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海藻酸辛酯衍生物载药微纳米胶束的合成及释药性 被引量:3

Synthesis and Release Properties of Drug-loaded Micro-/Nano-micelles Based on Octyl Alginate Derivative
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摘要 为了拓宽海藻酸盐的应用范围,以1-溴辛烷为疏水改性剂,采用双分子亲核取代反应(SN2)制备海藻酸辛酯衍生物(OAD),通过FTIR、1HNMR对其结构进行了鉴定,并采用TGA、XRD、荧光光谱(FM)、表面张力(SFT)、TEM、激光粒度和Zeta电位分析仪对其性能进行了表征。结果表明,辛基侧链的接枝使OAD的分子内氢键断裂,热稳定性下降,失重率增大,同时伴随微晶结构的改变。并且海藻酸钠(SA)与OAD的临界聚集质量浓度(CAC)分别为1.09和0.34 g/L,其SFT也随浓度的增大而逐步降低。相比SA,OAD胶束的水动力学粒径(dH)由446.7 nm变为342.0 nm,Zeta电位由-36.4 mV降为-39.3 mV,说明OAD具有一定的胶体界面活性。OAD胶束对负载的布洛芬具有一定的缓释作用,药物的释放过程属于Non-Fickian扩散机制。 In order to broaden the application range of alginate,an octylalginate derivative(OAD)was prepared by bimolecular nucleophilic substitution reaction(SN2)using 1-bromooctane as hydrophobic modifier.Its structure and properties were characterized by means of FTIR,1 HNMR,TGA,XRD,fluorescence spectrum(FM),surface tension(SFT),TEM,laser particle and zeta potential analyzers.The results showed that the graft of octyl side chains led to the fracture of the intramolecular hydrogen bond of OAD,the decrease of its thermal stability,the increase of its weight loss rate and the change of its microcrystalline structure.In addition,the critical aggregation mass concentration(CAC)of sodium alginate(SA)and OAD were 1.09 and 0.34 g/L,respectively.Meanwhile,the SFT gradually decreased as the concentration increased.Compared with those of SA,the hydrodynamic particle size(dH)of OAD decreased from 446.7 nm to 342.0 nm and the zeta potential decreased from?36.4 m V to?39.3 m V,indicating that OAD possessed certain colloidal interfacial activity.The ibuprofen-loaded OAD micelles had certain sustained-release properties,and the drug release process was fitted well with the Non-Fickian diffusion model.
作者 冯美西 王艳芳 陈秀琼 窦文杰 颜慧琼 林强 FENG Mei-xi;WANG Yan-fang;CHEN Xiu-qiong;DOU Wen-jie;YAN Hui-qiong;LIN Qiang(Key Laboratory of Tropical Medicinal Resource Chemistry of Ministry of Education,Hainan Normal University,Haikou571158,Hainan,China;Key Laboratory of Water Pollution Treatment and Resource Reuse of HainanProvince,Hainan Normal University,Haikou571158,Hainan,China)
出处 《精细化工》 EI CAS CSCD 北大核心 2019年第9期1780-1786,1856,共8页 Fine Chemicals
基金 海南省高等学校科学研究项目(Hnky2019-36) 海南省自然科学基金项目(218QN233) 海南省研究生创新科研课题资助项目(Hys2018-207)
关键词 双分子亲核取代反应 海藻酸辛酯衍生物 临界聚集浓度 微纳米胶束 缓释性能 功能材料 bimolecular nucleophilic substitution reaction octyl alginate derivative critical aggregation concentration micro-/nano-capsules sustained-release property functional materials
作者简介 冯美西(1991—),女,硕士生;联系人:颜慧琼(1986—),男,讲师,博士,E-mail:yanhqedu@163.com。
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