羟基乙酸乙基纤维素微球的研制

Preparation of glycolic acid ethyl cellulose microspheres

目的研究用于肝动脉栓塞治疗的羟基乙酸乙基纤维素微球的制备方法及其体外释药特征。方法选用乙基纤维素为载体,加入羟基乙酸,采用复乳法制备羟基乙酸乙基纤维素微球,以外观、粒径、载药量、包封率为考察指标,从微球的圆整度、光滑度、大小均匀度、含药量对微球综合评价,并采用恒温振荡透析法测定微球的体外药物释放特性。结果和结论羟基乙酸乙基纤维素微球外观光滑,球形圆整,平均粒径(233.38±1.62)μm,载药量114.32μg/mg,包封率78.61%,微球体外可释放药物72 h。羟基乙酸乙基纤维素微球可满足进一步动物实验要求,为化学腐蚀性药物用于肝动脉栓塞的研究提供重要的参考依据。

Objective To prepare glycolic acid ethyl cellulose microspheres（GAECM） for hepatic artery embolization treatment and to investigate their in vitro release property.Methods GAECM was prepared using ethyl cellulose as a carrier,adding glycolic acid,by a double emulsion method.The appearance,particle size,drug loading,and encapsulation efficiency were used as indices to assess the roundness,smoothness,size uniformity,and drug contents of the microspheres.The in vitro release characteristics of the microspheres were determined by constant temperature oscillation dialysis.Results and conclusion The prepared GAECM has a smooth round appearance,with a mean diameter of（233.38±1.62） μm,a mean drug loading of 114.32 μg/mg,an encapsulation efficiency of 78.61%,and a release period of 72 h.The microspheres can meet the requirements of further animal experiments,which provides important reference for using chemical corrosion in drugs used for hepatic arterial embolization studies.