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Preparation and in vitro evaluation of hydroxycamptothecin loaded transferrin modified stealth niosomes

机译:羟基美霉素的制备和体外评价加载转铁蛋白修饰隐身性憩室

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The aim was to prepare hydroxycamptothecin (HCPT) loaded transferrin modified stealth niosomes (Tf-PEG-NS) and to evaluate the physicochemical characteristics, cytotoxicity and cell uptake of Tf-PEG-NS. The amphiphilic copolymer of Poly (methoxy-polyethyleneglycol cyanoacrylate-con-hexadecyl cyanoacrylate) (PEG-PHDCA) acted as surface modified materials was synthesized and characterized. By coupling oxidized transferrin to PEG, Tf-PEG-NS were prepared by thin-film hydration-sonication dispersion method with particle size of (121.2±9.8)nm and encapsulation efficiency of (93.00±0.61)%. In vitro drug release of Tf-PEG-NS was up to 90% within 4B. In vitro cytotoxicity of Tf-PEG-NS was about 3 and 1.5 times that of HCPT injection and PEG-NS on KB cells, respectively. The relative uptake into nucleis of Tf-PEG-NS was significantly higher than other formulations, which was 79, 5.9 and 1.7 times that of HCPT injection, NS and PEG-NS respectively after 12h incubation. The in vitro results suggest that Tf conjugated PEG-coated niosomes could be a potentially effective HCPT delivery carrier for tumor therapy.
机译:其目的是制备羟基喜树碱加载的转铁蛋白修饰隐形泡囊(TF-PEG-NS),并评估TF-PEG-NS的物理化学特性,细胞毒性和细胞摄取。充当表面改性材料聚(甲氧基 - 聚乙二醇氰基丙烯酸酯-CON-十六烷基氰基丙烯酸酯)(PEG-PHDCA)的两亲共聚物的合成和表征。通过偶联氧化转到PEG,TF-PEG-NS是由薄膜水合 - 超声波分散法用的(93.00±0.61)%(121.2±9.8)nm和包封效率粒径制备。在TF-PEG-NS的体外药物释放达内4B 90%。在TF-PEG-NS的体外细胞毒性为约3和1.5倍HCPT注射和PEG-NS对KB细胞,分别。相对摄取到TF-PEG-NS的核团比其它制剂,其为79,5.9和1.7倍,HCPT注射,NS和PEG-NS的后分别孵育12小时更高显著。体外结果表明,TF缀合PEG涂覆类脂质体可以是用于肿瘤治疗潜在有效HCPT递送载体。

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