Abstract：
UNASSIGNED: To construct a novel liposomal drug delivery system co-modified with SP94 and BR2 ligands, encapsulating both the bitter ginseng derivative B21 and doxorubicin (DOX), to achieve superior anti-tumour efficacy and reduced toxic side effects.
UNASSIGNED: Liposomes were prepared using an organic phase reaction method, with B21 encapsulated in the lipid phase and DOX in the aqueous phase. The liposomes were further modified with SP94 and BR2 peptides. The characterisations, cytotoxicity, and in vitro targeting effects were assessed through various methods including ultraviolet spectrophotometry, high-performance liquid chromatography, nano-size analysis, ultrafiltration centrifugation, dialysis, transmission electron microscopy, flow cytometry, Methylthiazolyldiphenyl-tetrazolium bromide assay, confocal laser scanning microscopy, transwell assay, and tumorsphere assay.
UNASSIGNED: SP94/BR2-B21/DOX-LP liposomes were spherical with an average diameter of 120.87 ± 1.00 nm, a polydispersity index (PDI) of 0.223 ± 0.006, and a surface charge of -23.1 ± 1.27 mV. The encapsulation efficiencies for B21 and DOX were greater than 85% and 97% (mg/mg), respectively. The results indicated that SP94/BR2-B21/DOX-LP exhibited enhanced targeting and cytotoxicity compared to single-ligand modified and unmodified liposomes, with the combined encapsulation of B21 and DOX showing synergistic anti-hepatocarcinogenic effects.
UNASSIGNED: SP94/BR2-B21/DOX-LP liposomes represent a promising targeted drug delivery system for hepatocellular carcinoma, offering improved membrane penetration, enhanced therapeutic efficacy, and reduced systemic toxicity.
UNASSIGNED: Liposomes were prepared using an organic phase reaction method, with B21 encapsulated in the lipid phase and DOX in the aqueous phase. The liposomes were further modified with SP94 and BR2 peptides. The characterisations, cytotoxicity, and in vitro targeting effects were assessed through various methods including ultraviolet spectrophotometry, high-performance liquid chromatography, nano-size analysis, ultrafiltration centrifugation, dialysis, transmission electron microscopy, flow cytometry, Methylthiazolyldiphenyl-tetrazolium bromide assay, confocal laser scanning microscopy, transwell assay, and tumorsphere assay.
UNASSIGNED: SP94/BR2-B21/DOX-LP liposomes were spherical with an average diameter of 120.87 ± 1.00 nm, a polydispersity index (PDI) of 0.223 ± 0.006, and a surface charge of -23.1 ± 1.27 mV. The encapsulation efficiencies for B21 and DOX were greater than 85% and 97% (mg/mg), respectively. The results indicated that SP94/BR2-B21/DOX-LP exhibited enhanced targeting and cytotoxicity compared to single-ligand modified and unmodified liposomes, with the combined encapsulation of B21 and DOX showing synergistic anti-hepatocarcinogenic effects.
UNASSIGNED: SP94/BR2-B21/DOX-LP liposomes represent a promising targeted drug delivery system for hepatocellular carcinoma, offering improved membrane penetration, enhanced therapeutic efficacy, and reduced systemic toxicity.
摘要：
■为了构建一种新型的与SP94和BR2配体共修饰的脂质体药物递送系统，同时封装苦参衍生物B21和多柔比星（DOX），取得优越的抗肿瘤疗效，减少毒副作用。
■使用有机相反应方法制备脂质体，其中B21封装在脂质相中,DOX封装在水相中。用SP94和BR2肽进一步修饰脂质体。特征，细胞毒性，并通过包括紫外分光光度法在内的各种方法评估体外靶向效果，高效液相色谱法，纳米尺寸分析，超滤离心，透析,透射电子显微镜,流式细胞术,甲基噻唑基二苯基-溴化四唑盐测定，共聚焦激光扫描显微镜，transwell分析，和肿瘤球检测。
■SP94/BR2-B21/DOX-LP脂质体呈球形，平均直径为120.87±1.00nm，多分散指数(PDI)为0.223±0.006,表面电荷为-23.1±1.27mV。B21和DOX的包封效率分别大于85%和97%(mg/mg),分别。结果表明，与单配体修饰和未修饰的脂质体相比，SP94/BR2-B21/DOX-LP显示出增强的靶向性和细胞毒性。B21和DOX的联合封装显示出协同的抗肝癌作用。
■SP94/BR2-B21/DOX-LP脂质体代表了一种有前途的肝细胞癌靶向给药系统，提供改进的膜渗透，增强治疗功效，减少全身毒性。
■使用有机相反应方法制备脂质体，其中B21封装在脂质相中,DOX封装在水相中。用SP94和BR2肽进一步修饰脂质体。特征，细胞毒性，并通过包括紫外分光光度法在内的各种方法评估体外靶向效果，高效液相色谱法，纳米尺寸分析，超滤离心，透析,透射电子显微镜,流式细胞术,甲基噻唑基二苯基-溴化四唑盐测定，共聚焦激光扫描显微镜，transwell分析，和肿瘤球检测。
■SP94/BR2-B21/DOX-LP脂质体呈球形，平均直径为120.87±1.00nm，多分散指数(PDI)为0.223±0.006,表面电荷为-23.1±1.27mV。B21和DOX的包封效率分别大于85%和97%(mg/mg),分别。结果表明，与单配体修饰和未修饰的脂质体相比，SP94/BR2-B21/DOX-LP显示出增强的靶向性和细胞毒性。B21和DOX的联合封装显示出协同的抗肝癌作用。
■SP94/BR2-B21/DOX-LP脂质体代表了一种有前途的肝细胞癌靶向给药系统，提供改进的膜渗透，增强治疗功效，减少全身毒性。
