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

Gao Feng; Dong Qin; Cui Jie; Chen Pei; Wang Shao-liang

doi:10.3969/j.issn.2095-4344.2014.43.017

Abstract：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. <br> OBJECTIVE:To prepare poly D,L-lactide-co-glycolide-CXCR4-miRNA-nano-particles and to research the characteristics of the prepared nanoparticles. <br> 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. <br> 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.