大黄酚聚氰基丙烯酸丁酯纳米囊的制备工艺及质量研究

目的 采用界面聚合法制备大黄酚聚氰基丙烯酸丁酯纳米囊,筛选其最佳制备工艺,并进行质量考察.方法 在单因素法筛选制备工艺的基础上.以包封率为指标,采用L_s(3~4)正交设计法对处方中搅拌速度、水相pH值、α-氰基丙烯酸丁酯用量和醋酸乙酯用量进行筛选,以优化该制备工艺.对其进行包封率、载药量、粒径和粒度分布等的质量考察.结果 确定大黄酚投药量为5 mg时,最佳制备工艺:搅拌速度为800 r/min,水相pH值为2,α-氰基丙烯酸丁酯用量为13 μL,醋酸乙酯用量为0.6 mL.采用最佳工艺制备的大黄酚纳米囊平均包封率为82.19%,平均载药量为21.48%,平均粒径为246 nm,电镜照片显示粒度分布均匀.结论 采用界面聚合法制备的聚氰基丙烯酸丁酯大黄酚纳米囊粒径小,包封率和载药量高,粒度分布均匀,制备工艺稳定可行,可用于静脉注射给药.

Preparation of chrysophanol loaded polybutylcyanoacrylate nanocapsules and its quality inspection

Objective To optimize the preparation technology of chrysophanol loaded polybutylcyanoacrylate nanocapsules by interfacial polymerization, sieve the optimal technology conditions of preparation, and study its quality. Methods Based on the single factor experiment, the formulation was optimized by L+9(3~4) orthogonal design with entrapment efficiency as reference index. The factors including agitating speed, pH value of aqueous phase, amount of crbutylcyanoacrylate (BCA) and of ethyl acetate were screened. At last, its shape, particle size, the encapsulation efficiency, and the drug loading were investigated as its quality inspection. Results When the ammunt of chrysophanol was 5 mg, the optimum preparation conditions were established as follows: the agitating speed was 800 r/min, the pH value of aqueous phase was 2, the amount of α-BCA was 13 μL and ethyl acetate was 0. 6 mL. Under this optimum condition, the mean entrapment ratio was 82. 19% , and the mean drug loading was 21. 48%, the mean diameter of the nanocapsule was 246 nm. The particle size was well-distributed showed by electron microscope pictures. Conclusion The prepared chrysophanol loaded polybutylcy-anoacrylate nanocapsules has small size, high encapsulation efficiency, and drug loading. The preparation technique established in this study is stable and feasible. It also can be used for iv injection.