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载姜黄素的双靶向褐藻糖胶/壳聚糖纳米载体经鼻腔给药抑制脑炎症。

Curcumin-laden dual-targeting fucoidan/chitosan nanocarriers for inhibiting brain inflammation via intranasal delivery.

机构信息

Department of Chemical and Materials Engineering, Tamkang University, New Taipei City, Taiwan.

College of Life Sciences, Department of Food Science, National Taiwan Ocean University, Keelung, Taiwan.

出版信息

Int J Biol Macromol. 2021 Jun 30;181:835-846. doi: 10.1016/j.ijbiomac.2021.04.045. Epub 2021 Apr 18.

Abstract

Curcumin can reduce the production of brain inflammatory mediators and symptoms of brain diseases. However, a large amount of free curcumin needs to be administered to achieve an effective level in the brain because of its poor water-solubility. Fucoidan and chitosan were reported to respectively target P-selectin and acidic microenvironment expressed by pathologically inflammatory cells/tissues. Herein, the self-assembly of chitosan and fucoidan which could encapsulate curcumin was developed to form the multi-stimuli-responsive nanocarriers, and their pathological pH- and P-selectin-responsive aspects were characterized. Through intranasal delivery to the brain, these curcumin-containing chitosan/fucoidan nanocarriers with dual pH-/P-selectin-targeting properties to the brain lesions improved drug delivery, distribution, and accumulation in the inflammatory brain lesions as evidenced by an augmented inhibitory effect against brain inflammation. This promising multifunctional nanocarrier with a novel drug-delivery route should allow potential clinical biomedical uses by neurosurgeon in the future.

摘要

姜黄素可以减少大脑炎症介质的产生和大脑疾病的症状。然而,由于其水溶性差,需要大量的游离姜黄素才能在大脑中达到有效水平。褐藻聚糖硫酸酯和壳聚糖分别被报道可以靶向 P-选择素和病理炎症细胞/组织表达的酸性微环境。在这里,开发了壳聚糖和褐藻聚糖的自组装,其可以包裹姜黄素,形成多刺激响应纳米载体,并对其病理 pH 和 P-选择素响应方面进行了表征。通过鼻腔递送到大脑,这些具有双重 pH-/P-选择素靶向性的载有姜黄素的壳聚糖/褐藻聚糖纳米载体改善了药物在炎症性大脑病变中的传递、分布和积累,从而增强了对大脑炎症的抑制作用。这种有前途的多功能纳米载体具有新的药物传递途径,未来神经外科医生应该可以将其用于潜在的临床生物医学用途。

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