pH响应改性木质素纳米粒子的制备及释药性能  

Preparation and drug release properties of pH-responsive modified lignin nanoparticles

作　　者：聂少飞 王闻达 郭博森 祁颢卓 魏浩宇 罗卫华[1,2,3] NIE Shaofei;WANG Wenda;GUO Bosen;QI Haozhuo;WEI Haoyu;LUO Weihua(School of Materials Science and Engineering,Central South University of Forestry&Technology,Changsha 410004,Hunan,China;Hunan Province Key Laboratory of Materials Surface&Interface Science and Technology,Central South University of Forestry&Technology,Changsha 410004,Hunan,China;Hunan Engineering Research Center of Woody Biomass Conversion,Central South University of Forestry&Technology,Changsha 410004,Hunan,China)

机构地区：[1]中南林业科技大学材料科学与工程学院,湖南长沙410004 [2]中南林业科技大学材料表界面科学与技术湖南省重点实验室,湖南长沙410004 [3]中南林业科技大学湖南省木本生物质转化工程技术研究中心,湖南长沙410004

出　　处：《精细化工》2022年第4期761-768,共8页Fine Chemicals

基　　金：国家重点研发计划项目(2019YFB1503804,2018YFD0600302)。

摘　　要：以酶解木质素(EHL)和N-乙烯基吡咯烷酮(NVP)为主要原料,通过自由基聚合制备了共聚物马来酰化木质素-g-聚乙烯吡咯烷酮(MEHL-g-PVP),随后将共聚物自组装得到了直径约为40 nm的pH响应性纳米粒子。考察了化学修饰、聚合物浓度、水滴加速度、搅拌速度、水含量和投药量对纳米粒子形貌、尺寸和载药性能的影响。结果表明,当聚合物初始质量浓度为1.0 g/L、搅拌转速为600 r/min、去离子水滴加速度为60 mL/min、水含量为80%,纳米粒子与布洛芬(IBU)的质量比为10∶3时,纳米粒子的最大载药量可达35.29%±2.3%,包封率为68.17%±1.9%。体外药物释放实验结果表明,MEHL-g-PVP具有明显的pH响应能力,在模拟人体内肠道环境和胃液中,IBU的72 h累积释放量分别为63.75%和11.10%。体外细胞毒性实验结果表明,MEHL-g-PVP载药纳米粒子对正常细胞无细胞毒性,而对结肠癌细胞具有很好的抑制作用。Copolymer maleylated lignin-g-polyvinylpyrrolidone(MEHL-g-PVP) was prepared by freeradical polymerization using enzymatically hydrolyzed lignin(EHL) and N-vinylpyrrolidone(NVP) as main raw materials. And then the copolymer was self-assembled to obtain pH-responsive nanoparticles with a diameter of about 40 nm. The effects of chemical modification, polymer concentration, addition rate of water, stirring speed, water content and drug dosage on morphology, size and drug-carrying properties of nanoparticles were investigated. The results showed that when the initial mass concentration of polymer was 1.0 g/L, stirring speed was 600 r/min, addition rate of deionized water was 60 m L/min and water content was 80%, the mass ratio of nanoparticles and ibuprofen(IBU) was 10∶3, the maximum drug loading and encapsulation rate of nanoparticles could reach 35.29%±2.3% and 68.17%±1.9%, respectively.In vitro drug release indicated that MEHL-g-PVP had obvious pH response ability, and the release amount of IBU was 63.75% and 11.10% in 72 h in simulated intestinal environment and gastric juice of human body, respectively. The results of in vitro cytotoxicity test indicated that MEHL-g-PVP drug-loaded nanoparticles had no cytotoxicity to normal cells and had a good inhibitory effect on colon cancer cells.

关 键 词：木质素 N-乙烯基吡咯烷酮 响应释放 载药量 医药原料 

分 类 号：TQ469[化学工程—制药化工]