Freie Universität Berlin, Institute of Pharmacy, Department of Pharmaceutics, Biopharmaceutics & NutriCosmetics, Kelchstr. 31, 12169 Berlin, Germany.
Int J Pharm. 2011 Nov 25;420(1):141-6. doi: 10.1016/j.ijpharm.2011.08.026. Epub 2011 Aug 23.
Lutein is a well known antioxidant and anti-free radical used in cosmetic, nutraceutical industry with potential application in pharmaceutics as supportive antioxidant in treatments. As lipophilic molecule it is poorly soluble in water and has a low bioavailability. Lutein nanosuspension was prepared to enhance dissolution velocity, saturation solubility (C(s)), which are major factors determining oral bioavailability and penetration into the skin. High pressure homogenization (HPH) was used to prepare lutein nanosuspension. Particle size was determined by photon correlation spectroscopy (PCS) and laser diffractometry (LD). The lowest PCS diameter obtained was about 429 nm, the LD diameter 90% of 1.2 μm. The zeta potential was about -40 mV in water and -17 mV in the original dispersion medium. The 3 month storage study at different temperatures (4°C, 25°C, 40°C) confirmed physical stability despite the low zeta potential of -17 mV in original surfactant solution. A pronounced increase in saturation solubility by 26.3 fold was obtained for lutein nanocrystals compared to coarse powder. The lutein nanosuspension was converted into pellets and filled into hard gelatin capsules for nutraceutical use, showed a superior in vitro release (factor of 3-4). Lyophilized nanosuspension was prepared for subsequent incorporation into creams and gels. The lyophilized nanosuspension was very well re-dispersible (435 nm). Using cellulose nitrate membranes as in vitro model, permeation through this barrier was 14× higher for lutein nanocrystals compared to coarse powder. However, pig ear skin did not allow lutein to permeate but supported localization of the lutein in the skin where it should act anti-oxidatively.
叶黄素是一种众所周知的抗氧化剂和自由基清除剂，用于化妆品和营养保健品行业，也有在药剂学中作为支持抗氧化剂用于治疗的潜在应用。作为亲脂性分子，它在水中的溶解度差，生物利用度低。制备叶黄素纳米混悬剂以提高溶解速度和饱和溶解度（C(s)），这是决定口服生物利用度和穿透皮肤的主要因素。高压均质（HPH）用于制备叶黄素纳米混悬剂。粒径通过光子相关光谱（PCS）和激光衍射法（LD）确定。获得的最小 PCS 直径约为 429nm，LD 直径的 90%为 1.2μm。在水中的 ζ 电位约为-40mV，在原始分散介质中的 ζ 电位约为-17mV。在不同温度（4°C、25°C、40°C）下进行的 3 个月储存研究证实了物理稳定性，尽管原始表面活性剂溶液中的 ζ 电位低至-17mV。与粗粉相比，叶黄素纳米晶体的饱和溶解度显著提高了 26.3 倍。将叶黄素纳米混悬剂转化为微丸并填充到硬胶囊中用于营养保健品，显示出优越的体外释放（3-4 倍）。制备了冻干纳米混悬剂，以备后续掺入乳膏和凝胶中。冻干纳米混悬剂的再分散性非常好（435nm）。使用硝酸纤维素膜作为体外模型，与粗粉相比，叶黄素纳米晶体通过该屏障的渗透提高了 14 倍。然而，猪耳皮肤不允许叶黄素渗透，但支持叶黄素在皮肤中的定位，从而发挥抗氧化作用。
