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自组装纳米粒子结合小檗碱和牛磺胆酸钠增强抗高尿酸血症作用。

Self-Assembled nanoparticles Combining Berberine and Sodium Taurocholate for Enhanced Anti-Hyperuricemia Effect.

机构信息

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.

出版信息

Int J Nanomedicine. 2023 Jul 26;18:4101-4120. doi: 10.2147/IJN.S409513. eCollection 2023.

Abstract

PROPOSE

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.

METHODS

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.

RESULTS

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.

CONCLUSION

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.

摘要

目的

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。

方法

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。

结果

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。

结论

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d65c/10387259/7a5b7b7e3aad/IJN-18-4101-g0001.jpg

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