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经不同给药途径评估盐酸小檗碱包埋白蛋白纳米粒的药代动力学和神经保护作用:在大鼠中的比较研究。

The assessment of pharmacokinetics and neuroprotective effect of berberine hydrochloride-embedded albumin nanoparticles via various administration routes: comparative studies in rats.

机构信息

Department of Pharmacognosy, College of Pharmacy, Najran University, Najran, Saudi Arabia.

Department of Pharmaceutics, Zagazig University, Zagazig, Egypt.

出版信息

J Microencapsul. 2024 Nov;41(7):576-600. doi: 10.1080/02652048.2024.2395976. Epub 2024 Sep 4.

Abstract

The current study aimed to evaluate the pharmacokinetics and neuroprotective effect of well-characterised berberine-bovine serum albumin (BBR-BSA) nanoparticles. BBR-BSA nanoparticles were generated by desolvation method. Entrapment efficiency, loading capacity, particle size, polydispersity index, surface morphology, thermal stability, and release were estimated. pharmacokinetic and tissue distribution were conducted. Their neuroprotection was evaluated against lipopolysaccharides-induced neurodegeneration. BBR-BSA nanoparticles showed satisfactory particle size (202.60 ± 1.20 nm) and entrapment efficiency (57.00 ± 1.56%). Results confirmed the formation of spheroid-thermal stable nanoparticles with a sustained drug release over 48 h. Sublingual and intranasal routes had higher pharmacokinetic plasma profiles than other routes, with C values at 0.75 h (444 ± 77.79 and 259 ± 42.41 ng/mL, respectively). BBR and its metabolite distribution in the liver and kidney were higher than in plasma. Intranasal and sublingual treatment improves antioxidants, proinflammatory, amyloidogenic biomarkers, and brain architecture, protecting the brain. In conclusion, neuroinflammation and neurodegeneration may be prevented by intranasal and sublingual BBR-BSA nanoparticles.

摘要

本研究旨在评估经过充分表征的黄连素-牛血清白蛋白(BBR-BSA)纳米粒的药代动力学和神经保护作用。BBR-BSA 纳米粒通过去溶剂化法生成。测定包封效率、载药量、粒径、多分散指数、表面形态、热稳定性和释放。进行了药代动力学和组织分布研究。评价了它们对脂多糖诱导的神经退行性变的神经保护作用。BBR-BSA 纳米粒的粒径(202.60±1.20nm)和包封效率(57.00±1.56%)均令人满意。结果证实形成了具有热稳定性的类球形纳米粒,药物可在 48 小时内持续释放。与其他途径相比,舌下和鼻内途径具有更高的药代动力学血浆特征,C 值在 0.75 小时时分别为 444±77.79 和 259±42.41ng/mL。BBR 及其代谢物在肝脏和肾脏中的分布高于在血浆中的分布。鼻内和舌下治疗可改善抗氧化、促炎、淀粉样蛋白生物标志物和大脑结构,从而保护大脑。总之,鼻内和舌下 BBR-BSA 纳米粒可能预防神经炎症和神经退行性变。

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