Department of Pharmaceutical nanotechnology, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
Department of Pharmaceutical nanotechnology, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran; Biotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran; Nanotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran.
Colloids Surf B Biointerfaces. 2018 Apr 1;164:332-339. doi: 10.1016/j.colsurfb.2018.01.054. Epub 2018 Jan 31.
Auraptene (AUR) is a bioactive antioxidant coumarin with valuable pharmacological properties; however, poor water solubility is a substantial issue for the topical application of AUR. Therefore, we sought to prepare solid lipid nanoparticles (SLNs) containing AUR (AUR-SLNs) to enhance its anti-inflammatory effect. The prepared formulations were optimized by applying the response surface method. Furthermore, AUR-SLNs were compared to conventional cream containing AUR regarding both the permeation rate of the nanoparticles and the anti-inflammatory effect through both in vitro and in vivo studies. Particle size and entrapment efficiency of the optimized formulation were 140.9 ± 3.55 nm and 84.11% ± 3.30, respectively. Transmission electron microscopy revealed that the nanoparticles were spherical. Differential scanning calorimetry (DSC) analysis demonstrated no drug-lipid incompatibility in the formulation. Fourier transform-infrared spectroscopy (FTIR) spectra revealed the amorphous state of AUR and the encapsulation of this agent in SLNs. The in vitro permeation studies exhibited that AUR-SLNs could significantly enhance cutaneous uptake of AUR and skin targeting. The anti-inflammatory and histopathological studies exhibited no significant differences between AUR-SLNs and indomethacin. AUR-SLNs did not induce skin sensitization in guinea pigs. The results suggest that SLNs could be appropriate carriers for the topical application of AUR as a natural anti-inflammatory agent.
奥瑞宾（AUR）是一种具有重要药理活性的生物抗氧化香豆素，但由于其水溶性差，限制了其在局部应用中的发展。因此，我们试图制备含奥瑞宾的固体脂质纳米粒（AUR-SLNs）以增强其抗炎作用。通过响应面法优化了所制备的制剂。此外，通过体外和体内研究比较了载有 AUR 的 AUR-SLNs 与常规乳膏在纳米粒的渗透速率和抗炎效果方面的差异。优化后的制剂的粒径和包封效率分别为 140.9±3.55nm 和 84.11%±3.30%。透射电子显微镜显示纳米粒为球形。差示扫描量热法（DSC）分析表明制剂中无药物-脂质不相容性。傅里叶变换-红外光谱（FTIR）图谱显示 AUR 为无定形态，且该药物被包封于 SLNs 中。体外渗透研究表明，AUR-SLNs 可显著增加 AUR 的皮肤摄取量和皮肤靶向性。抗炎和组织病理学研究表明 AUR-SLNs 与吲哚美辛之间无显著差异。AUR-SLNs 未在豚鼠中引起皮肤致敏。结果表明，SLNs 可作为一种天然抗炎剂的局部应用的合适载体。
