摘要
目的研究c-FLIP反义寡核苷酸(c-FLIPantisenseoligodeoxynucleotide,c-FLIP ASODN)的聚乳酸聚羟乙酸(PL-GA)纳米粒的制备工艺,并通过实验对纳米粒子进行评价。方法通过二次超声乳化和溶剂挥发技术将PLGA用于基因导入的载体制备,并评价载c FLIP ASODN的PLGA纳米粒的特性,包括粒子形态、包封率和保护作用等。结果制备的纳米粒子外观呈规则的球形,其粒径尺寸平均为95.5nm,平均包封率为48%,载药量为(0.579±0.016)%,体外释放达15d,经过PLGA纳米粒的包裹,对c FLIP ASODN起到保护作用。结论纳米粒包裹的c FLIP ASODN制备工艺简便,粒子性状符合要求,并能有效保护反义寡核苷酸免于核酸酶的降解而延长其作用时间。
Objective:To study the technique for preparation of c-FLIP-antisense oligodeoxynucleotide-poly D,L-lacticco-glycolic acid (c-FLIP-ASODN-PLGA) nanoparticles and to evaluate the characteristics of the prepared nanoparticles. Methods: By double-emulsion evaporation technique, PLGA nanoparticle, a biodegradable and biocompatible polymer, was used to cover c-FLIP-ASODN as to prevent it from being degraded by nucleases. The characteristics of the nanoparticles, including morphology, encapsulation efficiency and protection rate were evaluated. Results: The prepared c-FLIP-ASODN-PLGA nanoparticles had regular spherical surfaces. The mean diameter of the particles was 95.5 nm and the mean encapsulation ratio was 48%. The proportion of c-FLIP-ASODN covered by the nanoparticles was (0.579±0.016)%, and the in vitro release duration was 15 d. The c-FLIP-ASODN was protected from degradation by nucleases after being covered by PLGA nanoparticles. Conclusion: The method for preparing c-FLIP-ASODN-PLGA nanoparticles is simple and can meet the requirement of pharmaceutics. The increased effective duration of c-FLIP-ASODN is due to encapsulation of nanoparticles, which protects c-FLIP-ASODN from degradation by nucleases.
出处
《第二军医大学学报》
CAS
CSCD
北大核心
2005年第5期547-550,共4页
Academic Journal of Second Military Medical University
基金
上海市科委专项基金(0352nm114).
