Zhou Huafeng, Yue Yang, Liu Guanlan, Li Yan, Zhang Jing, Yan Zemin, Duan Mingxing
Nanoscale Res Lett. 2010 Jul 20;5(10):1561-9. doi: 10.1007/s11671-010-9677-z.
The purpose of this study was to investigate the influence of the inner lipid ratio on the physicochemical properties and skin targeting of surfactant-free lecithin-based coenzyme Q10-loaded lipid nanocapsules (CoQ10-LNCs). The smaller particle size of CoQ10-LNCs was achieved by high pressure and a lower ratio of CoQ10/GTCC (Caprylic/capric triglyceride); however, the zeta potential of CoQ10-LNCs was above /- 60 mV/ with no distinct difference among them at different ratios of CoQ10/GTCC. Both the crystallisation point and the index decreased with the decreasing ratio of CoQ10/GTCC and smaller particle size; interestingly, the supercooled state of CoQ10-LNCs was observed at particle size below about 200 nm, as verified by differential scanning calorimetry (DSC) in one heating-cooling cycle. The lecithin monolayer sphere structure of CoQ10-LNCs was investigated by cryogenic transmission electron microscopy (Cryo-TEM). The skin penetration results revealed that the distribution of Nile red-loaded CoQ10-LNCs depended on the ratio of inner CoQ10/GTCC; moreover, epidermal targeting and superficial dermal targeting were achieved by the CoQ10-LNCs application. The highest fluorescence response was observed at a ratio of inner CoQ10/GTCC of 1:1. These observations suggest that lecithin-based LNCs could be used as a promising topical delivery vehicle for lipophilic compounds.
本研究的目的是探讨内部脂质比例对无表面活性剂的基于卵磷脂的辅酶Q10负载脂质纳米胶囊（CoQ10-LNCs）的物理化学性质和皮肤靶向性的影响。通过高压和较低的CoQ10/GTCC（辛酸/癸酸甘油三酯）比例可实现CoQ10-LNCs较小的粒径；然而，CoQ10-LNCs的zeta电位在不同CoQ10/GTCC比例下均高于/- 60 mV/，且无明显差异。随着CoQ10/GTCC比例的降低和粒径减小，结晶点和结晶指数均降低；有趣的是，通过差示扫描量热法（DSC）在一个加热-冷却循环中验证，在粒径低于约200 nm时观察到CoQ10-LNCs处于过冷状态。通过低温透射电子显微镜（Cryo-TEM）研究了CoQ10-LNCs的卵磷脂单层球结构。皮肤渗透结果表明，负载尼罗红的CoQ10-LNCs的分布取决于内部CoQ10/GTCC的比例；此外，通过应用CoQ10-LNCs实现了表皮靶向和真皮浅层靶向。在内部CoQ10/GTCC比例为1:1时观察到最高的荧光响应。这些观察结果表明，基于卵磷脂的LNCs可作为一种有前景的亲脂性化合物局部递送载体。
