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
投稿时间:2016-12-05      点此下载全文 HTML
引用本文:刘月华,季金苟,郭红霞,向存程,林辉焕,等.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[J].农药学学报,2017,19(4):528-532.
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作者单位E-mail
刘月华 重庆大学 化学化工学院 制药工程系, 重庆 400030  
季金苟 重庆大学 化学化工学院 制药工程系, 重庆 400030 725_tiger@sina.com 
郭红霞 重庆大学 化学化工学院 制药工程系, 重庆 400030  
向存程 重庆大学 化学化工学院 制药工程系, 重庆 400030  
林辉焕 重庆大学 化学化工学院 制药工程系, 重庆 400030  
基金项目:国家自然科学基金资助项目(213751569)
中文摘要: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/O-carboxymethyl 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)mV,PDI为0.055。在Tris-HCl(pH=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%。
中文关键词: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
 
Preparation and sustained-release of β-cyclodextrin/O-carboxymethyl chitosan nanocapsules loaded with hydrophobic diethyltoluamide
Abstract: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) mV, and PDI of 0.055. Release studies in Tris-HCl (pH = 7.4) evidenced β-CD/O-CMC nanocapsules have better sustained-release effect than DEET/β-CD. The DEET in DEET/β-CD/O-CMC and DEET/β-CD was released 27.04% and 38.10% within 24 h, respectively.
Key words:DEET  β-cyclodextrin  O-carboxymethyl chitosan  inclusion compound  nanocapsules  sustained-release
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