氢键,通过复杂的分子相互作用为稳定三元复合物的形成创造了有利条件,促进了其组装。体内研究表明,与纯地克珠利和商业饲料配方相比,饮用含地克珠利/HP-β-CD/TS三元复合物的水对球虫具有更高的抗球虫活性。这种创新的机械化学合成三元复合物在改进基于地克珠利的制剂方面显示出巨大的潜力,因为它同时提高了水溶性、渗透性和治疗效果。这些协同增强作用使该化合物成为药物开发的有力候选者。