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A promising oral fucoidan-based antithrombotic nanosystem: development, activity and safety

机译：基于口腔藻类的抗血红蛋白纳米系统：开发，活动和安全性

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Fucoidan-loaded nanoparticles emerge as great candidates for oral anticoagulant therapy, due to increases in the bioavailability and circulation time of this natural anticoagulant. Crosslinks between chitosan chains are performed using glutaraldehyde to confer higher gastric pH resistance to nanoparticle matrices. In this work, chitosan-fucoidan nanoparticles, without (NpCF) and with glutaraldehyde crosslink (NpCF 1% and NpCF 2%), were prepared to evaluate their anticoagulant, antithrombotic and hemorrhagic profiles. Nanoparticles were characterized by average diameter (AD), polydispersity index, zeta potential, Fourier transform infrared spectroscopy and fucoidan in vitro release. Anticoagulant and antithrombotic activities were determined by in vitro and in vivo models, respectively. Hemorrhagic profile was in vivo evaluated by tail bleeding assay. Preparations showed nanometric and homogeneous ADs. Zeta potentials of NpCF and NpCF 1% were stable over the gastrointestinal pH range, which was confirmed by low fucoidan release in gastric and enteric media. In pH 7.4, NpCF and NpCF 1% demonstrated fucoidan release of 65.5% and 60.6%, respectively, within the first 24 h. In comparison to fucoidan, NpCF and NpCF 1% showed increased in vitro anticoagulant activity. A significant difference in the oral antithrombotic profile of NpCF 1% was found in comparison to fucoidan. Bleeding profile of NpCF and NpCF 1% showed no differences to the control group, indicating the safety of these systems. Surprisingly, the oral antithrombotic profile of commercially available fucoidan, from Fucus vesiculosus, has not been previously determined, which reveals new possibilities. In this work, significant advances were observed in the anticoagulant and antithrombotic profiles of fucoidan through the preparation of NpCF 1%.
机译：由于这种天然抗凝血剂的生物利用度和循环时间增加，岩藻烷纳米颗粒作为口服抗凝血治疗的伟大候选者出现。使用戊二醛进行壳聚糖链之间的交联，以赋予纳米颗粒基质的胃pH抗性更高。在这项工作中，制备壳聚糖 - 岩藻糖烷纳米粒子，没有（NPCF）和戊二醛交联（NPCF 1％和NPCF 2％），以评估它们的抗凝血剂，抗血栓形成和出血性谱。纳米颗粒的特征在于平均直径（Ad），多分散指数，Zeta电位，傅里叶变换红外光谱和Fucoinean体外释放。通过体外和体内模型测定抗凝血剂和抗血栓形成活性。出血性概况通过尾部出血测定评估。制剂显示纳米型和均匀的广告。 NPCF和NPCF 1％的Zeta电位在胃肠道pH范围内稳定，其通过低骨藻释放在胃肠和肠溶介质中的低骨饼释放来证实。在pH7.4中，NPCF和NPCF 1％在前24小时内分别显示出抗果环释放65.5％和60.6％。与Fucoino oina相比，NPCF和NPCF 1％显示体外抗凝活性增加。与岩藻糖烷相比，发现NPCF 1％的口服抗血栓形成曲线的显着差异。 NPCF和NPCF的出血概况1％显示对对照组没有差异，表明这些系统的安全性。令人惊讶的是，从前发现，来自浮藻藻的市售岩藻糖糖的口服抗粘结型概况，揭示了新的可能性。在这项工作中，通过制备NPCF 1％，在抗凝血剂和抗凝血细胞谱中观察到显着进展。

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