Page 163 - 《精细化工》2020年第2期

第 2 期 孙苗苗，等: 可注射 CS/PLLA-SA 复合水凝胶的制备及载药性
2.8 载药 CS/PLLA-SA 复合水凝胶的释药性能
IBU 原料药及最佳条件制备的载药 CS/PLLA-
SA 复合水凝胶的体外药物累积释放曲线如图 8 所
示。从图 8 看出，IBU 原料药 3 h 的累积释放率已
达到 97.78%，而载药 CS/PLLA-SA 复合水凝胶对药
物有明显的控释能力，在释放过程中没有明显的突
释，30 h 内药物的累积释放率达到了 95.81%。IBU
在水凝胶中的药物释放过程大致分为 2 个阶段：
0~10 h 为第 1 阶段，药物释放速率较快速；10~30 h
为第 2 阶段，此阶段载药凝胶的药物释放速率增加
较为平缓。与姚伯龙等 [21] 制备的海藻酸钠凝胶载药
微球相比，将 IBU 为模型药物负载于 CS/PLLA-SA
复合水凝胶上缓释效果更为显著。
图 8 IBU 原料药及载药水凝胶的体外药物释放曲线
Fig. 8 In vitro drug release profiles of IBU and drug-loading
hydrogel
3 结论
（1）将 L-LA 采用配位开环聚合法制备 PET-
1
PLLA，并分别采用 FTIR、 HNMR 对 PET-PLLA 进
行结构表征，结果表明，产物为四臂星型 PET-PLLA，
在最优工艺条件下制备的 PLLA-SA 的 Zeta 电位值
为–21.89 mV。
（2）采用不添加表面活性剂的溶剂挥发法制备
了 PLLA-SA 分散液，通过单因素实验确定 PLLA-SA
分散液最佳制备工艺条件为：搅拌速率为 650 r/min，
PLLA-SA 质量浓度为 5 g/L，反应温度为 15 ℃。在
此条件下，制备的分散液中粒子平均粒径为 216 nm，
PDI 值为 0.236，颗粒表面形态较好，球形均匀。
（3）通过 SEM 观察到 CS/PLLA-SA 复合水凝胶
有明显孔结构，确定了制备 IBU 载药水凝胶的最佳
工艺条件为：m(IBU)∶m(PLLA-SA)=1∶2，PLLA-SA
质量浓度为 5 g/L，搅拌速率为 650 r/min，在此条件
下 制得载药凝胶的包封率为 85.38%，载药量为
28.46%。与 IBU 原料药的体外药物释放相比，IBU
载药水凝胶可以明显改善药物释放速率，达到缓释
效果。
·365·
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