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目的采用聚丙交酯乙交酯共聚物(PLGA)载体制备紫杉醇(TAX)纳米粒,并进行体外评价。方法采用改良的溶剂扩散法制备TAX-PLGA共聚物纳米粒,考察不同乳化剂类型和各工艺因素对纳米粒粒径的影响,通过动态激光粒度分析仪、透射电子显微镜(TEM)、扫描电子显微镜(SEM)、差示扫描量热法(DSC)及X线粉末衍射(XRD)初步研究其载药性质,并研究纳米粒冻干粉的体外释放特性。结果优选出制备工艺为:双十二烷基二甲基溴化铵(DMAB)作为乳化剂,浓度为1%(W/V),聚合物浓度为1%(W/V),水相与有机相的体积比例为20:10,均质机转速为16000r.min-1,药物浓度为0.1%(W/V)。所得纳米粒外观圆整,平均粒径为99.0nm,Zeta电位58.3mV,包封率为56.77%,载药量率为7.10%。TAX纳米粒具有缓释性,体外释放分为两相。DSC及XRD表明TAX被有效地包裹在纳米粒中。结论 PLGA纳米粒可成为TAX的新型载体。
OBJECTIVE To prepare paclitaxel (TAX) nanoparticles by poly (lactide-co-glycolide) (PLGA) carrier and evaluate in vitro. Methods TAX-PLGA copolymer nanoparticles were prepared by modified solvent diffusion method. The influences of different emulsifier types and technological factors on the particle size of nanoparticles were investigated. The effects of different emulsifiers on the particle size were investigated by dynamic laser particle size analyzer, transmission electron microscopy (TEM), scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray powder diffraction (XRD) were used to study the drug-loading properties and to study the in vitro release characteristics of lyophilized nanoparticles. The results showed that the preparation process was as follows: DMAB was used as the emulsifier, the concentration was 1% (W / V), the concentration of the polymer was 1% (W / V) The volume ratio of the organic phase was 20:10, the speed of the homogenizer was 16000 r.min-1, and the drug concentration was 0.1% (W / V). The obtained nanoparticles had a round appearance, an average particle diameter of 99.0 nm, a zeta potential of 58.3 mV, an entrapment efficiency of 56.77% and a drug loading rate of 7.10%. TAX nanoparticles with sustained release, in vitro release is divided into two phases. DSC and XRD showed that TAX was effectively encapsulated in the nanoparticles. Conclusion PLGA nanoparticles can be a new carrier of TAX.