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叶酸修饰的粉防己碱壳聚糖-硬脂酸纳米胶束的制备、表征及体

外抗炎活性考察
Δ

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薛 飞 ，杨 岚，常金花，刘 沛，王汝兴（承德医学院中药研究所/河北省中药研究与开发重点实验室，河北
承德 067000）

中图分类号 R943；R965 文献标志码 A 文章编号 1001-0408（2024）08-0925-06
DOI 10.6039/j.issn.1001-0408.2024.08.05

摘 要 目的 制备叶酸（FA）修饰的粉防己碱（TET）壳聚糖（CS）-硬脂酸（SA）纳米胶束（简称“FA-CS-SA/TET纳米胶束”），并进
行表征和体外抗炎活性考察。方法 采用超声法制备FA-CS-SA/TET纳米胶束，以包封率（EE）、载药量（DL）、粒径的综合评分为
评价指标，FA-CS-SA与TET质量比、超声功率和超声次数为考察因素，根据正交实验确定最优制备工艺并验证；对以最优工艺制
备的FA-CS-SA/TET纳米胶束进行表征，并考察其体外释放性能。以RAW264.7细胞为实验对象，考察其体外抗炎活性。结果 最
优制备工艺为 FA-CS-SA 与 TET 质量比 2∶1，超声功率 200 W，超声 200 次。以最优工艺制备的 FA-CS-SA/TET 纳米胶束的 EE 为
（98.86±0.30）%，DL 为（28.57±0.34）%，平均粒径为（227.0±9.4）nm，多分散性指数为 0.42±0.04，Zeta电位为（12.6±2.3）mV；该
纳米胶束呈类圆形且分布均匀，其在0.5%十二烷基硫酸钠溶液中释放较快，72 h内的累积释放度为（79.49±3.43）%，且其抗炎作
用强于 TET 原料药。结论 本研究成功制备了 FA-CS-SA/TET 纳米胶束，其载药性能良好，粒径均匀，且具有较好的体外抗炎
活性。
关键词 粉防己碱；纳米胶束；制备工艺；表征；抗炎活性；释放度

Preparation， characterization and in vitro anti-inflammatory activity of tetrandrine-loaded chitosan-stearic
acid nano micelles modified with folic acid
XUE Fei，YANG Lan，CHANG Jinhua，LIU Pei，WANG Ruxing（Institute of Chinese Materia Medica of Chengde

Medical University/Hebei Provincial Key Laboratory of Research and Development for Chinese Materia Medica，
Hebei Chengde 067000， China）

ABSTRACT OBJECTIVE To prepare tetrandrine （TET）-loaded chitosan（CS）-stearic acid （SA） nano micelles modified with
folic acid （FA） （FA-CS-SA/TET nano micelles）， characterize them and study the anti-inflammatory effect in vitro. METHODS FA-
CS-SA/TET nano micelles were prepared by ultrasonic method； the preparation technology was optimized by orthogonal test and
validation test was also performed with the mass ratio of FA-CS-SA to TET， ultrasound power and ultrasound times as the factors，
using the comprehensive score of entrapment efficiency （EE）， drug loading （DL） and particle size as evaluation index. FA-CS-SA/
TET nano micelles prepared by the optimal technology were characterized， and their release performance in vitro was investigated.
RAW264.7 cells were used as subjects to investigate their anti-inflammatory activity in vitro. RESULTS The optimal preparation
technology included that the mass ratio of FA-CS-SA to TET was 2∶1， ultrasonic power was 200 W， and the ultrasonic frequency
was 200 times. The parameters of FA-CS-SA/TET nano micelles prepared by optimized technology included that EE was （98.86±
0.30）%， DL was （28.57±0.34）%， the average particle size was （227.0±9.4） nm， polydispersity index was 0.42±0.04， and the
Zeta potential was（12.6±2.3）mV， respectively. The nano micelles were uniform in appearance and round in shape. The nano
micelles were released quickly in 0.5% sodium dodecyl sulfate solution， with a cumulative release rate of （79.49±3.43）% within
72 hours， and its anti-inflammatory effect was stronger than that of TET raw materials. CONCLUSIONS FA-CS-SA/TET nano
micelles are prepared successfully in the study， with good
Δ 基金项目 河北省自然科学基金项目（No.H2022406073）；河北
省高等学校科学技术研究重点项目（No.ZD2021004）；承德医学院高 drug loading performance， uniform particle size， and good in
层次人才科研启动基金项目（No.201705） vitro anti-inflammatory activity.
＊第一作者 硕士研究生。研究方向：药物新剂型。E-mail： KEYWORDS tetrandrine； nano micelles； preparation techno-
741376718@qq.com
logy； characterization； anti-inflammatory activity； release rate
# 通信作者 教授，硕士生导师，博士。研究方向：药物新剂型。E-
mail：wangru1973@sina.com

中国药房 2024年第35卷第8期 China Pharmacy 2024 Vol. 35 No. 8 · 925 ·