Abstract

Gelatin-rosin gum complex nanoparticles (GGR_NPs) have been synthesized by complex coacervation method. The particles were extensively characterized using Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), field emission scanning electron microscopy (FESEM), and particle size analysis based on dynamic light scattering (DLS). The GGR_NP3 were stable and their average particle size was ~ 153 nm. GGR_NPs were evaluated as the carrier matrix for 5-fluoro uracil (5-FU), and the release behavior of 5-FU was examined by swelling and in vitro dissolution tests in simulated gastrointestinal fluid (SGF) for first 2 h followed by 14 h in simulated intestinal fluid (SIF). About 71% drug release was witnessed (SGF = 21%; SIF = 50%) over a time span of 16 h, in contrast to native gelatin or rosin gum where under identical conditions the release exhausted within 7 h and 10 h, respectively. The release profile followed the first-order kinetics and the diffusion exponent (n) values obtained from the Korsemeyer−Peppas model ranged between 0.5 < n < 0.8 (both in SGF and SIF), which indicated non-Fickian diffusion mechanism. A549 cell line was used to carry out MTT assay test for investigating the cell toxicity of the drug-loaded GGR_NP3 (D GGR_NP3) where DGGR_NP3 exhibited greater toxicity as compared to GGR_NP3.

Graphic abstract

中文翻译：

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明胶-松香胶复合物纳米颗粒：5-氟尿嘧啶的制备，表征和结肠靶向递送

摘要

通过复合凝聚法合成了明胶-松香胶复合纳米颗粒（GGR _NPs）。使用傅立叶变换红外光谱（FTIR），X射线衍射（XRD），场发射扫描电子显微镜（FESEM）和基于动态光散射（DLS）的粒度分析对颗粒进行了广泛的表征。GGR _NP3稳定，其平均粒径约为153 nm。GGR _NP将其作为5-氟尿嘧啶（5-FU）的载体基质进行评估，并通过在模拟胃肠液（SGF）中溶胀和体外溶出试验，在最初的2 h和随后的14 h中检测了5-FU的释放行为。模拟肠液（SIF）。与天然明胶或松香胶在相同条件下分别在7 h和10 h内耗尽相比，在16小时内观察到约71％的药物释放（SGF = 21％； SIF = 50％）。释放曲线遵循一阶动力学，从Korsemeyer-Peppas模型获得的扩散指数（n）值介于0.5 <  n <0.8（均在SGF和SIF中），表明存在非菲克扩散机制。A549细胞系用于进行MTT测定试验用于调查载药GGR的细胞毒性_NP3（d GGR _NP3）其中DGGR _NP3相比表现出GGR更大的毒性_NP3。

图形摘要