载马钱子碱纳米粒的微球系统的制备与初步评价
Preliminary Evaluation and Preparation of Brucine Nanoparticles-in-microsphere System
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摘要: 目的 制备包载马钱子碱纳米粒的壳聚糖微球系统（Brucine nanoparticles-in-microsphere system，Brucine-NiMS），以期获得一种降低突释作用用于关节腔注射的长效制剂。方法 以牛血清白蛋白（BSA）为材料，采用去溶剂化法制备载马钱子碱的纳米粒（Brucine nanoparticles， Brucine-Nps）。再以壳聚糖(CS)为载体，利用喷雾干燥法将纳米粒包载于壳聚糖微球系统中。在电镜下观察Brucine-NiMS的外观，并测定其体外释放特性。结果 Brucine-NiMS的处方为：CS的型号为600 kDa，CS醋酸溶液的浓度为1%，BSA与CS的比例为1∶5。喷雾干燥的条件为：蠕动泵速度为20%，进口温度为120 ℃，Q-Flow为40 mL/h。在此条件下制备的Brucine-NiMS的包封率、载药量和粒径分别为97.35%、3.17%和1.48 μm。Brucine-NiMS外观圆整，性质稳定。结论 Brucine-NiMS制备方法稳定可控，为开发药物新剂型提供了新的思路。Abstract: OBJECTIVE To find a long-acting preparation which can reduce the burst effect in intra-articular injection by preparing the brucine nanoparticles-in-microsphere system (Brucine-NiMS).METHODS Brucine nanoparticles (Brucine-Nps) were prepared by desolvation of BSA. Chitosan was used as an carrier and the nanoparticles were contained in the microsphere system by the spray drying method. The appearances of Brucine-NiMS were observed under the electron microscope and then the in vitro release characteristics were determined.RESULTS The formulation of Brucine-NiMS was as follows: BSA/CS (600KDA) 1∶5 (w/w) and the concentration of CS in the acetic acid was 1%. The spry drying conditions were as follows: The speed of the peristaltic pump was adjusted to 20%， the temperature of inlet was 120 ℃， and Q-Flow was 40 mL/h. The envelop rate， drug loading and particle sizes of Brucine-NiMS were 97.35%， 3.17% and 1.48 μm respectively. The appearance of Brucine-NiMS was rounding and the nature was stable.CONCLUSION The preparation method of Brucine-NiMS is stable and controllable， providing a new way to develop new dosage forms of drugs.
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