Centre for Nanoscience and Nanotechnology, Kariavattom Campus, University of Kerala, Thiruvananthapuram, Kerala, India.
Department of Biochemistry, Kariavattom Campus, University of Kerala, Thiruvananthapuram, Kerala, India.
Chem Biol Interact. 2016 Sep 25;257:110-8. doi: 10.1016/j.cbi.2016.07.012. Epub 2016 Jul 11.
Naringenin (NAR) is one of the naturally occurring flavonoids found in citrus fruits and exerts a wide variety of pharmacological activities. The clinical relevance of naringenin is limited by its low solubility and minimal bioavailability, owing to its largely hydrophobic ring structure. The aim of the present study is to develop a novel naringenin nanoparticle system (NAR NP) using simple nanoprecipitation technique with polyvinylpyrrolidone (PVP) as the hydrophilic carrier. The synthesized nanoparticles were characterized using XRD, FTIR, SEM and EDX. The characterization study revealed the nanoscale properties and the interactions between NAR and PVP. In vivo toxicological evaluations were carried out at various doses (1, 5, 10 & 50 mg/kg body wt) in male Sprague-Dawley rats in comparison with silver nanoparticle (AgNP) at toxic concentration (50 mg/kg body wt). The altered hepatotoxicity markers, hematology parameters and antioxidant defense system were observed in AgNP- treated rats. But NAR NP - treated rats did not show any biochemical alterations and improved the antioxidant defense indices when compared to control group, by virtue of the pharmacological properties exerted by NAR. The modulatory effect of NAR NP over inflammatory and stress signaling cascades were confirmed by the normalized mRNA expressions of NF-κB, TNF-α and IL-6. The histopathological analysis of liver, kidney and heart reinforce our findings. These studies provide preliminary answers to some of the key biological issues raised over the use and safety of nanoparticles for diagnostic and therapeutic applications. Consequently, we suggest that the safe NAR NP can be used to reduce the dosage of NAR, improve its bioavailability and merits further investigation for therapeutic applications.
柚皮素（NAR）是在柑橘类水果中发现的一种天然类黄酮，具有广泛的药理活性。由于其疏水性环结构，柚皮素的临床相关性受到其低溶解度和最小生物利用度的限制。本研究旨在使用简单的纳米沉淀技术，以聚乙烯吡咯烷酮（PVP）作为亲水性载体，开发一种新的柚皮素纳米颗粒系统（NAR NP）。使用 XRD、FTIR、SEM 和 EDX 对合成的纳米粒子进行了表征。表征研究揭示了 NAR 与 PVP 之间的纳米级性质和相互作用。在雄性 Sprague-Dawley 大鼠中，以不同剂量（1、5、10 和 50mg/kg 体重）进行了体内毒理学评价，并与毒性浓度（50mg/kg 体重）的银纳米颗粒（AgNP）进行了比较。在 AgNP 处理的大鼠中观察到肝毒性标志物、血液学参数和抗氧化防御系统发生变化。但是，与对照组相比，NAR NP 处理的大鼠没有显示任何生化变化，并且通过 NAR 发挥的药理学特性改善了抗氧化防御指数。通过 NF-κB、TNF-α 和 IL-6 的归一化 mRNA 表达证实了 NAR NP 对炎症和应激信号级联的调节作用。肝、肾和心脏的组织病理学分析加强了我们的发现。这些研究为一些关于纳米粒子在诊断和治疗应用中使用和安全性提出的关键生物学问题提供了初步答案。因此，我们建议安全的 NAR NP 可用于降低 NAR 的剂量，提高其生物利用度，并值得进一步研究用于治疗应用。
