内水相结构对微球包封率及控释行为的影响

Influences of Microparticle Internal Phase on Hydrophilic Drug Loading Efficiency and Releasing

采用水-油-水双乳化溶剂挥发法制备了聚乳酸-羟基乙酸共聚物(PLGA)/氧氟沙星载药微球,并考察了介孔硅、透明质酸、多聚赖氨酸不同内水相成分对微球粒径及其分布、表面形态、包封率以及释放特性的影响。研究结果表明,采用该方法制备出了内部具有多孔结构的载药微球;透明质酸内水相组微球平均粒度最大,粒径分布最小;介孔硅和透明质酸的加入提高了微球包封率;3种内水相组的初期爆释均高于对照组;多聚赖氨酸内水相组释放速率最快,透明质酸内水相组释放速率最慢。释放拟合曲线表明,4组不同内水相的微球,在释放区间内,释放行为都符合Slogistic方程式。

Poly（lactic-co-glycolic acid） （PLGA） microspheres containing ofloxacine were made using the doubleemulsion （water-in-oil-in-water） solvent extraction/evaporation method. The influences of mesoporous silica, hyaluronic acid, polylysine in internal aqueous solution on the microparticle size distribution, surface morphology, ofloxacine loading efficiency and release behavior were investigated. SEM pictures indicate that microparticles with the microcavities inside are fabricated. The average particle size of Haluronic acid （HA） internal phase group is largest and the span index is smallest. Loading efficiency increases in both raesoporous silica （MS） and HA internal phase groups but decreases in polylysine group. The burst release of all groups is higher than that of the control group. Releasing profiles present the release rates of polylysine internal phase microparticle is fastest, while HA internal phase microparticles present the slowest release rates. The fit curves of the drug release pattern of the microparticles with different internal phases accord with the Slogistic mathematic mode.