肝细胞癌的靶向治疗：利用乳糖化 pH 响应性纳米粒共递送索拉非尼和姜黄素。

Targeted Therapy for Hepatocellular Carcinoma: Co-Delivery of Sorafenib and Curcumin Using Lactosylated pH-Responsive Nanoparticles.

机构信息

Department of Pharmacy, Affiliated Hospital of Jiangnan University, The Fourth People's Hospital of Wuxi City, WuXi 214000, Jiangsu Province, People's Republic of China.

Affiliated Hospital of Jiangnan University, The Fourth People's Hospital of Wuxi City, Wuxi 214000, Jiangsu Province, People's Republic of China.

出版信息

Drug Des Devel Ther. 2020 Feb 18;14:647-659. doi: 10.2147/DDDT.S238955. eCollection 2020.

PURPOSE

Hepatocellular carcinoma (HCC) is a leading cancer worldwide. In the present investigation, sorafenib (SFN) and curcumin (CCM) were co-delivered using pH-sensitive lactosylated nanoparticles (LAC-NPs) for targeted HCC treatment.

METHODS

pH-responsive lactosylated materials were synthesized. SFN and CCM co-delivered, pH-responsive lactosylated nanoparticles (LAC-SFN/CCM-NPs) were self-assembled by using the nanoprecipitation technique. The nanoparticles were characterized in terms of particle size, charge and drug release profile. The anti-cancer effects of the nanoparticles were evaluated in human hepatic carcinoma cells (HepG2) cells and HCC tumor xenograft models.

RESULTS

LAC-SFN/CCM-NPs are spherical particles with light coats on the surface. The size and zeta potential of LAC-SFN/CCM-NPs were 115.5 ± 3.6 nm and -34.6 ± 2.4, respectively. The drug release of LAC-SFN/CCM-NPs in pH 5.5 was more efficient than in pH 7.4. LAC-SFN/CCM-NPs group exhibited the smallest tumor volume (239 ± 14 mm), and the inhibition rate of LAC-SFN/CCM-NPs was 77.4%.

CONCLUSION

In summary, LAC-SFN/CCM-NPs was proved to be a promising system for targeted HCC therapy.

目的

肝细胞癌（HCC）是全球主要的癌症之一。在本研究中，采用 pH 敏感的乳糖化纳米粒（LAC-NPs）共载索拉非尼（SFN）和姜黄素（CCM），用于靶向 HCC 治疗。

方法

合成 pH 响应性乳糖化材料。采用纳米沉淀技术自组装 SFN 和 CCM 共载、pH 响应性乳糖化纳米粒（LAC-SFN/CCM-NPs）。从粒径、电荷和药物释放曲线等方面对纳米粒进行了表征。在人肝癌细胞（HepG2）和 HCC 肿瘤异种移植模型中评价了纳米粒的抗癌作用。

结果

LAC-SFN/CCM-NPs 为表面有轻微涂层的球形颗粒。LAC-SFN/CCM-NPs 的粒径和 Zeta 电位分别为 115.5±3.6nm 和-34.6±2.4。LAC-SFN/CCM-NPs 在 pH5.5 下的药物释放效率高于 pH7.4。LAC-SFN/CCM-NPs 组的肿瘤体积最小（239±14mm），抑制率为 77.4%。