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Preparation of Curcumin-Loaded Liposomes and Evaluation of Their Skin Permeation and Pharmacodynamics

机译:姜黄素负载脂质体的制备及其皮肤渗透和药效学评价

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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.
机译:本研究旨在研究脂质体作为透皮给药系统对姜黄素的体外皮肤渗透和体内抗肿瘤作用。选择了大豆磷脂(SPC),蛋黄磷脂(EPC)和氢化大豆磷脂(HSPC)来制备由载有姜黄素的脂质体组成的各种磷脂:C-SPC-L(载有姜黄素的SPC脂质体), C-EPC-L(姜黄素负载的EPC脂质体)和C-HSPC-L(姜黄素负载的HSPC脂质体)。对不同脂质体的物理性质进行了如下研究:光子相关光谱表明,三种类型的姜黄素负载脂质体的平均粒径分别为82.37±2.19 nm(C-SPC-L),83.13±4.89 nm(C-EPC) -C)和92.42±4.56 nm(C-HSPC-L)。发现封装效率值分别为82.32±3.91%,81.59±2.38%和80.77±4.12%。一项体外皮肤渗透研究表明,C-SPC-L最明显地促进了药物的渗透和沉积,其次是C-EPC-L,C-HSPC-L和姜黄素溶液。此外,C-SPC-L表现出所有负载脂质体抑制B16BL6黑色素瘤细胞生长的最大能力。因此,选择了C-SPC-L进行进一步的药效评估。与在体内用姜黄素溶液治疗相比,用C-SPC-L观察到了对炭疽病活性的显着影响。这些结果表明,C-SPC-L将成为姜黄素在癌症治疗中有希望的透皮载体。

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