Page 156 - 《精细化工》2020年第2期

第 38 卷第 2 期 精 细 化 工 Vol.38, No.2
202 1 年 2 月 FINE CHEMICALS Feb. 2021

医药与日化原料
可注射 CS/PLLA-SA 复合水凝胶的制备及载药性

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孙苗苗 ，魏培贺 ，康 纯 1,2 ，刘魏征 ，郝 红
（1. 西北大学 化工学院，陕西 西安 710069；2. 西安理工大学 水利水电学院，陕西 西安 710048）
摘要：采用先核后臂法以及丁二酸酐（SA）羧基化修饰合成了末端为羧基的四臂星型聚乳酸（PLLA-SA），将
其加入丙酮中得到 PLLA-SA 纳米分散液。壳聚糖（CS）与分散液通过静电作用自组装形成可注射 CS/PLLA-SA
复合水凝胶，采用 Zeta 电位及激光粒度仪、FTIR 和 SEM 等对 PLLA-SA、分散液及水凝胶的组成、结构和性能
进行表征与测定。结果表明，PLLA-SA 的 Zeta 电位值为–21.89 mV，其分散液的平均粒径为 216 nm。在温度为
15 ℃，PLLA-SA 质量浓度为 5 g/L，布洛芬（IBU）与 PLLA-SA 质量比为 1∶2，650 r/min 搅拌 1 h，550 r/min
搅拌 4 h 的条件下，制备出载 IBU 的 PLLA-SA 分散液。将该分散液与质量浓度为 10 g/L 的壳聚糖盐酸盐
（CS-HCl）水溶液按体积比为 7∶3 混合，快速自组装形成载药 CS/PLLA-SA 复合水凝胶，包封率和载药量分
别达到 85.38%和 28.46%。体外药物释放结果表明，可注射载药水凝胶对 IBU 具有明显的缓释作用，30 h 内药
物的累积释放率可达到 95.81%。
关键词：PLLA-SA；壳聚糖；可注射水凝胶；布洛芬；医药原料
中图分类号：TQ427.3；TQ460.4 文献标识码：A
文章编号：1003-5214 (2021) 02-0358-08 开放科学 (资源服务) 标识码 (OSID)：

Preparation and drug loading properties of an injectable
CS/PLLA-SA composite hydrogel

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SUN Miaomiao , WEI Peihe , KANG Chun , LIU Weizheng , HAO Hong
（1. School of Chemical Engineering, Northwest University, Xi'an 710069, Shaanxi, China; 2. Conservancy and
Hydropower College, Xi´an University of Technology, Xi'an 710048, Shaanxi, China）
Abstract: A four-armed star-shaped polylactic acid (PLLA-SA) copolymer with carboxyl carboxyl terminus
was synthesized by core-first technique and carboxylation of succinic anhydride (SA), and was dispersed
into acetone to obtain PLLA-SA nano-dispersion solution. Then, an injectable CS/PLLA-SA composite
hydrogel was obtained by electrostatic action between chitosan (CS) and the dispersion. The composition,
structure and properties of PLLA-SA, PLLA-SA nano-dispersion and CS/PLLA-SA hydrogel were
characterized by laser particle size and Zeta potential analyzer, FTIR and SEM. The Zeta potential value of
PLLA-SA was –21.89 mV, the average particle size of PLLA-SA nano-dispersion solution was 216 nm.
Ibuprofen (IBU)-PLLA-SA nano-dispersion solution was prepared under the conditions of temperature of
15 ℃, PLLA-SA mass concentration of 5 g/L, m(IBU)∶m(PLLA-SA) = 1∶2, stirring speed of 650 r/min
for 1 h, then 550 r/min for 4 h. The IBU-PLLA-SA nano-dispersion was mixed chitosan hydrochloride
(CS-HCl) with a mass concentration of 10 g/L at a volume ratio of 7∶3, which was rapid self-assembly to
form a drug-loaded CS/PLLA-SA composite hydrogel. The loading efficiency and loading content of the
composite hydrogel reached 85.38% and 28.46%, respectively. In vitro drug release results indicated that
the injectable CS/PLLA-SA composite hydrogel exhibited an obvious sustained-release capability for IBU,
and the cumulative release rate of IBU within 30 h could reach 95.81%.
Key words: PLLA-SA; chitosan; injectable hydrogel; ibuprofen; drug materials

收稿日期：2020-07-04; 定用日期：2020-10-10; DOI: 10.13550/j.jxhg.20200593
作者简介：孙苗苗（1996—），女，硕士生。联系人：郝 红（1966—），女，教授，E-mail：haohong@nwu.edu.cn。