PEG-PCL载姜黄素胶束的构建及其评价  

Construction and evaluation of curcumin-loaded micelles of PEG-PCL

作　　者：张琳暄 白思蕊 陈彬[1,2] 杨丹 ZHANG Lin-xuan;BAI Si-rui;CHEN Bin;YANG Dan(School of Food Science and Engineering,Shaanxi University of Science&Technology,Xi′an 710021,China;Xi′an Key Laboratory of Antiviral and Anti-multidrug Resistant Bacteria Drugs Research and Development,Xi′an 710021,China)

机构地区：[1]陕西科技大学食品科学与工程学院,陕西西安710021 [2]西安市抗病毒与抗多药耐药菌药物研发重点实验室,陕西西安710021

出　　处：《陕西科技大学学报》2024年第6期69-78,共10页Journal of Shaanxi University of Science & Technology

基　　金：国家自然科学基金项目(82003699);陕西省西安市科学技术协会青年人才托举计划项目(959202313046)。

摘　　要：姜黄素(Curcumin,CUR)来源于植物姜黄的干燥根茎,价格低廉易获得,颜色鲜亮且具有抗炎、抗氧化、抗癌等多种活性,已被广泛应用于食品、药品领域.但因水溶性差,生物利用度低,CUR的用途受到限制.为应对这些问题,选用了两亲性共聚物聚(乙二醇)-b-聚(ε-己内酯)(poly(ethylene glycol)-b-poly(ε-caprolactone),PEG-PCL)制备胶束,并对系列PEG-PCL胶束的形成机制、载药性能、稳定性、释放和细胞摄取进行系统的评价.基于不同分子量PEG-PCL(PEG 2K-PCL 3.5K、PEG 2K-PCL 5K、PEG 5K-PCL 3K、PEG 5K-PCL 5K、PEG 5K-PCL 13K)制备所得的系列胶束显示出很高的封装效率,其中PEG 2K-PCL 5K包封率可达98.38±3.06%.PEG-PCL的封装有效改善了CUR的溶出,并表现出一定的缓释能力,同时提升了CUR的抗氧化活性.胶束外观清澈透亮,冻干后可重新分散于水中,具有很好的稳定性.细胞实验表明PEG-PCL胶束生物相容性良好,且能够被细胞摄取.另外,研究发现胶束的粒径、包封率等载药性能、细胞摄取效率与PEG-PCL分子量有关.总之,PEG-PCL胶束提高了CUR的溶解度、稳定性及细胞摄取能力,可为疏水生物活性分子的有效递送提供思路.Curcumin(CUR)is extracted from the dried rhizome of Curcuma longa.It is cost-effective and easily accessible,exhibiting vibrant hues.Moreover,it encompasses a wide range of activities including anti-inflammatory,antioxidant,and anticancer properties.However,the application of CUR is constrained by its limited water solubility and low bioavailability.The amphiphilic copolymer poly(ethylene glycol)-b-poly(ε-caprolactone)(PEG-PCL)was employed for the preparation of micelles to solve these issues.The formation mechanism,drug loading performance,stability,release and cellular uptake of PEG-PCL micelles were comprehensively evaluated.A series of micelles based on PEG-PCL with different molecular weights(PEG 2K-PCL3.5K,PEG 2K-PCL 5K,PEG 5K-PCL 3K,PEG 5K-PCL 5K,PEG 5K-PCL 13K)showed high encapsulation efficiency.The encapsulation efficiency of PEG 2K-PCL 5K reached 98.38±3.06%,demonstrating high efficacy in encapsulation.The encapsulation of PEG-PCL significantly enhanced the dissolution rate of CUR and exhibited a sustained release effect,concurrently augmenting the antioxidant capacity of CUR.The micelles exhibit a transparent appearance,demonstrating excellent stability,and they can be re-dispersed in water after freeze-drying.PEG-PCL micelles demonstrated the excellent biocompatibility and could be internalized by enterocyte.Meanwhile,the molecular weight of PEG-PCL was correlated with the particle size,encapsulation efficiency,drug loading performance,and cellular uptake efficiency of micelles.In summary,the utilization of PEG-PCL micelles enhanced the solubility,stability,and cellular uptake of CUR,thereby offering potential strategies for the efficient delivery of hydrophobic bioactive molecules.

关 键 词：PEG-PCL 胶束 姜黄素 体外释放 抗氧化 

分 类 号：R944.9[医药卫生—药剂学]