Department of Pharmaceutics, School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of China.
Int J Nanomedicine. 2013;8:2533-41. doi: 10.2147/IJN.S46578. Epub 2013 Jul 22.
In the present study, nanostructured lipid carriers (NLCs) were prepared and optimized for the intravenous delivery of β-Elemene (β-E). Aqueous dispersions of NLCs were successfully prepared by high-pressure homogenization method using glycerol monostearate as the solid lipid and a mixture of Maisine 35-1 and Labrafil M1944 CS as the liquid lipid. The results revealed that the morphology of the NLCs was spheroidal. The particle size, zeta potential, and entrapment efficiency (EE) for the optimized formulation were observed as 138.9 nm, -20.2 mV, and 82.11%, respectively. X-ray diffraction analysis revealed the formation of less ordered structures in the inner core of the NLC particles. Moreover, the β-E-loaded NLCs were also less irritating and less toxic compared to Elemene injection. In addition, β-E-NLCs showed a significantly higher bioavailability and anti-tumor efficacy than Elemene injection. Taken together, our data indicate that the β-E-NLCs described in this study are well-suited for the intravenous delivery of β-E.
在本研究中，制备了纳米结构脂质载体（NLC），并对其进行了优化，以用于β-榄香烯（β-E）的静脉给药。通过高压匀质法成功制备了 NLC 的水性分散体，其中甘油单硬脂酸酯作为固体脂质，Maisine 35-1 和 Labrafil M1944 CS 的混合物作为液体脂质。结果表明，NLC 的形态为球形。优化配方的粒径、Zeta 电位和包封效率（EE）分别为 138.9nm、-20.2mV 和 82.11%。X 射线衍射分析表明，NLC 颗粒的内核中形成了较少有序的结构。此外，与注射用榄香烯相比，载有β-E 的 NLC 刺激性更小，毒性更低。此外，β-E-NLC 的生物利用度和抗肿瘤疗效明显高于注射用榄香烯。综上所述，我们的数据表明，本研究中描述的β-E-NLC 非常适合β-E 的静脉给药。
