You Xiaoyan, Liu Hui, Chen Yue, Zhao Guoping
College of Food and Bioengineering, Henan University of Science and Technology, Luoyang 471023, China.
Tianjin Institute of Industrial Biotechnology, Chinese Academy of Sciences, Tianjin 300308, China.
Polymers (Basel). 2024 Feb 1;16(3):405. doi: 10.3390/polym16030405.
Liposomes show promise for anti-cancer drug delivery and tumor-targeted therapy. However, complex tumor microenvironments and the performance limitations of traditional liposomes restrict clinical translation. Hyaluronic acid (HA)-modified nanoliposomes effectively target CD44-overexpressing tumor cells. Combination therapy enhances treatment efficacy and delays drug resistance. Here, we developed paclitaxel (PTX) liposomes co-modified with ginsenoside compound K (CK) and HA using film dispersion. Compared to cholesterol (Ch), CK substantially improved encapsulation efficiency and stability. In vitro release studies revealed pH-responsive behavior, with slower release at pH 7.4 versus faster release at pH 5. In vitro cytotoxicity assays demonstrated that replacing Ch with CK in modified liposomes considerably decreased HCT-116 cell viability. Furthermore, flow cytometry and fluorescence microscopy showed a higher cellular uptake of PTX-CK-Lip-HA in CD44-high cells, reflected in the lower half maximal inhibitory concentrations. Overall, CK/HA-modified liposomes represent an innovative, targeted delivery system for enhanced tumor therapy via pH-triggered drug release and CD44 binding.
脂质体在抗癌药物递送和肿瘤靶向治疗方面显示出前景。然而,复杂的肿瘤微环境和传统脂质体的性能限制阻碍了其临床转化。透明质酸(HA)修饰的纳米脂质体可有效靶向CD44高表达的肿瘤细胞。联合治疗可提高治疗效果并延缓耐药性。在此,我们采用薄膜分散法制备了人参皂苷Compound K(CK)和HA共修饰的紫杉醇(PTX)脂质体。与胆固醇(Ch)相比, CK显著提高了包封率和稳定性。体外释放研究显示出pH响应行为,在pH 7.4时释放较慢,而在pH 5时释放较快。体外细胞毒性试验表明,在修饰的脂质体中用CK替代Ch可显著降低HCT-116细胞活力。此外,流式细胞术和荧光显微镜显示,PTX-CK-Lip-HA在CD44高表达细胞中的细胞摄取更高,这体现在较低的半数最大抑制浓度上。总体而言,CK/HA修饰的脂质体代表了一种创新的靶向递送系统,可通过pH触发的药物释放和CD44结合增强肿瘤治疗效果。