涂膜粉碎法制备原花青素缓释微粒的研究

Study on Preparation of Proanthocyanidin-loaded Sustained-release Microparticles by Casting Method

目的考察涂膜粉碎工艺对原花青素载药微粒形态和性能的影响。方法分别制备原花青素、乙基纤维素及载药微粒,观测微粒形成过程和形态粒径,比较其红外光谱图,并测定载药量、包封率和体外释放曲线。结果随着乙基纤维素含量的增加,所得载药微粒更均匀;在载药量10%~50%范围内其包封率均高于65%;载药高达48%的微粒仍显示缓释特征,释放机制为Fick扩散,但因粒径较小导致释放较原料稍快。结论涂膜粉碎法简单、高效、可控,适于制备载药微粒。

Objective To investigate the influence of casting technique on morphology and properties of proanthocyanidin-loaded ethyl cellulose microparticles.Methods The microparticles of pure drug,ethyl cellulose(EC)and their mixture were prepared via the casting method.The formation process and morphology of microparticles were observed by microscope and scanning electron microscope,respectively.The obtained samples were determined on their drug loading capacity,encapsulation efficiency and in vitro release profiles,and the interaction between drug and carrier was analyzed by Fourier transform infrared spectroscopy.Results The particle sizes were more uniform as EC content increased,and the entrapment efficiency was above 65%within the range of 10%-50%of drug loading.The microparticles with the highest loading capacity of 48%still showed a sustained-release pattern and a drug release mechanism of Fick diffusion,but their smaller size induced a slightly faster release than pure drug.Conclusion The casting method is a simple,efficient and controllable technique for the preparation of drug-loaded microparticles.