School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou, 510006, People's Republic of China.
Dongguan Institute of Guangzhou University of Chinese Medicine, Dongguan, 523808, People's Republic of China.
Int J Nanomedicine. 2023 Jul 26;18:4101-4120. doi: 10.2147/IJN.S409513. eCollection 2023.
Berberine (BBR) is extensively studied as an outstanding anti-hyperuricemia drug. However, the clinical application of BBR was limited due to its poor absorption and low bioavailability. Therefore, there is an urgent necessity to find a novel drug formulation to address the issues of BBR in clinical application.
Herein, we conducted the solubility, characterization experiments to verify whether BBR and sodium taurocholate (STC) self-assembled nanoparticles (STC@BBR-SANPs) could form. Furthermore, we proceeded the release experiment in vitro and in vivo to investigate the drug release effect. Finally, we explored the therapeutic effect of STC@BBR-SANPs on hyperuricemia (HUA) through morphological observation of organs and measurement of related indicators.
The solubility, particle size, scanning electron microscopy (SEM), and stability studies showed that the stable STC@BBR-SANPs could be formed in the BBR-STC system at ratio of 1:4. Meanwhile, the tissue distribution experiments revealed that the STC@BBR-SANPs could accelerate the absorption and distribution of BBR. In addition, the pharmacology study demonstrated that both BBR and STC@BBR-SANPs exhibited favorable anti-HUA effects and nephroprotective effects, while STC@BBR-SANPs showed better therapeutic action than that of BBR.
This work indicated that STC@BBR-SANPs can be self-assembly formed, and exerts excellent uric acid-lowering effect. STC@BBR-SANPs can help to solve the problems of poor solubility and low absorption rate of BBR in clinical use, and provide a new perspective for the future development of BBR.
小檗碱(BBR)作为一种出色的抗高尿酸血症药物得到了广泛研究。然而,由于其吸收不良和生物利用度低,BBR 的临床应用受到限制。因此,迫切需要寻找新的药物制剂来解决 BBR 在临床应用中的问题。
本研究通过溶解度、表征实验来验证 BBR 和牛磺胆酸钠(STC)是否自组装成纳米粒(STC@BBR-SANPs)。此外,我们进行了体外和体内释放实验来研究药物释放效果。最后,通过观察器官形态和测量相关指标来探讨 STC@BBR-SANPs 对高尿酸血症(HUA)的治疗作用。
溶解度、粒径、扫描电子显微镜(SEM)和稳定性研究表明,在 BBR-STC 系统中,当比例为 1:4 时,可以形成稳定的 STC@BBR-SANPs。同时,组织分布实验表明,STC@BBR-SANPs 可以加速 BBR 的吸收和分布。此外,药理学研究表明,BBR 和 STC@BBR-SANPs 均具有良好的抗 HUA 作用和肾脏保护作用,而 STC@BBR-SANPs 的治疗作用优于 BBR。
本研究表明 STC@BBR-SANPs 可以自组装形成,并具有优异的降尿酸作用。STC@BBR-SANPs 可以帮助解决 BBR 在临床应用中溶解度差和吸收率低的问题,为 BBR 的未来发展提供了新的视角。