Biodegradable nanoparticles for improved kidney bioavailability of rhein: preparation, characterization, plasma, and kidney pharmacokinetics

• Published in: Drug development and industrial pharmacy 2017-11, Vol.43 (11), p.1885-1891
• Main Authors: Wei, Yinghui, Luo, Xiaoting, Guan, Jiani, Ma, Jianping, Zhong, Yicong, Luo, Jingwen, Li, Fanzhu
• Format: Article
• Language: English
• Subjects: Animals; Anthraquinones - chemistry; Anthraquinones - metabolism; Anthraquinones - pharmacokinetics; Biological Availability; Drug Delivery Systems - methods; Kidney - chemistry; Kidney - metabolism; Kidney bioavailability; microdialysis; nanoparticles; Nanoparticles - administration & dosage; Nanoparticles - chemistry; pharmacokinetics; Rats; rhein
• ISSN: 0363-9045; 1520-5762
• DOI: 10.1080/03639045.2017.1353519

The aim of this work is to develop biodegradable nanoparticles for improved kidney bioavailability of rhein (RH). RH-loaded nanoparticles were prepared using an emulsification solvent evaporation method and fully characterized by several techniques. Kidney pharmacokinetics was assessed by implanting a microdialysis probe in rat's kidney cortex. Blood samples were simultaneously collected (via femoral artery) for assessing plasma pharmacokinetics. Optimized nanoparticles were small, with a mean particle size of 132.6 ± 5.95 nm, and homogeneously dispersed. The charge on the particles was nearly zero, the encapsulation efficiency was 62.71 ± 3.02%, and the drug loading was 1.56 ± 0.15%. In vitro release of RH from the nanoparticles showed an initial burst release followed by a sustained release. Plasma and kidney pharmacokinetics showed that encapsulation of RH into nanoparticles significantly increased its kidney bioavailability (AUC kidney /AUC plasma  = 0.586 ± 0.072), clearly indicating that nanoparticles are a promising strategy for kidney drug delivery.