大豆黄素-磷脂复合物自乳化前体药物的设计、体外和体内评价。
Self-emulsifying preconcentrates of daidzein-phospholipid complex: design, in vitro and in vivo appraisal.
机构信息
Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.
Department of Pharmaceutics, Faculty of Pharmacy & Drug Manufacturing, Pharos University in Alexandria, Alexandria, Egypt.
出版信息
Nanomedicine (Lond). 2017 Apr;12(8):893-910. doi: 10.2217/nnm-2016-0387. Epub 2017 Mar 24.
AIM
Self-emulsifying phospholipid-complex preconcentrates (SEPPs) were fabricated to improve oral bioavailability of daidzein (DAI), an anticancer drug with challenging amphiphobic nature and extensive presystemic metabolism.
METHODS
DAI-phosphatidylcholine complex was prepared to enhance DAI lipophilicity and loading in SEPPs. The physicochemical characteristics and the pharmacokinetic behavior in rats were studied.
RESULTS
Surfactant-free SEPP (plain DAI:Phosal 53MCT complex) was monodisperse upon aqueous dilution with nanorange globule size (485 ± 15 nm). Compared with drug suspension, it showed enhanced drug release and 2.38-fold enhanced oral bioavailability with minimized drug-induced intestinal irritation. Addition of 30% surfactant/co-surfactant mixture did not show any significant difference in drug release rate or absorption profile.
CONCLUSION
The highly safe surfactant-free SEPP could be an effective approach to improve DAI oral bioavailability.
目的
自乳化磷脂复合物前体（SEPPs）被制备以提高具有挑战性的两亲性和广泛的前体代谢的抗癌药物大豆苷元（DAI）的口服生物利用度。
方法
制备了 DAI-磷脂复合物以增强 DAI 的亲脂性和 SEPP 中的载药量。研究了其理化性质和在大鼠体内的药代动力学行为。
结果
无表面活性剂的 SEPP（普通 DAI：Phosal 53MCT 复合物）在水稀释后呈单分散纳米级球粒大小（485±15nm）。与药物混悬剂相比，它表现出增强的药物释放和 2.38 倍的口服生物利用度，同时最小化了药物引起的肠道刺激。添加 30%的表面活性剂/助表面活性剂混合物在药物释放速率或吸收特征方面没有显示出任何显著差异。
结论
高度安全的无表面活性剂 SEPP 可能是提高 DAI 口服生物利用度的有效方法。
Zotero 插件