Deoxycholic acid-functionalised nanoparticles for oral delivery of rhein.
作者： Jingwen Luo , Jiang Sun , Wenjie Yao , Yinghui Wei , Zhishi Xu
DOI: 10.1016/J.EJPS.2021.105713
关键词:
摘要: Rhein (RH) is a candidate for the treatment of kidney diseases. However, clinical application RH impeded by low aqueous solubility and oral bioavailability. Deoxycholic acid-conjugated nanoparticles (DNPs) were prepared ionic interaction enhancing intestinal absorption targeting apical sodium-dependent bile acid transporter in small intestine. Resultant DNPs showed relatively high entrapment efficiency (90.7 ± 0.73)% drug-loading (6.5 0.29)% with particle size approximately 190 nm good overall dispersibility. In vitro release from exhibited sustained pH-dependent profiles. Cellular uptake apparent permeability coefficient (Papp) 3.25- 5.05-fold higher than that suspensions, respectively. An vivo pharmacokinetic study demonstrated significantly enhanced bioavailability when encapsulated DNPs, 2.40- 3.33-fold Cmax AUC0-inf compared to are promising delivery platforms poorly absorbed drugs administration.
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