骨碎补总黄酮/聚乳酸-羟基乙酸微囊的制备

背景：微囊是目前靶向治疗给药体系的主要方向之一，其大小为数微米到数百微米，可用于口服、注射、动脉给药及局部靶器官治疗等多种治疗途径。目的：制备骨碎补总黄酮/聚乳酸-羟基乙酸共聚物微囊，并对微囊制备条件进行优化。方法：采用乳化溶剂挥发法制备骨碎补总黄酮/聚乳酸-羟基乙酸共聚物微囊，单因素分析聚乳酸-羟基乙酸共聚物质量浓度(60，100，140，180 g/L)、搅拌速度(50，1 000，2 000，4 000 r/min)、初乳乳化时间(2，4，6，8 min)及水油比(1∶5、1∶10、1∶15、1∶20)对微囊大体形态、粒径分布宽度与微囊中总黄酮包封率的影响，筛选出微囊粒径较小、分散均匀、包封率较高的骨碎补总黄酮/聚乳酸-羟基乙酸共聚物微囊。结果与结论：确定最佳工艺参数为：140 g/L 聚乳酸-羟基乙酸共聚物溶液，匀浆机2 000 r/min搅拌速度，初乳乳化时间6 min，水油比为1∶15。优化工艺下所制备的微囊分布均匀，平均粒径为(789.8±712.3) nm，粒径分布宽度较窄，基本小于5 μm；扫描电镜下观察所见微囊呈圆形，边缘较规则；微囊平均包封率为47.72%。 中国组织工程研究杂志出版内容重点：人工关节；骨植入物；脊柱；骨折；内固定；数字化骨科；组织工程

The preparation of rhizoma drynariae total flavonoids/polylactic-co-glycolic acid microcapsules

BACKGROUND: Microcapsules is one of the main directions of targeted therapeutic dosing system. With a size of several microns to several hundred microns, it can be used for injection, oral, arterial administration and local treatment of targeted organs and other treatment approaches.OBJECTIVE: To prepare rhizoma drynariae total flavonoids/polylactic-co-glycolic acid microcapsules and optimize the preparation conditions.METHODS: The rhizoma drynariae total flavonoids/polylactic-co-glycolic acid microcapsules was prepared by ultrasonic emulsification. The effect of the mass concentration (60, 100, 140, 180 g/L), stirring speed (50, 1 000,  2 000, 4 000 r/minutes), colostrum emulsification time (2, 4, 6, 8 minutes), colostrum water oil ratio (1:5, 1:10, 1:15, 1:20) of rhizoma drynariae total flavonoids/polylactic-co-glycolic acid microcapsules on gross morphology, particle size distribution width and total flavonoids encapsulation efficiency of microcapsules was univariately analyzed. The rhizoma drynariae total flavonoids/polylactic-co-glycolic acid microcapsules with smaller particle size, uniform dispersion and higher encapsulation efficiency was filtered out. RESULTS AND CONCLUSION: The optimum process parameters were as follows: 140 g/L polylactic acid-glycolic acid solution, the stirring speed of 2 000 r/min, the colostrum emulsification time of 6 minutes, and the colostrum water-oil ratio of 1:15. The microcapsules prepared in the optimized process displayed a uniform distribution and its average particle size was (789.8±712.3) nm, which distributed relative narrowly and basically less than 5 μm. Microcapsules presented round, with a regular edge under scanning electron microscope. The average encapsulation efficiency was 47.72%.