目的 为提高芍药苷的稳定性和口服生物利用度,制备了实心和中空玉米醇溶蛋白-芍药苷纳米粒,并比较其性质和体外释药特性。方法 采用相分离法制备了实心和中空玉米醇溶蛋白-芍药苷纳米粒,以包封率为指标,采用正交设计优化处方并进行表征,考察体外释放度。结果 实心玉米醇溶蛋白-芍药苷纳米粒的最优处方为:芍药苷质量为10 mg,玉米醇溶蛋白质量浓度为10 mg·mL-1,搅拌时间为2 h;包封率为53.87%,载药量为26.94%,平均粒径110 nm左右。中空玉米醇溶蛋白-芍药苷纳米粒的最优处方为:芍药苷质量为20 mg,玉米醇溶蛋白质量浓度为5 mg·mL-1,搅拌时间为1 h;包封率为55.65%,载药量为44.52%,平均粒径50 nm左右。体外释放表明,2种制剂均具有缓释作用。结论 采用相分离法成功制备了实心和中空玉米醇溶蛋白-芍药苷纳米粒,方法简单可靠。和实心纳米粒相比较,中空纳米粒载药量和体外缓释效果均有明显提高。
Abstract
OBJECTIVE To improve the stability and oral bioavailability of paeoniflorin, develop solid and hollow zein-paeoniflorin nanoparticles, and compare their properties and in vitro release. METHODS The solid and hollow zein-paeoniflorin nanoparticles were fabricated by phase separation method, and the processing parameters were optimized according to the entrapment efficiency by orthogonal design. The morphology and mean size of nanoparticles were investigated and in vitro release was carried out using the optimal prescription. RESULTS The mass of paeoniflorin, the concentration of zein and the stirring time in optimal prescription of solid zein-paeoniflorin nanoparticles were 10 mg, 10 mg·mL-1 and 2 h, respectively. These three factors in optimal prescription of hollow zein-paeoniflorin nanoparticles were 20 mg, 5 mg·mL-1 and 1 h, respectively. The obtained nanoparticles of solid and hollow zein-paeoniflorin nanoparticles were spherical with a mean particle size of 110 and 50 nm. And the drug load efficiency and entrapment efficiency of solid and hollow zein-paeoniflorin nanoparticles were 26.94%, 53.87%, 44.52% and 55.65%, respectively. In vitro release of both formulations indicated sustained release effect. CONCLUSION The solid and hollow zein-paeoniflorin nanoparticles are successfully prepared by phase separation method. The method is simple and reliable. Compared with solid nanoparticles, the drug load efficiency of hollow nanoparticles is greatly improved, and in vitro studies of hollow zein-paeoniflorin nanoparticles show much slower release.
关键词
芍药苷 /
中空玉米醇溶蛋白 /
实心 /
纳米粒 /
载药量 /
体外释放
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Key words
paeoniflorin /
zein hollow /
solid /
nanoparticle /
drug loading /
in vitro release
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中图分类号：
R944
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参考文献
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脚注
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基金
国家自然科学基金项目资助(51303006);安徽省重大科研项目资助(KJ2018ZD031);安徽省自然科学基金项目资助(1408085MH196)
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