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载姜黄素脂质体的制备及其经皮渗透和药效学评价。

Preparation of curcumin-loaded liposomes and evaluation of their skin permeation and pharmacodynamics.

机构信息

Key Laboratory of New Drug Delivery Systems of Chinese Meteria Medical, Jiangsu Provincial Academy of Chinese Medicine, Nanjing 210028, China.

出版信息

Molecules. 2012 May 18;17(5):5972-87. doi: 10.3390/molecules17055972.

Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2de5/6268695/466b98090468/molecules-17-05972-g001.jpg

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