Cancer Center, Chonnam National University Hwasun Hospital, Hwasun, South Korea.
Int J Nanomedicine. 2013;8:485-93. doi: 10.2147/IJN.S40580. Epub 2013 Jan 30.
All-trans retinoic acid (RA)-incorporated nanoparticles were prepared using deoxycholic acid-conjugated dextran (DexDA). Anticancer activity of RA-incorporated DexDA nanoparticles were tested in vitro and in vivo.
RA-incorporated nanoparticles were prepared by dialysis. Antiproliferative and anti-invasive potential of RA-incorporated nanoparticles were studied using CT26 colorectal carcinoma cells.
RA-incorporated nanoparticles have small particle sizes of around 70-300 nm and spherical shapes. The higher drug-feeding ratio and higher substitution degree of deoxycholic acid in the conjugates resulted in higher drug contents, lower loading efficiency, and larger particle size. RA release rate became slower at higher drug contents and higher substitution degree of deoxycholic acid in the DexDA conjugates. The antiproliferation activity, anti-invasive activity, and matrix metalloproteinase 2 expression of RA-incorporated nanoparticles against CT26 cells in vitro was similar to RA. However, RA-incorporated nanoparticles had superior antimetastatic activity in an animal pulmonary metastatic model of CT26 cells compared to RA itself.
RA-incorporated nanoparticles showed similar anticancer activity in vitro and superior antimetastatic activity in vivo in a pulmonary metastatic model of CT26 cells. We suggest that RA-incorporated nanoparticles are promising vehicles for efficient delivery of RA.
采用去氧胆酸修饰的葡聚糖（DexDA）制备全反式维甲酸（RA）纳米粒。在体外和体内研究了 RA 结合的 DexDA 纳米粒的抗癌活性。
通过透析法制备 RA 纳米粒。采用 CT26 结直肠癌细胞研究 RA 结合纳米粒的增殖抑制和抗侵袭潜力。
RA 结合纳米粒的粒径约为 70-300nm，呈球形。药物喂养比例较高和缀合物中去氧胆酸的取代度较高导致药物含量较高、载药效率较低、粒径较大。DexDA 缀合物中药物含量和去氧胆酸取代度较高时，RA 释放速率变慢。RA 结合纳米粒对 CT26 细胞的体外增殖抑制活性、抗侵袭活性和基质金属蛋白酶 2 表达与 RA 相似。然而，与 RA 相比，RA 结合纳米粒在 CT26 细胞的动物肺转移模型中具有更好的抗转移活性。
RA 结合纳米粒在 CT26 细胞的肺转移模型中显示出相似的体外抗癌活性和体内优越的抗转移活性。我们认为 RA 结合纳米粒是高效传递 RA 的有前途的载体。
