[关键词]
[摘要]
目的 建立镶囊包封率的测定方法,以包封率为指标,对积雪草苷脂质体镶囊的处方和工艺进行考察。方法 建立HPLC法测定积雪草苷,用薄膜分散法制备脂质体,采用层层自组装法制备镶囊。采用低速离心法测定积雪草苷镶囊的包封率,并对方法进行验证。通过单因素实验,考察一系列处方及制备工艺对镶囊包封率的影响,选择影响较大的3个因素进一步采用星点设计-效应面法优化处方工艺。结果 低速离心法测定镶囊包封率准确、可靠。通过单因素实验,确定十八胺用量为磷脂量的4%,海藻酸钠(ALG)和壳聚糖(CS)溶液的质量浓度为1 mg/mL,脂质体混悬液的pH值为7.9,前体层为2层,包埋层为1层。星点设计-效应面法优化得到的最优处方为ALG和CS溶液pH值7.00,反应转速450 r/min,反应时间0.30 h,通过拟合方程计算得到的最优处方的包封率为81.21%。激光共聚焦显微镜显示脂质体成功地包埋在聚电解质微囊的囊壁中。结论 所得积雪草苷镶囊的包封率较高,粒径均匀,激光共聚焦显微镜下形态良好。
[Key word]
[Abstract]
Objective To fabricate the asiaticoside loaded capsosomes with CaCO3 as core (CASI) and establish the method for determination of entrapment efficiency, then the prescription of formulation and preparation process were screened with the entrapment efficiency as index.Methods An HPLC method was established to determine the contents of asiaticoside. CASI were prepared by co-precipitation method and layer-by-layer assembly technique. The encapsulation efficiency was determined by a proved centrifugation. In this study, the effect of concentrations of capsule material, pH and rotating speed on encapsulation efficiency was investigated.Results The encapsulation efficiency obtained by centrifugation was accurate and reliable. The optimized prescription was concentrations of 1 mg/mL capsule material with pH value 12, pH 7.9 of liposomes, two precursor layers, one liposome layer, rotating speed 500 r/min, and 15 min of reaction time. The CLSM images confirmed the structural integrity of the CASI.Conclusion This formulation endowed with high encapsulation efficiency, and the CASI observed by CLSM turned out to be globular shapes and was narrow in size distribution.
[中图分类号]
[基金项目]
武警后勤学院基础研究项目(WHJ2015012,WHJ201501)