Key Laboratory of New Drug Delivery Systems of Chinese Meteria Medical, Jiangsu Provincial Academy of Chinese Medicine, Nanjing 210028, China.
Molecules. 2012 May 18;17(5):5972-87. doi: 10.3390/molecules17055972.
This study aimed to investigate the in vitro skin permeation and in vivo antineoplastic effect of curcumin by using liposomes as the transdermal drug-delivery system. Soybean phospholipids (SPC), egg yolk phospholipids (EPC), and hydrogenated soybean phospholipids (HSPC) were selected for the preparation of different kinds of phospholipids composed of curcumin-loaded liposomes: C-SPC-L (curcumin-loaded SPC liposomes), C-EPC-L (curcumin-loaded EPC liposomes), and C-HSPC-L (curcumin-loaded HSPC liposomes). The physical properties of different lipsomes were investigated as follows: photon correlation spectroscopy revealed that the average particle sizes of the three types of curcumin-loaded liposomes were 82.37 ± 2.19 nm (C-SPC-L), 83.13 ± 4.89 nm (C-EPC-L), and 92.42 ± 4.56 nm (C-HSPC-L), respectively. The encapsulation efficiency values were found to be 82.32 ± 3.91%, 81.59 ± 2.38%, and 80.77 ± 4.12%, respectively. An in vitro skin penetration study indicated that C-SPC-L most significantly promoted drug permeation and deposition followed by C-EPC-L, C-HSPC-L, and curcumin solution. Moreover, C-SPC-L displayed the greatest ability of all loaded liposomes to inhibit the growth of B16BL6 melanoma cells. Therefore, the C-SPC-L were chosen for further pharmacodynamic evaluation. A significant effect on antimelanoma activity was observed with C-SPC-L, as compared to treatment with curcumin solution in vivo. These results suggest that C-SPC-L would be a promising transdermal carrier for curcumin in cancer treatment.
本研究旨在通过使用脂质体作为透皮药物传递系统,研究姜黄素的体外皮肤渗透和体内抗肿瘤作用。选择大豆磷脂(SPC)、蛋黄磷脂(EPC)和氢化大豆磷脂(HSPC)来制备不同种类的载姜黄素脂质体:C-SPC-L(载姜黄素 SPC 脂质体)、C-EPC-L(载姜黄素 EPC 脂质体)和 C-HSPC-L(载姜黄素 HSPC 脂质体)。研究了不同脂质体的物理性质如下:光子相关光谱法显示,三种载姜黄素脂质体的平均粒径分别为 82.37±2.19nm(C-SPC-L)、83.13±4.89nm(C-EPC-L)和 92.42±4.56nm(C-HSPC-L)。包封效率值分别为 82.32±3.91%、81.59±2.38%和 80.77±4.12%。体外皮肤渗透研究表明,C-SPC-L 最显著地促进了药物渗透和沉积,其次是 C-EPC-L、C-HSPC-L 和姜黄素溶液。此外,C-SPC-L 在所有负载脂质体中表现出最强的抑制 B16BL6 黑色素瘤细胞生长的能力。因此,选择 C-SPC-L 进行进一步的药效学评价。与体内使用姜黄素溶液相比,C-SPC-L 对抑瘤活性有显著影响。这些结果表明,C-SPC-L 可能是治疗癌症的姜黄素透皮载体的一种有前途的选择。