目的:用异双官能低分子量聚乙二醇(PEG)(600和1395Da)修饰聚烯丙胺盐酸盐(PAH),以及随后的甘露糖附着,葡萄糖,或乳糖糖PEG,可导致形成具有凝集素结合亲和力和窄尺寸分布的聚胺磷酸盐纳米颗粒(PANs)。
方法:尺寸,多分散性,用透射电子显微镜(TEM)对糖基化聚乙二醇化PAN的内部结构进行了表征,动态光散射(DLS)和小角度X射线散射(SAXS)。荧光相关光谱(FCS)用于研究标记的乙二醇-聚乙二醇化PAN的缔合。形成纳米颗粒的聚合物链的数量由纳米颗粒形成后聚合物的互相关函数的幅度变化来确定。SAXS和荧光交叉相关光谱用于研究PAN与凝集素的相互作用:伴刀豆球蛋白A与甘露糖修饰的PAN,和Jacalin用乳糖改性的。
结果:Glyco-PEG化PAN是高度单分散的,具有几十纳米的直径和低电荷,和对应于具有高斯链的球体的结构。FCS显示PAN是单链纳米颗粒或由两个聚合物链形成。伴刀豆球蛋白A和Jamalin对糖聚乙二醇化的PAN显示出特异性相互作用,其亲和力高于牛血清白蛋白。
OBJECTIVE: Modification of polyallylamine hydrochloride (PAH) with heterobifunctional low molecular weight polyethylene glycol (PEG) (600 and 1395 Da), and subsequent attachment of mannose, glucose, or lactose sugars to PEG, can lead to formation of polyamine phosphate nanoparticles (PANs) with lectin binding affinity and narrow size distribution.
METHODS: Size, polydispersity, and internal structure of glycosylated PEGylated PANs were characterized by transmission electron microscopy (TEM), dynamic light scattering (DLS) and small angle X-ray scattering (SAXS). Fluorescence correlation spectroscopy (FCS) was used to
study the association of labelled glycol-PEGylated PANs. The number of polymer chains forming the nanoparticles was determined from the changes in amplitude of the cross-correlation function of the polymers after formation of the nanoparticles. SAXS and fluorescence cross-correlation spectroscopy were used to investigate the interaction of PANs with lectins: concanavalin A with mannose modified PANs, and jacalin with lactose modified ones.
RESULTS: Glyco-PEGylated PANs are highly monodispersed, with diameters of a few tens of nanometers and low charge, and a structure corresponding to spheres with Gaussian chains. FCS shows that the PANs are single chain nanoparticles or formed by two polymer chains. Concanavalin A and jacalin show specific interactions for the glyco-PEGylated PANs with higher affinity than bovine serum albumin.