目的制备载紫杉醇固体脂质纳米粒,并对其理化性质、体外释药特性及体外抗肿瘤活性进行初步研究。方法矩形微通道内制备载药纳米粒,正交实验筛选最优处方;动态光散射法测定其粒径;高效液相色谱法测定其载药量和包封率;透析法测定其体外释药特性;四甲基偶氮唑蓝(MTT)法测定其体外抗肿瘤活性。结果最优处方制备的纳米粒为规整球形,无明显团聚现象,平均粒径为(129.73±2.41)nm,载药量和包封率分别为(3.11±1.90)%和(43.67±0.55)%;体外释放药物分为突释和持续释放两个阶段,120 h累计释药率为87.3%;体外抗肿瘤活性明显高于紫杉醇原药。结论微通道法制备紫杉醇纳米粒简便可行,制剂质量符合要求,该方法在药学领域应用前景广阔。 OBJECTIVE: To prepare paclitaxel-loaded solid lipid nanoparticles, and to study its physical and chemical properties, drug release in vitro and anti-tumor activity in vitro. Methods The drug-loaded nanoparticles were prepared in rectangular microchannels, and the optimal prescription was screened by orthogonal experiment. The particle size was determined by dynamic light scattering method. The drug loading and entrapment efficiency were determined by HPLC. The anti-tumor activity was measured by MTT assay. Results The nanoparticles prepared by the optimal prescription were regular spherical with no agglomeration. The mean particle size was (129.73 ± 2.41) nm, the drug loading and entrapment efficiency were (3.11 ± 1.90)% and (43.67 ± 0.55)%, respectively ; Drug release in vitro was divided into two stages of burst release and sustained release. The cumulative release rate at 120 h was 87.3%. The anti-tumor activity in vitro was significantly higher than that of paclitaxel. Conclusion The microchannel method for the preparation of paclitaxel nanoparticles is simple and feasible, and the preparation quality meets the requirements. The method has broad application prospect in the field of pharmacy.