Guangxi Key Laboratory of Special Biomedicine, School of Medicine, Guangxi University, Nanning, China.
Department of Thoracic Surgery, The People's Hospital of Guangxi Zhuang Autonomous Region, Guangxi Academy of Medical Sciences, Nanning, China.
J Microencapsul. 2024 Sep;41(6):419-433. doi: 10.1080/02652048.2024.2376114. Epub 2024 Jul 11.
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 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.
构建具有双重配体的新型纳米载体，以实现优异的抗肿瘤疗效和较低的毒副作用。
采用薄膜水化法制备脂质体。利用紫外分光光度法、高效液相色谱法、纳米粒度分析仪、超滤离心法、透析法、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 实验和肿瘤球实验研究 dg-Bcan 靶向肽（BTP-7）/pHA-替莫唑胺（TMZ）/四（4-羧基苯基）卟啉（TCPP）-脂质体的性质、细胞毒性和靶向性。
BTP-7/pHA-TMZ/TCPP-Lip 呈类球形，平均粒径为 143±3.214nm，多分散指数为 0.203±0.025，表面电荷为-22.8±0.425mV。药物载药量（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±0.64%（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 可以特异性地靶向肿瘤细胞，实现高效的药物传递，提高抗肿瘤疗效，降低全身毒性。
