超滤离心法测定柚皮素非离子表面活性剂囊泡的包封率

Determination of entrapment efficiency of nonionic surfactant vesicles of naringin by ultrafiltration centrifugation

目的为解决柚皮素溶解度低、不易定量测定的问题,建立一种测定柚皮素非离子表面活性剂囊泡(naringenin niosomes,Nar-Nio)包封率的方法。方法采用超滤离心法分离Nar-Nio和游离柚皮素(naringenin,Nar),并通过高效液相色谱仪测定包载Nar和游离Nar含量,计算包封率。通过单因素实验进行Nar-Nio处方优化,使用该法平行测定3批Nar-Nio的包封率和载药量。结果柚皮素在0.5~100μg/ml范围内峰面积与浓度呈良好线性关系(R^(2)=0.9999)。日内及日间精密度RSD均小于2%。超滤膜吸附率、加样处理回收率以及超滤加样回收率在98%~102%之间。Nar-Nio的最佳处方和工艺为柚皮素3 mg,Span-60质量24 mg,胆固醇16 mg,水化介质体积15 ml,水化温度60℃,搅拌速度800 r/min,搅拌时间60 min。使用该法平行测定3批Nar-Nio,平均包封率和载药量分别为81.23%和1.88%。结论超滤离心法重复性好、准确度高、操作方便,能够较好分离游离药物,可用于Nar-Nio包封率的测定。

Objective To establish a method of determining the encapsulation rate of naringenin niosomes(Nar-Nio),and solve the problem of low solubility and difficult quantitation.Methods Nar-Nio and free naringenin(Nar)were isolated by ultrafiltration centrifugation,and the contents of encapsulated Nar and free Nar were determined by high performance liquid chromatography to calculate the encapsulation rate.Nar-Nio prescription was optimized through single-factor experiment,and verifred by parallel determination of the encapsulation rate and the drug loading capacity in three batches of Nar-Nio.Results Naringenin.showed a good linear relationship between peak area and concentration in the range of 0.5-100μg/ml(R^(2)=0.9999).The RSDs of both intra-day and inter-day precision were less than 2%.The ultrafiltration membrane adsorption rate,the recovery rate of spiked samples and the recovery rate of spiked samples in ultrafiltration were 98%-102%.The optimal prescription and process for Nar-Nio were as follows:3 mg naringenin,24 mg Span-60,16 mg cholesterol,a hydration medium volume of 15 ml,a hydration temperature of 60℃,a stirring speed of 800 r/min,and a stirring time of 60 min.The mean encapsulation rate and the drug loading capacity was 81.23%and 1.88%in three parallel batches of Nar-Nio by the established method,respectively.Conclusion Ultrafiltration centrifugation method has the advantages of good repeatability,high accuracy and easy operation,and can better isolate free drugs,which can be used for determining the encapsulation rate of Nar-Nio.