Biodegradable nanoparticles for improved kidney bioavailability of rhein: preparation,characterization, plasma,and kidney pharmacokinetics |
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Authors: | Yinghui Wei Xiaoting Luo Jiani Guan Jianping Ma Yicong Zhong Jingwen Luo |
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Affiliation: | College of Pharmaceutical Science, Zhejiang Chinese Medical University, Hangzhou, China |
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Abstract: | 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 (AUCkidney/AUCplasma?=?0.586?±?0.072), clearly indicating that nanoparticles are a promising strategy for kidney drug delivery. |
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Keywords: | Kidney bioavailability nanoparticles microdialysis pharmacokinetics rhein |
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