聚乳酸羟基乙酸CXCR4-miRNA纳米微粒的制备及其特征  

Preparation and characterization of poly D,L-lactide-co-glycolide CXCR4-miRNA nanoparticles

作　　者：高烽[1] 董勤[1] 崔杰[1] 陈培 王少良[1] 

机构地区：[1]武警上海总队医院肾脏内科,上海市201103

出　　处：《中国组织工程研究》2014年第43期6990-6995,共6页Chinese Journal of Tissue Engineering Research

基　　金：上海市卫生局青年课题项目(2011Y126);项目名称:不同载体介导CXCR4-miRNA抑制肾癌转移及其机制研究~~

摘　　要：背景:有关研究表明聚乳酸羟基乙酸能够有效包裹反义寡核苷酸、小的干扰RNA、微小RNA等,可以较好地保护其在体内不受各种酶的破坏,并可以起到缓慢释放药物的作用,从而可以减少药物的给药次数,达到长期、有效的治疗效果。目的:制备聚乳酸羟基乙酸CXCR4-miRNA纳米微粒,并研究纳米微粒的特性。方法:运用二次超声乳化溶剂挥发法制备聚乳酸羟基乙酸CXCR4-miRNA纳米微粒,采用紫外分光光度法测定纳米微粒的载药量及包封率,透射电镜观察微粒形态,激光粒径仪测定纳米微粒的大小和分布;将纳米微粒悬浮于磷酸盐缓冲液中观察其缓释特性。结果与结论:制备的纳米微粒形态呈圆形,表面光滑,分散性好,不粘连,其粒径分布在143-502 nm,平均粒径为280 nm,平均载药量为(0.515±0.023)%,平均包封率为50.2%,批间差异小。纳米微球在体外可以缓慢释放,经过前几天的快速释放后,在第14天进入平台期。结果充分表明运用二次超声乳化溶剂挥发法制备聚乳酸-羟基乙酸CXCR4-miRNA纳米微粒的工艺过程简单,粒子性状符合要求且具有缓释性。BACKGROUND：Related studies have showed that poly D,L-lactide-co-glycolide can effectively package antisense oligonucleotides, smal interfering RNA, microRNA. Poly D,L-lactide-co-glycolide can better protect them against the destruction of the enzymes in vivo and have slow the drug release. Therefore, the number of drug administration can be reduced to achieve a long-term and effective therapeutic effect. OBJECTIVE：To prepare poly D,L-lactide-co-glycolide-CXCR4-miRNA-nano-particles and to research the characteristics of the prepared nanoparticles. METHODS：Poly D,L-lactide-co-glycolide-CXCR4-miRNA nanoparticles were prepared by double emulsion-evaporation process. Ultraviolet spectrophotometry was utilized for measurement of encapsulation efficiency and drug-loading rate, observing the shape of nanoparticles by transmission electron microscope, and measuring the size and distribution of nanoparticles by laser particle size analyzer. Sustained-release characteristics of nanoparticle suspension were observed in phosphate buffer. RESULTS AND CONCLUSION：The prepared nanoparticles were spherical-shaped, smooth, evently distributed and inadhesive. The particle size was mainly distributed within 143-502 nm, with an average diameter of 280 nm. The average drug loading was （0.515±0.023）%, the average encapsulation ratio was 50.2%and difference＆amp;nbsp;between batches was smal . The nanoparticles could slowly release in vitro and the process initial y experienced the fast-release stage, and then reached a basical y stable platform stage at day 14. These finding indicate that the process to prepare poly D,L-lactide-co-glycolide CXCR4-miRNA-nanoparticles by double emulsion-evaporation is simple. The prepared nanoparticles are wel targeted and exhibit sustained-release effects.

关 键 词：乳酸 受体 CXCR4 微RNAS 微球体 

分 类 号：R318[医药卫生—生物医学工程]