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用于制备基于自组装两亲性聚(ε-己内酯)-聚(乙二醇)嵌段共聚物的胶束纳米颗粒以用于药物递送的热冷法。

The heat-chill method for preparation of self-assembled amphiphilic poly(ε-caprolactone)-poly(ethylene glycol) block copolymer based micellar nanoparticles for drug delivery.

作者信息

Payyappilly Sanal Sebastian, Dhara Santanu, Chattopadhyay Santanu

机构信息

Rubber Technology Centre, Indian Institute of Technology, Kharagpur, West Bengal 721302, India.

出版信息

Soft Matter. 2014 Apr 7;10(13):2150-9. doi: 10.1039/c3sm52699b.

Abstract

A new method is developed for preparation of amphiphilic block copolymer micellar nanoparticles and investigated as a delivery system for celecoxib, a hydrophobic model drug. Biodegradable block copolymers of poly(ethylene glycol) (PEG) and poly(ε-caprolactone) (PCL) were synthesized by ring opening copolymerization and characterized thoroughly using FTIR, (1)H NMR and GPC. The block copolymer was dispersed in distilled water at 60 °C and then it was chilled in an ice bath for the preparation of the micellar nanoparticles. Polymers self-assembled to form micellar nanoparticles (<50 nm) owing to their amphiphilic nature. The prepared micellar nanoparticles were analyzed using HR-TEM, DLS and DSC. The cytotoxicity of the polymer micellar nanoparticles was investigated against HaCaT cell lines. The study of celecoxib release from the micellar nanoparticles was carried out to assess their suitability as a drug delivery vehicle. Addition of the drug to the system at low temperature is an added advantage of this method compared to the other temperature assisted nanoparticle preparation techniques. In a nutshell, polymer micellar nanoparticles prepared using the heat-chill method are believed to be promising for the controlled drug release system of labile drugs, which degrade in toxic organic solvents and at higher temperatures.

摘要

开发了一种制备两亲性嵌段共聚物胶束纳米颗粒的新方法,并将其作为疏水性模型药物塞来昔布的递送系统进行了研究。通过开环共聚合成了聚乙二醇(PEG)和聚己内酯(PCL)的可生物降解嵌段共聚物,并使用傅里叶变换红外光谱(FTIR)、核磁共振氢谱(¹H NMR)和凝胶渗透色谱(GPC)对其进行了全面表征。将嵌段共聚物在60℃下分散于蒸馏水中,然后在冰浴中冷却以制备胶束纳米颗粒。由于其两亲性,聚合物自组装形成胶束纳米颗粒(<50 nm)。使用高分辨率透射电子显微镜(HR-TEM)、动态光散射(DLS)和差示扫描量热法(DSC)对制备的胶束纳米颗粒进行了分析。研究了聚合物胶束纳米颗粒对HaCaT细胞系的细胞毒性。进行了塞来昔布从胶束纳米颗粒中的释放研究,以评估它们作为药物递送载体的适用性。与其他温度辅助纳米颗粒制备技术相比,在低温下将药物添加到系统中是该方法的一个额外优势。简而言之,使用热冷法制备的聚合物胶束纳米颗粒被认为在不稳定药物的控释系统中具有前景,这些药物在有毒有机溶剂中和较高温度下会降解。

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