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首页> 外文期刊>Nanobiotechnology, IET >Synthesis of biotin-targeted chitosan/poly (methyl vinyl ether-alt-maleic acid) copolymeric micelles for delivery of doxorubicin
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Synthesis of biotin-targeted chitosan/poly (methyl vinyl ether-alt-maleic acid) copolymeric micelles for delivery of doxorubicin

机译：靶向生物素的壳聚糖/聚（甲基乙烯基醚-马来酸甲基）共聚物胶束的合成，用于递送阿霉素

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Biotinylated chitosan/poly(methyl vinyl ether--maleic acid) (PMVEMA) copolymer was synthesised by an amide reaction in two steps Structural characterisation was performed using HNMR and Fourier transform infra-red (FTIR) spectra. Critical micelle concentration (CMC) of the copolymer was determined by pyrene as a fluorescent probe. Doxorubicin (DOX) was loaded in the micelles by the direct dissolution method. The effects of different variables including type of copolymer, copolymer concentration, stirring rate and stirring time were studied on the physicochemical properties of the micelles including: particle size, zeta potential, release efficiency and loading efficiency of nanoparticles using an irregular factorial design. The cytotoxicity of DOX-loaded biotin-targeted micelles was studied in HepG2 cells which over express biotin receptors by 3, 5-[dimethylthiazol-2-yl]-2, 5-diphenyl tetrazolium bromide assay. The successful synthesis of the biotinylated copolymer of chitosan/PMVEMA was confirmed by FTIR and HNMR. The optimised micelles showed the CMC of 33 μg/ml, particle size of 247 ± 2 nm, zeta potential of +9.46 mV, polydispersity index of 0.22, drug-loading efficiency of 71% and release efficiency of 84.5 ± 1.6%. The synthesised copolymer was not cytotoxic. The cytotoxicity of DOX-loaded in targeted micelles on HepG2 cell line was about 2.2-fold compared with free drug.
机译：通过酰胺反应分两步合成生物素化的壳聚糖/聚（甲基乙烯基醚-马来酸）（PMVEMA）共聚物。结构表征使用HNMR和傅立叶变换红外（FTIR）光谱进行。用pyr作为荧光探针测定共聚物的临界胶束浓度（CMC）。通过直接溶解法将阿霉素（DOX）装载在胶束中。使用不规则因子设计研究了不同变量（包括共聚物类型，共聚物浓度，搅拌速率和搅拌时间）对胶束的理化性质的影响，包括：粒径，ζ电势，纳米粒子的释放效率和负载效率。通过3，5- [5- [二甲基噻唑-2-基] -2，5-二苯基四氮唑溴化物]研究了在过量表达生物素受体的HepG2细胞中，DOX负载生物素靶向的胶束的细胞毒性。 FTIR和HNMR证实了壳聚糖/ PMVEMA生物素化共聚物的成功合成。优化的胶束显示CMC为33μg/ ml，粒度为247±2 nm，ζ电位为+9.46 mV，多分散指数为0.22，载药效率为71％，释放效率为84.5±1.6％。合成的共聚物没有细胞毒性。与游离药物相比，负载在靶向胶束中的DOX对HepG2细胞系的细胞毒性约为2.2倍。

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