用BTP-7和pHA修饰的双靶向脂质体联合递送TCPP和TMZ以增强胶质母细胞瘤细胞的抗肿瘤作用。
Dual-targeting liposomes modified with BTP-7 and pHA for combined delivery of TCPP and TMZ to enhance the anti-tumour effect in glioblastoma cells.
发表日期:2024 Jul 11
作者:
Lili Li, Lin Jing, Zijun Tang, Jingguo Du, Yonglong Zhong, Xu Liu, Mingqing Yuan
来源:
BIOMEDICINE & PHARMACOTHERAPY
摘要:
构建新型双配体纳米载体,以达到优异的抗肿瘤功效和较低的毒副作用。采用薄膜水化法制备脂质体。使用紫外线、高效液相色谱、纳米尺寸分析仪、超滤离心、透析、透射电子显微镜、流式细胞术、细胞计数试剂盒-8、共焦激光扫描显微镜、Transwell 和肿瘤球测定来研究表征、细胞毒性和体外靶向 dg-Bcan 靶向肽 (BTP-7)/pHA-替莫唑胺 (TMZ)/四(4-羧基苯基)卟啉 (TCPP)-Lip。BTP-7/pHA-TMZ/TCPP-Lip 是一个球体,具有平均直径为143±3.214nm,多分散指数为0.203±0.025,表面电荷为-22.8±0.425mV。载药量(TMZ和TCPP)分别为7.40±0.23%和2.05±0.03%(mg/mg);包封率分别为81.43±0.51%和84.28±1.64%(mg/mg)。结果表明,BTP-7/pHA-TMZ/TCPP-Lip具有增强的靶向性和细胞毒性。BTP-7/pHA-TMZ/TCPP-Lip可以特异性靶向肿瘤细胞,实现高效药物递送,提高抗肿瘤效果。功效并降低全身毒性。
To construct a novel nano-carrier with dual ligands to achieve superior anti-tumour efficacy and lower toxic side effects.Liposomes were prepared by thin film hydration method. Ultraviolet, high performance liquid chromatography, nano-size analyser, ultrafiltration centrifugation, dialysis, transmission electron microscope, flow cytometry, Cell Counting Kit-8, confocal laser scanning microscopy, transwell, and tumorsphere assay were used to study the characterisations, cytotoxicity, and in vitro targeting of dg-Bcan targeting peptide (BTP-7)/pHA-temozolomide (TMZ)/tetra(4-carboxyphenyl)porphyrin (TCPP)-Lip.BTP-7/pHA-TMZ/TCPP-Lip was a spheroid with a mean diameters of 143 ± 3.214 nm, a polydispersity index of 0.203 ± 0.025 and a surface charge of -22.8 ± 0.425 mV. The drug loadings (TMZ and TCPP) are 7.40 ± 0.23% and 2.05 ± 0.03% (mg/mg); and the encapsulation efficiencies are 81.43 ± 0.51% and 84.28 ± 1.64% (mg/mg). The results showed that BTP-7/pHA-TMZ/TCPP-Lip presented enhanced targeting and cytotoxicity.BTP-7/pHA-TMZ/TCPP-Lip can specifically target the tumour cells to achieve efficient drug delivery, and improve the anti-tumour efficacy and reduces the systemic toxicity.