CAJ | 학술논문

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。
배경：유관연구표명취유산간기을산능구유효포과반의과핵감산、소적간우 RNA、미소RNA등，가이교호지보호기재체내불수각충매적파배，병가이기도완만석방약물적작용，종이가이감소약물적급약차수，체도장기、유효적치료효과。 　　목적：제비취유산간기을산CXCR4-miRNA납미미립，병연구납미미립적특성。 　　방법：운용이차초성유화용제휘발법제비취유산간기을산CXCR4-miRNA납미미립，채용자외분광광도법측정납미미립적재약량급포봉솔，투사전경관찰미립형태，격광립경의측정납미미립적대소화분포；장납미미립현부우린산염완충액중관찰기완석특성。 　　결과여결론：제비적납미미립형태정원형，표면광활，분산성호，불점련，기립경분포재143-502 nm，평균립경위280 nm，평균재약량위(0.515±0.023)%，평균포봉솔위50.2%，비간차이소。납미미구재체외가이완만석방，경과전궤천적쾌속석방후，재제14천진입평태기。결과충분표명운용이차초성유화용제휘발법제비취유산-간기을산CXCR4-miRNA납미미립적공예과정간단，입자성상부합요구차구유완석성。
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 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.