Physical Chemistry Department, Faculty of Chemistry, Jagiellonian University, Kraków, Poland.
Colloids Surf B Biointerfaces. 2011 Nov 1;88(1):231-9. doi: 10.1016/j.colsurfb.2011.06.037. Epub 2011 Jul 1.
Curcumin shows huge potential as an anticancer and anti-inflammatory agent. However, to achieve a satisfactory bioavailability and stability of this compound, its liposomal form is preferable. Our detailed studies on the curcumin interaction with lipid membranes are aimed to obtain better understanding of the mechanism and eventually to improve the efficiency of curcumin delivery to cells. Egg yolk phosphatidylcholine (EYPC) one-component monolayers and bilayers, as well as mixed systems containing additionally dihexadecyl phosphate (DHP) and cholesterol, were studied. Curcumin binding constant to EYPC liposomes was determined based on two different methods: UV/Vis absorption and fluorescence measurements to be 4.26×10(4)M(-1) and 3.79×10(4)M(-1), respectively. The fluorescence quenching experiment revealed that curcumin locates in the hydrophobic region of EYPC liposomal bilayer. It was shown that curcumin impacts the size and stability of the liposomal carriers significantly. Loaded into the EYPC/DPH/cholesterol liposomal bilayer curcumin stabilizes the system proportionally to its content, while the EYPC/DPH system is destabilized upon drug loading. The three-component lipid composition of the liposome seems to be the most promising system for curcumin delivery. An interaction of free and liposomal curcumin with EYPC and mixed monolayers was also studied using Langmuir balance measurements. Monolayer systems were treated as a simple model of cell membrane. Condensing effect of curcumin on EYPC and EYPC/DHP monolayers and loosening influence on EYPC/DHP/chol ones were observed. It was also demonstrated that curcumin-loaded EYPC liposomes are more stable upon interaction with the model lipid membrane than the unloaded ones.
姜黄素作为一种抗癌和抗炎药物具有巨大的潜力。然而，为了实现该化合物令人满意的生物利用度和稳定性，其脂质体形式是优选的。我们对姜黄素与脂质膜相互作用的详细研究旨在更好地理解其机制，并最终提高姜黄素向细胞传递的效率。我们研究了蛋黄磷脂酰胆碱 (EYPC) 单分子层和双层膜，以及包含另外的二己基磷酸酯 (DHP) 和胆固醇的混合体系。基于两种不同的方法确定了姜黄素与 EYPC 脂质体的结合常数：紫外/可见吸收和荧光测量分别为 4.26×10(4)M(-1)和 3.79×10(4)M(-1)。荧光猝灭实验表明姜黄素位于 EYPC 脂质体双层的疏水区。结果表明，姜黄素对脂质体载体的大小和稳定性有显著影响。负载到 EYPC/DPH/胆固醇脂质双层中的姜黄素会根据其含量稳定该体系，而在药物负载时 EYPC/DPH 体系会被破坏。因此，三组分脂质组成的脂质体系统似乎是最有前途的姜黄素递送系统。还使用 Langmuir 天平测量研究了游离和载药姜黄素与 EYPC 和混合单分子层的相互作用。单层系统被视为细胞膜的简单模型。观察到姜黄素对 EYPC 和 EYPC/DHP 单层的缩合效应以及对 EYPC/DHP/胆固醇单层的松动影响。还证明与模型脂质膜相互作用时，载药 EYPC 脂质体比未载药的脂质体更稳定。
