2种骨架材料制备盐酸小檗碱囊泡的比较

Comparison of Two Kinds of Berberine Hydrochloride Niosomes Prepared by Different Matrix Materials

关键词:  盐酸小檗碱  β-谷甾醇  胆固醇  囊泡  包封率  体外释放  稳定性

Key words:  berberine hydrochloride  β-sitosterol  cholesterol  niosomes  encapsulating rate  release profile in vitro  stability

摘要:

目的 比较胆固醇和β-谷甾醇作为囊材制备的盐酸小檗碱囊泡的特性和体外释药差异。方法 采用薄膜蒸发法用2种囊材分别制备盐酸小檗碱囊泡，光学显微镜观察比较囊泡形态，微粒分析仪评价囊泡粒径分布差异；采用HPLC测定盐酸小檗碱囊泡包封率和载药量，比较2种囊泡的体外释放情况，并考察温度对囊泡稳定性的影响。结果 镜下观察2种囊材制备的囊泡圆整度均较好，粒径分布范围比较相似；用胆固醇和β-谷甾醇制备的囊泡包封率分别为28.5%和25.21%，载药量分别为1.32%和1.26%；体外释放试验中，在人工肠液和人工胃液中的胆固醇囊泡12 h累积释放百分率在50%左右，而β-谷甾醇囊泡的累积释放百分率>70%；40℃以下放置8 h，温度对2种小檗碱囊泡的包封率影响较小，当温度高于40℃时，2种小檗碱囊泡的包封率均显著降低。结论 用薄膜分散法制备的2种小檗碱囊泡镜下形态相似，包封率近似；用β-谷甾醇制备的囊泡释药快，释药量多；40℃以下放置稳定性均较好。β-谷甾醇作为载体材料制备囊泡具有可行性。

Abstract:

OBJECTIVE To prepare the berberine hydrochloride-loaded niosomes with cholesterol or β-sitosterol separately, and compare their particle size, characteristics under the optical microscope, encapsulating rate, release profile in vitro and the stability of two kinds of niosomes.METHODS Thin-film evaporation method was applied to prepare the niosomes. Optical microscope was used to observe the morphology of the niosomes, and the particle diameter was observed and computed by Motic Images Advanced 3.2 system. HPLC was used to determine the encapsulating rate and loading capacity of the niosomes. The releasing profiles in vitro of the niosomes were observed and compared with each other, and the effect of temperature on the stability of the niosomes was invesgated.RESULTS The two kinds of niosomes both showed good sphericity, their particle diameter appenred to be similar. The encapsulating rate of cholesterol and β-sitosterol niosomes determined by HPLC was 28.5% and 25.21%, and the loading capacity of niosomes was 1.32% and 1.26%, respectively. The releasing study in vitro showed that the cholesterol niosomes reached an accumulative releasing rate about 50% at 12 h, while the accumulative releasing rate of β-sitosterol niosomes was higher than 70% in the artificial intestinal juice and in the artificial gastric juice. The encapsulating rate was not affected significantly by the temperature when the niosomes were storage under 8 h and the temperature was lower than 40℃. When the temperature was higher than 40℃, the encapsulating rate decreased significantly in both niosomes.CONCLUSION The two kinds of niosomes prepared by thin-film evaporation method have a similar appearance and a high encapsulating rate. The stability is good when the temperature is lower than 40℃. Compared with the cholesterol niosomes, the rate and the amount of drug release from β-sitosterol niosomes are better. The β-sitosterol can be used to prepare berberine hydrochloride niosomes.