Role of berberine nanoformulation in epilepsy: A novel therapeutic strategy

IF 2 4区医学 Q3 CLINICAL NEUROLOGY Epilepsy Research Pub Date : 2024-07-18 DOI:10.1016/j.eplepsyres.2024.107419

Lekha Saha , Puja kumari , V.R. Sinha , Vipasha Gautam , Lavjot Kaur , Sunil Sharma , Amitava Chakrabarti

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Abstract

The aim of the present study was to develop a novel formulation of berberine (BBR) and demonstrate its anti-seizure effect in pentylenetetrazole (PTZ) induced kindling model in rats. Nanoparticles of BBR were formulated using Poly Lactic-co-Glycolic Acid (PLGA) as a polymer. Emulsification and solvent evaporation technique was used. PTZ induced kindling model in male wistar rat was used to demonstrate the anti-seizure effect of nano-BBR. The particle size obtained for the final formulation was 242.8 ± 67.35 nm with a PDI of 0.140 ± 0.01. PLGA encapsulated BBR nanoparticles showed the % encapsulation efficiency of 87.33 ± 2.42 % and % drug loading of 48.47 ± 1.34 %. In-vitro drug release data showed sustained release of nano-BBR as compared to BBR. Kinetic study data showed increase in AUC of nano-BBR (35,429.46 h.ng/ml) as compared to BBR (28,211.07 h.ng/ml). Cmax for nano- BBR (2251.90 ng/ml) is approximately 1.6 times greater than BBR (1505.50 ng/ml). Nano- BBR has shown the significant effect on the seizure score. The PLGA encapsulated berberine nanoparticles were prepared by an innovative simple method and offers excellent potential as an antiepileptic agent.

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小檗碱纳米制剂在癫痫中的作用：新型治疗策略

本研究旨在开发小檗碱（BBR）的新型制剂，并证明其在戊四唑（PTZ）诱导的大鼠激惹模型中的抗癫痫效果。以聚乳甘酸（PLGA）为聚合物配制了小檗碱纳米颗粒。采用了乳化和溶剂蒸发技术。用雄性wistar大鼠PTZ诱导的电击模型来证明纳米BBR的抗癫痫效果。最终制剂的粒径为 242.8 ± 67.35 nm，PDI 为 0.140 ± 0.01。PLGA 封装的 BBR 纳米粒子的封装效率为 87.33 ± 2.42%，药物负载率为 48.47 ± 1.34%。体外药物释放数据显示，与 BBR 相比，纳米 BBR 可持续释放药物。动力学研究数据显示，与 BBR（28,211.07 h.ng/ml）相比，纳米 BBR 的 AUC（35,429.46 h.ng/ml）有所增加。纳米 BBR 的 Cmax（2251.90 纳克/毫升）约为 BBR（1505.50 纳克/毫升）的 1.6 倍。纳米小檗碱对癫痫发作评分有明显影响。采用创新的简单方法制备的 PLGA 封装小檗碱纳米粒子具有作为抗癫痫药物的巨大潜力。

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来源期刊

Epilepsy Research 医学-临床神经学

CiteScore

0.10

自引率

4.50%

发文量

143

审稿时长

62 days

期刊介绍： Epilepsy Research provides for publication of high quality articles in both basic and clinical epilepsy research, with a special emphasis on translational research that ultimately relates to epilepsy as a human condition. The journal is intended to provide a forum for reporting the best and most rigorous epilepsy research from all disciplines ranging from biophysics and molecular biology to epidemiological and psychosocial research. As such the journal will publish original papers relevant to epilepsy from any scientific discipline and also studies of a multidisciplinary nature. Clinical and experimental research papers adopting fresh conceptual approaches to the study of epilepsy and its treatment are encouraged. The overriding criteria for publication are novelty, significant clinical or experimental relevance, and interest to a multidisciplinary audience in the broad arena of epilepsy. Review articles focused on any topic of epilepsy research will also be considered, but only if they present an exceptionally clear synthesis of current knowledge and future directions of a research area, based on a critical assessment of the available data or on hypotheses that are likely to stimulate more critical thinking and further advances in an area of epilepsy research.