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肝细胞癌是全世界最常见的恶性肿瘤之一,居癌症相关死亡原因第三位。通过在纳米载体系统上修饰靶向配体可将药物主动靶向至肿瘤细胞。随着药物制剂学的发展,采用纳米给药系统共递送化疗药物与基因药物成为了治疗肿瘤的一种手段。本研究通过薄膜超声法制备了共包载多西他赛(DTX)和小干扰RNA(siRNA)的脂质体,并用SP94对其进行修饰。血清稳定性试验表明,脂质体能较好地保护siRNA免受血清中核酸酶的降解。与未修饰的阳离子脂质体相比,SP94修饰的阳离子脂质体显著增强了制剂的在肿瘤细胞内的摄取和对肿瘤细胞的抗增殖作用,表明了SP94的主动靶向作用。本课题成功构建了主动靶向肝癌的共包载DTX和siRNA的阳离子纳米粒给药系统,为肝细胞癌的治疗提供了新的研究思路。
Hepatocellular carcinoma is one of the most common malignancies in the world and ranks third among cancer-related causes of death. Drugs can be actively targeted to tumor cells by modifying the targeting ligand on the nanocarrier system. With the development of pharmaceutics, the delivery of chemotherapeutic drugs and gene drugs using nanometer drug delivery systems has become a means of treating tumors. In this study, liposomes co-encapsulated with docetaxel (DTX) and small interfering RNA (siRNA) were prepared by membrane ultrasonography and modified with SP94. Serum stability tests showed that liposomes can better protect siRNA from the degradation of nuclease in serum. The SP94-modified cationic liposomes significantly enhanced uptake of the formulation in tumor cells and anti-proliferative effect on tumor cells compared to unmodified cationic liposomes, indicating the active targeting of SP94. This topic has successfully constructed cationic nanoparticle drug delivery system that co-encapsulates DTX and siRNA actively targeting liver cancer, which provides a new research idea for the treatment of hepatocellular carcinoma.