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目的:以海藻酸钠为主要材料制备紫杉醇的缓释微囊/微球,对其形态、粒径、体外释放以及抑瘤活性进行研究。方法:扫描电镜观察微球的形态和大小。HPLC法测定紫杉醇在释放介质中的浓度。MTT法测定体外抑瘤活性。结果:制备的紫杉醇/海藻酸钠微囊/微球的形态呈规则圆形,粒径相近,平均粒径256μm。冷冻干燥后呈不规则球形,颗粒长径约100μm,表面形成皱襞。微囊载药量为25%左右,而微球不足10%。微囊与微球均具有缓释作用,体外实验证明保持了抑瘤活性。结论:海藻酸钠紫杉醇微囊/微球具有缓释作用,可以维持较长时间的有效药物浓度,达到更好的抑瘤效果。
OBJECTIVE: To prepare paclitaxel sustained-release microcapsules / microspheres with sodium alginate as the main material and study its morphology, particle size, in vitro release and antitumor activity. Methods: Scanning electron microscopy was used to observe the shape and size of microspheres. Determination of paclitaxel in the release medium by HPLC method. MTT assay in vitro antitumor activity. Results: The morphology of paclitaxel / alginate microcapsules / microspheres was regular and round with similar particle size and the average particle diameter was 256μm. After freeze-drying irregular spherical, particle diameter of about 100μm, the surface of folds. Microcapsule drug loading of 25%, while the microspheres less than 10%. Microcapsules and microspheres have a sustained release effect, in vitro experiments show that maintain the anti-tumor activity. Conclusion: Sodium alginate paclitaxel microcapsules / microspheres have a sustained release effect, which can maintain effective drug concentration for a longer time and achieve better antitumor effect.