Lipid Nanocarriers Overlaid with Chitosan for Brain Delivery of Berberine via the Nasal Route.
Lipid Nanocarriers Overlaid with Chitosan for Brain Delivery of Berberine via the Nasal Route.
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DOI：
10.3390/ph15030281
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发表时间：
2022-02-24
期刊：
影响因子：
--
通讯作者：
Eid HM
中科院分区：
文献类型：
--
作者：
Abo El-Enin HA;Elkomy MH;Naguib IA;Ahmed MF;Alsaidan OA;Alsalahat I;Ghoneim MM;Eid HM
本研究旨在设计、优化和评价壳聚糖覆盖的小檗碱纳米结构脂质载体（BER-CTS-NLC），用于通过鼻内途径进行有效的脑递送。通过热均质和超声处理策略配制含小檗碱的纳米结构脂质载体（BER-NLC），并针对各种因果变量（包括单硬脂酸甘油酯（固体脂质）的量、泊洛沙姆407（表面活性剂）浓度和油酸（液体脂质）的量）对颗粒大小、包封率和24 h后的总药物释放的影响进行优化。然后用壳聚糖涂覆最佳BER-NLC制剂。它们的直径，在体外释放，表面电荷，形态，离体渗透性，pH值，组织学，和在体内（药代动力学和脑摄取）参数进行了估计。BER-CTS-NLC具有180.9 ± 4.3 nm的尺寸、持续释放特性、36.8 mV的正表面电荷和增强的通过鼻粘膜的离体渗透。组织病理学评估显示，BER-CTS-NLC系统用于鼻腔递送是安全的。药代动力学和脑蓄积实验表明，鼻内用BER-CTS-NLC治疗的动物在脑中具有显著更高的药物水平。与BER溶液（IN）相比，BER-CTS-NLC（IN）的30分钟时BER脑/血液水平的比率、AUC脑/AUC血液、药物转运百分比和药物靶向效率更高，表明增强的脑靶向。据推测，优化的纳米颗粒系统是一种成功的方法，用于增强BER在治疗CNS疾病，如阿尔茨海默病，通过鼻内治疗的效果。
This research aimed to design, optimize, and evaluate berberine-laden nanostructured lipid carriers overlaid with chitosan (BER-CTS-NLCs) for efficient brain delivery via the intranasal route. The nanostructured lipid carriers containing berberine (BER-NLCs) were formulated via hot homogenization and ultrasonication strategy and optimized for the influence of a variety of causal variables, including the amount of glycerol monostearate (solid lipid), poloxamer 407 (surfactant) concentration, and oleic acid (liquid lipid) amount, on size of the particles, entrapment, and the total drug release after 24 h. The optimal BER-NLCs formulation was then coated with chitosan. Their diameter, in vitro release, surface charge, morphology, ex vivo permeability, pH, histological, and in vivo (pharmacokinetics and brain uptake) parameters were estimated. BER-CTS-NLCs had a size of 180.9 ± 4.3 nm, sustained-release properties, positive surface charge of 36.8 mV, and augmented ex-vivo permeation via nasal mucosa. The histopathological assessment revealed that the BER-CTS-NLCs system is safe for nasal delivery. Pharmacokinetic and brain accumulation experiments showed that animals treated intranasally with BER-CTS-NLCs had substantially greater drug levels in the brain. The ratios of BER brain/blood levels at 30 min, AUCbrain/AUCblood, drug transport percentage, and drug targeting efficiency for BER-CTS-NLCs (IN) were higher compared to BER solution (IN), suggesting enhanced brain targeting. The optimized nanoparticulate system is speculated to be a successful approach for boosting the effect of BER in treating CNS diseases, such as Alzheimer’s disease, through intranasal therapy.
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影响因子：
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作者：
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DOI：
10.3390/molecules16086732
发表时间：
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期刊：
Molecules (Basel, Switzerland)
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