Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla 90112, Thailand; Phytomedicine and Pharmaceutical Biotechnology Excellence Research Center, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla 90112, Thailand.
Phytomedicine and Pharmaceutical Biotechnology Excellence Research Center, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla 90112, Thailand; Department of Clinical Pharmacy, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla 90112, Thailand.
Colloids Surf B Biointerfaces. 2015 Jul 1;131:182-90. doi: 10.1016/j.colsurfb.2015.04.055. Epub 2015 May 4.
The aim of this study was to develop and assess nanostructured lipid carriers (NLC) compared to solid lipid nanoparticles (SLN) for improving the oral bioavailability of oxyresveratrol (OXY). The OXY formulated as SLN (OXY-SLN) and NLC (OXY-NLC) were prepared by a high shear homogenization technique. The optimized OXY-NLC (NLC3) produced smaller nanoparticle sizes (96±0.9nm) than that of the OXY-SLN (108±0.3nm) with a homogeneous size distribution and a high zeta potential. The spherical NLC had a significantly higher efficiency for OXY entrapment (89±0.1%) and a better stability than the SLN after storage for 12 months at 4±2°C according to parameters such as smaller particles, greater zeta potential and a higher loading capacity (p<0.05). Differential scanning calorimetry (DSC) showed a less ordered crystalline structure of NLC than SLN. The accumulated drug in an amorphous state in the NLC was also confirmed by powder X-ray diffraction (PXRD). The in vitro release profiles of the OXY-NLC showed a more sustained release compared to the SLN and unformulated OXY. The in vivo pharmacokinetic profiles implied enterohepatic recycling of OXY in the Wistar rat. Meanwhile, the oral absorption pattern of OXY was modified by both types of lipid nanoparticles. The SLN and NLC increased the relative bioavailability of OXY to 125% and 177%, respectively, compared with unformulated OXY. These findings indicated that NLC could be used as a potential carrier to improve the oral bioavailability of OXY.
本研究旨在开发和评估纳米结构脂质载体 (NLC)，与固体脂质纳米粒 (SLN) 相比，以提高白藜芦醇 (OXY) 的口服生物利用度。通过高剪切匀化技术将 OXY 制成 SLN (OXY-SLN) 和 NLC (OXY-NLC)。优化的 OXY-NLC (NLC3) 产生的纳米颗粒尺寸 (96±0.9nm) 小于 OXY-SLN (108±0.3nm)，具有均匀的粒径分布和高 zeta 电位。球形 NLC 对 OXY 的包封效率显著更高 (89±0.1%)，并且在 4±2°C 下储存 12 个月后比 SLN 具有更好的稳定性，这是根据更小的颗粒、更大的 zeta 电位和更高的载药量等参数得出的 (p<0.05)。差示扫描量热法 (DSC) 显示 NLC 的结晶结构比 SLN 更无序。NLC 中无定形状态的累积药物也通过粉末 X 射线衍射 (PXRD) 得到证实。OXY-NLC 的体外释放曲线显示出比 SLN 和未配方 OXY 更持久的释放。体内药代动力学曲线表明 OXY 在 Wistar 大鼠中存在肠肝循环。同时，两种类型的脂质纳米粒都改变了 OXY 的口服吸收模式。与未配方 OXY 相比，SLN 和 NLC 分别将 OXY 的相对生物利用度提高到 125%和 177%。这些发现表明 NLC 可以用作提高 OXY 口服生物利用度的潜在载体。
