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Preparation and characterization of biodegradable nanoparticles based on amphiphilic poly(3-hydroxybutyrate)–poly(ethylene glycol)–poly(3-hydroxybutyrate) triblock copolymer

机译:基于两亲性聚3-羟基丁酸酯-聚乙二醇-聚3-羟基丁酸酯三嵌段共聚物的可生物降解纳米粒子的制备与表征

摘要

Amphiphilic triblock copolymers of poly(3-hydroxybutyrate)–poly(ethylene glycol)–poly(3-hydroxybutyrate) (PHB–PEG–PHB) were directly synthesized by the ring-opening copolymerization of β-butyrolactone monomer using PEG as macroinitiator. Their structure, thermal properties and crystallization were investigated by 1H NMR, differential scanning calorimetry (DSC) and X-ray diffraction. It was found that both PHB and PEG blocks were miscible. With the increase in the PHB block length, the triblock copolymers became amorphous because amorphous PHB block remarkably depressed the crystallization of the PEG block. Biodegradable nanoparticles with core-shell structure were prepared in aqueous solution from the amphiphilic triblock copolymers, and characterized by 1H NMR, SEM and fluorescence. The hydrophobic PHB segments formed the central solid-like core, and stabilized by the hydrophilic PEG block. The nanoparticle size was close related to the initial concentrations of the nanoparticle dispersions and the compositions of the triblock copolymers. Moreover, the PHB–PEG–PHB nanoparticles also showed good drug loading properties, which suggested that they were very suitable as delivery vehicles for hydrophobic drugs.
机译:聚(3-羟基丁酸酯)-聚(乙二醇)-聚(3-羟基丁酸酯)(PHB-PEG-PHB)的两亲三嵌段共聚物是通过以PEG为大分子引发剂的β-丁内酯单体的开环共聚反应直接合成的。通过1 H NMR,差示扫描量热法(DSC)和X射线衍射研究了它们的结构,热性质和结晶。发现PHB和PEG嵌段都是可混溶的。随着PHB嵌段长度的增加,三嵌段共聚物变成无定形的,因为无定形的PHB嵌段显着降低了PEG嵌段的结晶。由两亲三嵌段共聚物在水溶液中制备具有核-壳结构的可生物降解的纳米颗粒,并通过1 H NMR,SEM和荧光进行表征。疏水性PHB链段形成了中心的固态核,并被亲水性PEG嵌段稳定。纳米颗粒尺寸与纳米颗粒分散体的初始浓度和三嵌段共聚物的组成密切相关。此外,PHB–PEG–PHB纳米颗粒还显示出良好的载药性能,这表明它们非常适合用作疏水性药物的输送载体。

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