Abstract:
In response to the pressing demand for functional nanomaterials synthesis and applications, two polyelectrolyte complexes (PECs) [electrostatic and cross-linked nanogels (NGs)] loaded individually with caffeic acid (CafA) and eugenol (Eug) demonstrating multifunctionalities were proposed for the first time. Curdlan (Curd) and glucomannan (GM) were carboxymethylated (CMCurd and CMGM) successfully and polymeric ratios of 1:1 and 4:1 (v/v) for chitosan (Cs): CMCurd and lactoferrin (Lf): CMGM were selected for the synthesis of Cs/CMCurd and Lf/CMGM NGs. Due to the use of EDC/NHS, Cs/CMCurd/CafA and Lf/CMGM/Eug NGs possessed very uniform particles sizes of 177 ± 18 and 230 ± 17 nm with marked encapsulation efficiencies (EEs) of 76 ± 4 and 88 ± 3 %, respectively. The formation of a carbonyl-amide linkage in both cross-linked NGs was confirmed by FTIR. It should be noted, the self-assembly was not reliable in retaining enough of the encapsulated compounds. Owing to the excellent physicochemical characteristics of the loaded cross-linked NGs, they were prioritized over the electrostatic ones. Both Cs/CMCurd/CafA and Lf/CMGM/Eug NGs exhibited high colloidal stability over 12 weeks, elevated hemocompatibility, and in vitro serum stability. The generated NGs were also tailored to possess controlled release profiles for CafA and Eug over 72 h. Cs/CMCurd/CafA and Lf/CMGM/Eug NGs had promising antioxidant efficacies and could remarkably inhibit 4 bacterial pathogens at low 2-16 μg/mL concentration of encapsulated NGs compared to their unencapsulated counterparts. Interestingly, the respective NGs could significantly decline the IC50 against colorectal cancer HCT-116 than conventional drugs. Based on these data, it was conferred that the investigated NGs could be promising candidates for functional foods and pharmaceutics.
摘要:
针对功能纳米材料合成和应用的迫切需求,首次提出了两种分别负载咖啡酸(CafA)和丁香酚(Eug)的聚电解质复合物(PECs)[静电和交联纳米凝胶(NGs)],它们具有多功能性。Curdlan(Curd)和葡甘露聚糖(GM)被成功地羧甲基化(CMCurd和CMGM),壳聚糖(Cs):CMCurd和乳铁蛋白(Lf)的聚合物比例为1:1和4:1(v/v):选择CMGM用于合成Cs/CMCurd和Lf/CMGMNG。由于使用EDC/NHS,Cs/CMCurd/CafA和Lf/CMGM/EugNG具有非常均匀的177±18和230±17nm的粒径,显着封装效率(EEs)为76±4和88±3%,分别。通过FTIR确认在两个交联的NG中形成羰基-酰胺键。应该注意,自组装在保留足够的包封化合物方面是不可靠的。由于负载的交联NG具有优异的物理化学特性,它们优先于静电。Cs/CMCurd/CafA和Lf/CMGM/EugNGs在12周内都表现出很高的胶体稳定性,血液相容性升高,和体外血清稳定性。生成的NG也被定制为在72小时内具有CafA和Eug的受控释放曲线。Cs/CMCurd/CafA和Lf/CMGM/EugNG具有有希望的抗氧化功效,并且可以在低2-16μg/mL浓度的包封NG下显著抑制4种细菌病原体。有趣的是,与常规药物相比,各自的NG可显著降低对结直肠癌HCT-116的IC50.基于这些数据,据认为,所调查的NG可能是功能性食品和药物的有希望的候选人。