带叔胺的两亲嵌段共聚物的合成及其载光敏剂胶束用于光疗抗菌

Synthesis of Amphiphilic Block Copolymer and Its Photosensitizer-Loaded Micelles for Photothermal Sterilization

光照杀菌具有精准可控、不会使细菌产生耐药性的特点,同时细菌微环境显酸性、细菌细胞壁带负电。针对上述特性,设计并合成了能在细菌微酸中质子化的两亲聚合物聚乙二醇单甲醚-b-聚(2-(二乙氨基)甲基丙烯酸乙酯)和聚乙二醇单甲醚-b-聚(甲基丙烯酸羟乙酯-co-甲基丙烯酸二乙氨基乙酯)(分别记为PD和PHD),将其胶束包载光敏剂IR780和白藜芦醇(RES)并用于光照杀菌。采用核磁、红外对聚合物结构进行了表征。用动态光散射仪、透射电子显微镜、紫外光谱和荧光光谱对空白和载IR780/RES胶束的粒径、粒径分布、表面电荷、形貌以及载药量等性质进行了表征。结果表明,PD或PHD及载药胶束均呈现球形结构,包载IR780/RES双药时,载药量明显比单独包载IR780时增加。载药胶束808 nm光照对金黄色葡萄球菌(S.aureus)和大肠杆菌(E.coli)的杀菌率均在99%及以上。PD胶束减弱IR780光漂白的效果略优于PHD,两者均可用于多次光照杀菌。

Based on the characteristics of accurate and controllable sterilization and non-development of bacterial resistance by light,as well as the slightly acidic environment at the site of bacterial infection and the negatively charged,in this paper,two amphiphilic polymers,polyethylene glycol monomethyl ether-b-poly(2-(diethylamino)ethyl methacrylate) and polyethylene glycol monomethyl ether-b-poly(hydroxyethyl methacrylate-co-diethylamino ethyl methacrylate)(PD and PHD,respectively) were designed and synthesized,which can be protonated in bacterial micro acid.Their micelles were loaded with photosensitizers IR780 and resveratrol(RES) for light sterilization.The structures of the polymers were characterized by NMR and FT-IR.The particle size,size distribution,surface charge,morphology and drug loading of blank and IR780/RES loaded micelles were characterized by dynamic light scattering(DLS),transmission electron microscopy(TEM),ultraviolet(UV) and fluorescence spectroscopy(FL).The results show that PD or PHD micelles and their drug loaded micelles are spherical in structure.The drug loading amounts of IR780 or RES alone in PD or PHD are very low,while the drug loading amounts of IR780 and RES together in PD or PHD dramatically increase.The bactericidal rates of the drug loaded micelles against S.aureus and E.coli under 808 nm light are above 99%.The two drug loaded micelles repeatedly demonstrate excellent antibactericidal effect.