微通道法制备载紫杉醇聚乳酸羟基乙酸固体脂质纳米粒

发布时间：2019-03-07 19:33

【摘要】：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。
[Abstract]:Aim to prepare paclitaxel-loaded solid lipid nanoparticles and to study their physicochemical properties in vitro release characteristics and antitumor activity in vitro. Methods the drug-loaded nanoparticles were prepared in rectangular microchannel, the optimal prescription was screened by orthogonal experiment, the particle size was measured by dynamic light scattering, the drug loading and entrapment efficiency were measured by high performance liquid chromatography (HPLC), the drug release characteristics in vitro were determined by dialysis. The antineoplastic activity in vitro was determined by (MTT) method with tetramethylazo blue. Results the nanoparticles prepared by the optimal prescription were regular spherical and had no obvious agglomeration. The average particle size was (129.73 卤2.41) nm, and entrapment efficiency was (3.11 卤1.90)% and (43.67 卤0.55)%, respectively, and the drug loading and entrapment efficiency of the nanoparticles were (129.73 卤2.41)% and (43.67 卤0.55)%, respectively. Drug release in vitro was divided into two stages: sudden release and sustained release, the cumulative release rate was 87.3% at 120 h, and the antitumor activity in vitro was significantly higher than that of paclitaxel. Conclusion the preparation of paclitaxel nanoparticles by microchannel method is simple and feasible, and the quality of the preparation meets the requirements. This method has a wide application prospect in pharmaceutical field.
【作者单位】：台州市立医院;浙江工业大学药学院;
【基金】：国家自然科学基金资助项目(21376223)
【分类号】：R944

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