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Elevating Bioavailability of Curcumin via Encapsulation with a Novel Formulation of Artificial Oil Bodies

机译:通过封装与新型人工油体制剂提高姜黄素的生物利用度

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Utilization of curcumin has been limited due to its poor oral bioavailability. Oral bioavailability of hydrophobic compounds might be elevated via encapsulation in artificial seed oil bodies. This study aimed to improve oral bioavailability of curcumin via this encapsulation. Unfortunately, curcumin was indissoluble in various seed oils. A mixed dissolvent formula was used to dissolve curcumin, and the admixture was successfully encapsulated in artificial oil bodies stabilized by recombinant sesame caleosin. The artificial oil bodies of relatively small sizes (150 nm) were stably solidified in the forms of powder and tablet. Oral bioavailability of curcumin with or without encapsulation in artificial oil bodies was assessed in Sprague—Dawley male rats. The results showed that encapsulation of curcumin significantly elevated its bioavailability and provided the highest maximum whole blood concentration (C_(max)), 37 ± 28 ng/mL, in the experimental animals 45 ± 17 min (t_(max)) after oral administration. Relative bioavailability calculated on the basis of the area under the plasma concentration—time curve (AUC) was increased by 47.7 times when curcumin was encapsulated in the artificial oil bodies. This novel formulation of artificial oil bodies seems to possess great potential to encapsulate hydrophobic drugs for oral administration.
机译:由于姜黄素口服生物利用度差,因此其使用受到限制。疏水性化合物的口服生物利用度可通过封装在人造种子油体内来提高。这项研究旨在通过这种封装改善姜黄素的口服生物利用度。不幸的是,姜黄素不溶于各种种子油。使用混合溶剂配方来溶解姜黄素,并将该混合物成功地封装在由重组芝麻古钙素稳定的人造油体中。相对较小尺寸(150 nm)的人造油体以粉末和片剂的形式稳定固化。在Sprague-Dawley雄性大鼠中评估了姜黄素在有或没有胶囊的情况下口服生物利用度。结果表明,姜黄素的封装显着提高了其生物利用度,并在口服后45±17分钟(t_(max))的实验动物中提供了最高的最大全血浓度(C_(max)),为37±28 ng / mL。 。当姜黄素被封装在人造油体中时,基于血浆浓度-时间曲线下的面积(AUC)计算的相对生物利用度增加了47.7倍。这种人造油体的新颖配方似乎具有封装疏水性药物以口服的巨大潜力。

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