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Abstract：
Fibroin nanoparticles (FNP) have been employed in numerous biomedical applications. However, limited research has focused on the oral delivery of FNP and in-depth molecular interactions between the encapsulated drug and FNP. Therefore, this work developed the FNP, functionalized with poly(vinyl alcohol) (PVA), to orally deliver the zwitterionic ciprofloxacin, focused on the molecular interactions. The particles were formulated using both desolvation (the drug precipitated during the particles formulation) and adsorption (the drug adsorbed on the particles surfaces) methods. The optimal formula possessed a size of ~630 nm with narrow size distribution (measured by DLS method), spherical shape (determined by SEM), and moderate drug loading (confirmed by FT-IR, XRD, and DSC techniques) of ~50% for the desolvation method and ~43% for the adsorption method. More than 80% of the drug molecules resided on the particle surfaces, mainly via electrostatic forces with fibroin. The drug was physically adsorbed onto FNP, which followed Langmuir model and pseudo second-order kinetics. In the in-vitro simulated gastric condition at pH 1.2, the ciprofloxacin bound strongly with FNP via electrostatic forces, thus hindering the drug release (< 40%). Contrastingly, in the simulated intestinal condition at pH 6.8, the particles could control the drug release rates dependent on the PVA amount, with up to ~100% drug release. Lastly, the particles possessed adequate antibacterial activities on Bacillus subtilis, Escherichia coli, and Salmonella enterica, with MIC of 128, 8, and 32 μg/mL, respectively. In summary, the FNP and PVA functionalized FNP could be a potential oral delivery system for zwitterionic drugs.
摘要：
纤维蛋白纳米颗粒(FNP)已用于许多生物医学应用中。然而,有限的研究集中在FNP的口服递送以及包封药物与FNP之间的深入分子相互作用。因此,这项工作开发了FNP，用聚乙烯醇(PVA)官能化，口服两性离子环丙沙星，集中在分子相互作用上。使用去溶剂化(药物在颗粒配制期间沉淀)和吸附(药物吸附在颗粒表面上)方法来配制颗粒。最佳配方尺寸为~630nm,尺寸分布窄(DLS法测定),球形（通过SEM确定），和中等载药量(通过FT-IR确认，XRD,和DSC技术）的去溶剂化法为〜50％，吸附法为〜43％。超过80％的药物分子位于颗粒表面，主要通过与丝心蛋白的静电力。药物物理吸附在FNP上，遵循Langmuir模型和伪二阶动力学。在pH1.2的体外模拟胃条件下，环丙沙星通过静电力与FNP强烈结合，从而阻碍药物释放（<40％）。相反，在pH6.8的模拟肠道条件下，该颗粒可以根据PVA的量控制药物释放速率，具有高达~100%的药物释放。最后,颗粒对枯草芽孢杆菌具有足够的抑菌活性，大肠杆菌,和肠沙门氏菌,MIC为128、8和32μg/mL，分别。总之,FNP和PVA功能化的FNP可能是两性离子药物的潜在口服给药系统。
