RGD 偶联白藜芦醇 HSA 纳米粒作为一种新型卵巢癌治疗给药系统。

RGD-Conjugated Resveratrol HSA Nanoparticles as a Novel Delivery System in Ovarian Cancer Therapy.

机构信息

Department of Gynecology and Obstetrics, The Second Affiliated Hospital of Soochow University, Suzhou, People's Republic of China.

出版信息

Drug Des Devel Ther. 2020 Dec 30;14:5747-5756. doi: 10.2147/DDDT.S248950. eCollection 2020.

BACKGROUND

To establish a novel delivery system of RGD-conjugated resveratrol human serum albumin (HAS) nanoparticles in ovarian cancer therapy.

METHODS

The nanoparticles system was characterized for physicochemical properties, the stability in the serum and in vitro release. The comparison between RVT injection, HSA-RVT NPs and RGD-HSA-RVT NPs regarding tissue distributions and pharmacokinetics was also carried out using mice as the animal models.

RESULTS

The results showed that RGD-HSA-RVT NPs were characterized of small particle size about 128.2 nm and negative zeta potential about -21.42 mV, and drug controlled to release slowly on a biphasic pattern. Compared with control groups, RGD-HSA-RVT NPs showed the higher cellular uptake and cell inhibition rates. In vivo data showed that RGD-HSA-RVT NPs have good tumor enrichment characteristics and a significant difference in tumor inhibition, compared with the control group.

CONCLUSION

RGD-conjugated resveratrol HSA nanoparticles are an ideal drug delivery system, which can play a role in the treatment of ovarian cancer.

背景

建立一种新型的 RGD 修饰的白藜芦醇人血清白蛋白（HAS）纳米粒递药系统用于卵巢癌治疗。

方法

对纳米粒系统进行理化性质、血清稳定性和体外释放研究。采用小鼠作为动物模型，比较 RVT 注射液、HSA-RVT NPs 和 RGD-HSA-RVT NPs 的组织分布和药代动力学。

结果

结果表明，RGD-HSA-RVT NPs 的粒径约为 128.2nm，Zeta 电位约为-21.42mV，具有双相缓慢释药的特点。与对照组相比，RGD-HSA-RVT NPs 表现出更高的细胞摄取率和细胞抑制率。体内数据表明，与对照组相比，RGD-HSA-RVT NPs 具有良好的肿瘤富集特性和显著的肿瘤抑制作用。