The present study aims at the development, characterization, biocompatibility investigation and oral bioavailability evaluation of ceftriaxone (CFT)-loaded N'-methacryloylisonicotinohydrazide (MIH)-functionalized magnetic nanoparticles (CFT-MIH-MNPs). Atomic force microscopy (AFM) and dynamic light scattering (DLS) showed that the developed CFT loaded MIH-MNPs are spherical, with a measured hydrodynamic size of 184.0 ± 2.7 nm and negative zeta potential values (–20.2 ± 0.4 mV). Fourier transformed infrared spectroscopic (FTIR) analysis revealed interactions between the nanocarrier and the drug. Nanoparticles showed high drug entrapment efficiency (EE) of 79.4% ±1.5%, and the drug was released gradually in vitro and showed prolonged in vitro stability using simulated gastrointestinal tract (GIT) fluids. The formulations were found to be highly biocompatible (up to 100 µg/mL) and hemocompatible (up to 1.0 mg/mL). Using an albino rabbit model, the formulation showed a significant enhancement in drug plasma concentration up to 14.4 ± 1.8 µg/mL in comparison with its control (2.0 ± 0.6 µg/mL). Overall, the developed CFT-MIH-MNPs formulation was promising for provision of high drug entrapment, gradual drug release and suitability for enhancing the oral delivery of CFT.

中文翻译：

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高度官能化的磁性氧化铁纳米颗粒增强头孢曲松钠的口服吸收。

本研究的目的是开发，表征，头孢曲松钠（CFT）负载N'-甲基丙烯酰油烟酰肼（MIH）功能化的磁性纳米粒子（CFT-MIH-MNPs）的生物相容性研究和口服生物利用度评估。原子力显微镜（AFM）和动态光散射（DLS）表明，已开发的加载CFT的MIH-MNP是球形的，测得的流体动力学尺寸为184.0±2.7 nm，ζ电势值为负（–20.2±0.4 mV）。傅立叶变换红外光谱（FTIR）分析揭示了纳米载体与药物之间的相互作用。纳米颗粒显示出79.4％±1.5％的高药物截留效率（EE），并且使用模拟胃肠道（GIT）液体在体外逐渐释放药物并显示出延长的体外稳定性。发现该制剂具有高度生物相容性（最高100 µg / mL）和血液相容性（最高1.0 mg / mL）。使用白化病兔模型，与对照（2.0±0.6 µg / mL）相比，该制剂显示出最高14.4±1.8 µg / mL的血浆血浆浓度显着提高。总体而言，已开发的CFT-MIH-MNPs制剂有望提供高的药物截留率，逐渐的药物释放以及增强CFT口服递送的适用性。