Abstract：
UNASSIGNED: To construct a novel nano-carrier with dual ligands to achieve superior anti-tumour efficacy and lower toxic side effects.
UNASSIGNED: 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.
UNASSIGNED: 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.
UNASSIGNED: 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.
UNASSIGNED: 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.
UNASSIGNED: 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.
UNASSIGNED: 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.
摘要：
■构建具有双配体的新型纳米载体，以实现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。紫外线,高效液相色谱法,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，共聚焦激光扫描显微镜，transwell,和肿瘤球体测定法用于研究其特征，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，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)为7.40±0.23%和2.05±0.03%(mg/mg);包封效率为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，实现高效的药物输送，提高抗肿瘤疗效，降低全身毒性。
■采用薄膜水化法制备脂质体。紫外线,高效液相色谱法,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，共聚焦激光扫描显微镜，transwell,和肿瘤球体测定法用于研究其特征，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，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)为7.40±0.23%和2.05±0.03%(mg/mg);包封效率为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，实现高效的药物输送，提高抗肿瘤疗效，降低全身毒性。
