基于避蚊胺/β-环糊精/O-羧甲基壳聚糖亲水性纳米胶囊载药及缓释性能研究  

Preparation and sustained-release of β-cyclodextrin/O-carboxymethyl chitosan nanocapsules loaded with hydrophobic diethyltoluamide

作　　者：刘月华[1] 季金苟[1] 郭红霞[1] 向存程 林辉焕 

机构地区：[1]重庆大学化学化工学院制药工程系,重庆400030

出　　处：《农药学学报》2017年第4期528-531,532,共5页Chinese Journal of Pesticide Science

基　　金：国家自然科学基金资助项目(213751569)

摘　　要：为了改善避蚊胺(diethyltoluamide,以下简称DEET)在水中的溶解度,首先采用饱和溶液法制备了避蚊胺/β-环糊精(diethyltoluamide/β-cyclodextrin,以下简称DEET/β-CD)包合物,其结构通过差示扫描量热仪(DSC)和X-射线衍射仪(XRD)表征;再采用离子交联法,以氯化钙为交联剂,制备了避蚊胺/β-环糊精/O-羧甲基壳聚糖(diethyltoluamide/β-cyclodextrin/Ocarboxymethyl chitosan,以下简称DEET/β-CD/O-CMC)亲水性纳米胶囊,用紫外-可见分光光度计(UV)、激光粒度分析仪和扫描电子显微镜(SEM)考察其理化性质;最后,考察包合物和纳米胶囊的缓释性能。结果表明:DEET与β-CD以物质的量之比1:1进行了包合,β-CD的加入使DEET的溶解度增加约27倍,该纳米胶囊的包封率为(79.93±2.08)%,载药量为(12.11±0.09)%,纳米胶囊呈椭圆形,平均粒径为(230.50±11.34)nm,Zeta电位为(–19.08±0.99)m V,PDI为0.055。在Tris-HCl(p H=7.4)缓冲液中释放试验显示,DEET/β-CD/O-CMC亲水性纳米胶囊比DEET/β-CD包合物有更好的缓释性能,24 h累积释放率分别为27.04%和38.10%。To improve water solubility of diethyltoluamide（DEET）, DEET/β-cyclodextrin（DEET/β-CD） inclusion compound was prepared by homogeneous coprecipition method. Differential scanning calorimetry（DSC） and XRD were used for the characterization of the inclusion compound. Then DEET/β-CD/O-CMC nanocapsules were prepared via a cross-linking reaction. DEET/β-CD/O-CMC nanocapsules were determined by UV spectrophotometer, mastersizer and SEM. Finally, the drug release property of DEET/β-CD and DEET/β-CD/O-CMC was studied. An inclusion complex was formed in 1：1 molar ratio. DEET solubility in the water was improved 27 times by introducing β-CD into the system. And the encapsulation efficiency and loading capacity of the prepared nanocapsules were（79.93 ± 2.08） % and（12.11 ± 0.09） %, respectively. The nanocapsules were oval in shape with average particle sizes of（230.50 ± 11.34） nm, Zeta potential of（–19.08 ± 0.99） m V, and PDI of 0.055.Release studies in Tris-HCl（pH = 7.4） evidenced β-CD/O-CMC nanocapsules have better sustainedrelease effect than DEET/β-CD. The DEET in DEET/β-CD/O-CMC and DEET/β-CD was released27.04% and 38.10% within 24 h, respectively.

关 键 词：避蚊胺 Β-环糊精 O-羧甲基壳聚糖 包合物 纳米胶囊 缓释性能 

分 类 号：TQ450.68[化学工程—农药化工]