羟基喜树碱壳聚糖纳米冻干粉的制备及表征

为研究制备载羟基喜树碱的叶酸-壳聚糖纳米冻干粉的制备方法，以羟基喜树碱、叶酸、壳聚糖、三聚磷酸钠为原料，以葡萄糖和甘露醇为保护剂，应用真空冷冻干燥技术，制备了载羟基喜树碱的叶酸-壳聚糖纳米粒冻干粉。以冻干粉外观及在水中再分散性为指标，分别考察了冻干保护剂的种类、体积分数、用量及加入方式对冻干的影响。并利用扫描电镜及透射电镜对冻干粉的微观形态进行观察。结果表明，甘露醇作为冻干保护剂优于葡萄糖。当甘露醇体积分数为8％，与纳米粒水分散体系体积比为1∶1时，所制备的冻干粉呈颜色均一、外表光滑、致密松脆的完整的饼状，且在水中再分散迅速，无任何悬浮物，成均一乳状胶体。在扫描电镜下观察冻干粉呈花瓣形，再分散后于透射电镜下观察，纳米粒子呈规则球形，大小均匀，平均粒径约200 nm左右。该工艺所制备得冻干粉针剂有望成为羟基喜树碱的新剂型。

Preparation and characterization of lyophilized powder of hydroxycamptothecin chitosan nanoparticles

To research the preparation method of lyophilized powder of hydroxycamptothecin using hydroxycamptothecin , folic acid, chitosan and sodium tripolyphosphate as raw materi-als, glucose and mannitol as cryoprotectants , the nanoparticles lyophilized powder was pre-pared with the method of vacuum freeze drying technology .With the appearance and redis-persibility in water of lyophilized powder as examining index , the factors were respectively investigated , including the types , concentration , amount and adding method of the cryopro-tectants .The morphology of the lyophilized powder was observed by scanning electron micro-scope （SEM） and transmitting electron microscope （ TEM） respectively.Results indicated that as cryoprotectant mannitol was better than glucose .When mannitol concentration was 8%, and the volume ratio of nanoparticles water dispersion system to mannitol solution was 1∶1, the lyophilized powder was the whole pie with uniformly yellow , smooth, compact crunchy .Furthermore , it dispersed quickly into a homogeneous emulsion colloid without any suspended substance in distilled water .The morphology of lyophilized powder was regularly＆amp;nbsp;spherical and uniform with the average grain diameter of 200 nm under TEM , and appeared petaling under the SEM .The lyophilized powder injection prepared by the process is expec-ted to become a new pharmaceutical dosage form of hydroxycamptothecin .