Page 125 - 《精细化工》2022年第4期

第 39 卷第 4 期 精 细 化 工 Vol.39, No.4
2022 年 4 月 FINE CHEMICALS Apr. 2022

医药与日化原料
pH 响应改性木质素纳米粒子的制备及释药性能

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聂少飞 ，王闻达 ，郭博森 ，祁颢卓 ，魏浩宇 ，罗卫华 1,2,3*
（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）

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。
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
中图分类号：TQ469 文献标识码：A
文章编号：1003-5214 (2022) 04-0761-08 开放科学 (资源服务) 标识码 (OSID)：

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

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NIE Shaofei , WANG Wenda , GUO Bosen , QI Haozhuo , WEI Haoyu , LUO Weihua 1,2,3*
（1. School of Materials Science and Engineering, Central South University of Forestry & Technology, Changsha 410004,
Hunan, China; 2. Hunan Province Key Laboratory of Materials Surface & Interface Science and Technology, Central South
University of Forestry & Technology, Changsha 410004, Hunan, China; 3. Hunan Engineering Research Center of Woody
Biomass Conversion, Central South University of Forestry & Technology, Changsha 410004, Hunan, China）
Abstract: Copolymer maleylated lignin-g-polyvinylpyrrolidone (MEHL-g-PVP) was prepared by free-
radical 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 mL/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.
Key words: lignin; N-vinylpyrrolidone; response release; drug loading; drug materials

收稿日期：2021-11-25; 定用日期：2022-01-17; DOI: 10.13550/j.jxhg.20211206
基金项目：国家重点研发计划项目(2019YFB1503804，2018YFD0600302)
作者简介：聂少飞(1997—)，男，硕士生，E-mail：876554461@qq.com。联系人：罗卫华(1968—)，男，教授，E-mail：lwh6803@163.com。