Wang Jianmin, Wang Hongxia, Zhou Xuefeng, Tang Zuming, Liu Guoqing, Liu Guangyu, Xia Qiang
School of Biological Science and Medical Engineering, State Key Laboratory of Bioelectronics, Southeast University, Nanjing 210096, China.
J Nanosci Nanotechnol. 2012 Mar;12(3):2136-48. doi: 10.1166/jnn.2012.5790.
Nanostructured lipid carrier (NLC) is prospective active ingredients delivery systems based on combinations of solid lipids and liquid oil. Aqueous dispersion of NLC was prepared via hot high pressure homogenization technique. The CoQ10-NLC aqueous dispersion was prepared in order to improve the water solubility, photo-stability of Coenzyme Q10 (CoQ10). The physicochemical characterization parameters of CoQ10-NLC have been explored regarding particle size, zeta potential, polydispersity index (PDI) value and stability of CoQ10, which is an antioxidant. HPLC was employed to monitor the loading of CoQ10 encapsulated in NLC system. Morphology profile and hydrophobicity/hydrophilicity were determined and analyzed using atomic force microscopy (AFM) and water contact angle measurements, respectively. Infrared (IR) spectrometry was exploited to confirm the possible interaction and complex formation between CoQ10 and lipids. The photo-stability of CoQ10 was powerfully improved by NLC, more than 80% of CoQ10 remained unchanged in one month under natural daylight, while the retention of free CoQ10 only 33.5% under the same conditions. CoQ10-NLC offered comparatively high protection. The retention of CoQ10 in NLC system was about 65% after five-month exposure to natural daylight, the retention of free CoQ10 only 13.3%. The CoQ10 in the NLC-based formulation showed considerably enhanced photo-stability compared with CoQ10 itself, and displayed the better protection of CoQ10. The obtained results opened new perspectives on the photo-stability of CoQ10. The MTT analysis determined CoQ10-NLC lower cytotoxicity. In conclusion, the present investigation demonstrated that the CoQ10-NLC significantly improved the water solubility, especially the enhancement of photo-stability of CoQ10 under natural daylight.
纳米结构脂质载体(NLC)是基于固体脂质和液体油组合的有前景的活性成分递送系统。NLC的水分散体通过热高压均质技术制备。制备辅酶Q10-NLC水分散体是为了提高辅酶Q10(CoQ10)的水溶性和光稳定性。已探究了CoQ10-NLC的物理化学表征参数,包括粒径、zeta电位、多分散指数(PDI)值以及作为抗氧化剂的CoQ10的稳定性。采用高效液相色谱法监测包封在NLC系统中的CoQ10的负载量。分别使用原子力显微镜(AFM)和水接触角测量来确定和分析形态轮廓以及疏水性/亲水性。利用红外(IR)光谱法确认CoQ10与脂质之间可能的相互作用和复合物形成。NLC有力地提高了CoQ10的光稳定性,在自然日光下一个月内超过80%的CoQ10保持不变,而在相同条件下游离CoQ10的保留率仅为33.5%。CoQ10-NLC提供了相对较高的保护。在自然日光下暴露五个月后,CoQ10在NLC系统中的保留率约为65%,游离CoQ10的保留率仅为13.3%。与CoQ10本身相比,基于NLC的制剂中的CoQ10显示出显著增强的光稳定性,并对CoQ10表现出更好的保护作用。所得结果为CoQ10的光稳定性开辟了新的前景。MTT分析确定CoQ10-NLC的细胞毒性较低。总之,本研究表明CoQ10-NLC显著提高了水溶性,尤其是在自然日光下增强了CoQ10的光稳定性。