普鲁兰多糖微球制备及影响因素考察

Preparation of pullulan microparticles and its influencing factors

目的采用水/油(W/O)乳化交联法制备普鲁兰多糖微球并观察多种因素对微球形态及粒径的影响。方法采用W/O乳化交联法,司班20作为表面活性剂,分别以蓖麻油和正己烷作为油相,不同浓度的普鲁兰多糖水溶液为水相,形成均一乳液后加入交联剂戊二醛,普鲁兰多糖被固化形成微球。观察普鲁兰多糖水溶液浓度、水/油比例、交联剂浓度、转速等多种因素对微球形态及大小的影响。通过扫描电镜观察微球形态,MastersizerS激光粒度仪进行粒径分析。结果油的成分、水/油比例、多糖水溶液浓度、交联剂浓度及搅拌速度均不同程度影响微球形态和大小。蓖麻油为油相形成微球条件:水/油<1∶5,普鲁兰多糖水溶液浓度1%,交联剂浓度5%～50%。这些条件下形成微球表面光滑、粒径分布均一。正己烷为油相形成微球条件:1∶5<水/油<1∶2,普鲁兰多糖水溶液浓度1%,交联剂浓度<25%,形成微球表面光滑,但粒径分布不均一。0.2%或5%普鲁兰多糖水溶液、转速<200r/min均不能形成微球。结论采用W/O乳化交联法能够制备普鲁兰多糖微球,这种制备方法简单,多种因素控制微球形态与大小。

Objective To prepare microparticles ofpullulan by cross linking with water-in-oil emulsion and observe the effect of different factors on morphosis and size of microparticles. Methods A W/O emulsion system was adopted,in this system application of span-20 as a surfactant, castor oil or n-hexane as the oil phase and aqueous solutions of pullulan as the aqueous phase. By adding glytaraldehyde solution into the emulsion system, the pullulan polymer was solidified and the microparticles formed from the emulsion system. Scan electron microscope （SEM） image showed the morphosis of microparticles and the size distribution of pullulan microparticles were measured by Mastevsizer S. Resolts The pullulan microparticles formation and their size were influenced by the constituents of oil,the W/O ratio,pullulan and glytaraldehyde concentration in emulsion and stirring speed. The formulation conditions of caster oil were as follows：W/O ratio 〈 1 ： 5,1% aqueous solutions of pullulan,5 % ～ 50 % glymraldehyde. The microparlicles had a smooth sudace with narrow size distribution. The formulation conditions of n-hexane were： 1 ： 5 〈 W/O ratio 〈 1 ： 2,1% aqueous solutions of pullulan, glytaraldehyde 〈 25 %. The microparticles had a smooth surface and the particles were less monodispersed. However, in case of pullulan concentration （0.2 % or 5 %） and lower stirring speed （200 r/ min）,microparticles would not form. Conclusion Pullulan microparticles as a drug delivery vehicle were prepared by a W/O emulsion crosslink technique. The preparation method is simple and there are many factors influencing the morphosis of particles.