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

IF 3 4区 医学 Q2 CHEMISTRY, APPLIED
Hany G Attia, Maha E Elmataeeshy, Mohamed Aleraky, Samar R Saleh, Doaa A Ghareeb, Maha A El Demellawy, Hanan M El-Nahas, Tarek M Ibrahim
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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 in-vitro release were estimated. In-vitro 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 Cmax 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.

通过不同给药途径评估盐酸小檗碱嵌入白蛋白纳米颗粒的药代动力学和神经保护作用:大鼠体内对比研究。
本研究旨在评估特征明确的小檗碱-牛血清白蛋白(BBR-BSA)纳米颗粒的药代动力学和神经保护作用。小檗碱-牛血清白蛋白(BBR-BSA)纳米颗粒由脱溶法生成。对其包封效率、负载能力、粒度、多分散指数、表面形态、热稳定性和体外释放进行了估算。还进行了体外药代动力学和组织分布研究。评估了它们对脂多糖诱导的神经变性的神经保护作用。BBR-BSA 纳米粒子的粒径(202.60 ± 1.20 nm)和包埋效率(57.00 ± 1.56%)均令人满意。舌下和鼻内途径的药代动力学血浆曲线高于其他途径,0.75 h时的Cmax值分别为(444 ± 77.79和259 ± 42.41 ng/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剂、促炎症、淀粉样蛋白生成生物标志物和大脑结构,从而保护大脑。总之,鼻内和舌下含服 BBR-BSA 纳米粒子可预防神经炎症和神经变性。
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来源期刊
Journal of microencapsulation
Journal of microencapsulation 工程技术-工程:化工
CiteScore
6.30
自引率
2.60%
发文量
39
审稿时长
3 months
期刊介绍: The Journal of Microencapsulation is a well-established, peer-reviewed journal dedicated to the publication of original research findings related to the preparation, properties and uses of individually encapsulated novel small particles, as well as significant improvements to tried-and-tested techniques relevant to micro and nano particles and their use in a wide variety of industrial, engineering, pharmaceutical, biotechnology and research applications. Its scope extends beyond conventional microcapsules to all other small particulate systems such as self assembling structures that involve preparative manipulation. The journal covers: Chemistry of encapsulation materials Physics of release through the capsule wall and/or desorption from carrier Techniques of preparation, content and storage Many uses to which microcapsules are put.
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