制备工艺和包封材料对3种成分脂质体包封率的影响  

Effects of preparation technologies and entrapment materials on encapsulation efficiencies of three constituents' liposomes

作　　者：王理想[1,2] 瞿鼎[1,2] 刘聪燕[1,2] 刘明健[1,2] 范晨怡[1,2] 陈彦[1,2] 

机构地区：[1]南京中医药大学附属中西医结合医院,江苏南京210023 [2]江苏省中医药研究院,江苏南京210028

出　　处：《中成药》2017年第1期60-64,共5页Chinese Traditional Patent Medicine

基　　金：国家自然科学青年基金(81503264);江苏省自然科学基金(BK20151038);中国中医科学院肿瘤专项(ZZ08080015)

摘　　要：目的制备雷公藤红素、丹参酮ⅡA、丹参酮ⅡA磺酸钠脂质体,并评价制备工艺和包封材料对其包封率的影响。方法分别以薄膜分散法和逆向蒸发法制备3种成分脂质体,以50%大豆卵磷脂、80%蛋黄卵磷脂、92%大豆卵磷脂和复合磷脂(二棕榈酰磷脂酰胆碱与50%大豆卵磷脂比例5∶1)为包封材料,测定所得脂质体的平均粒径和多分散系数,再计算其包封率。结果雷公藤红素和丹参酮ⅡA磺酸钠脂质体采用逆向蒸发法制备时的包封率均高于薄膜分散法,而且雷公藤红素高于丹参酮ⅡA磺酸钠,并分别以80%蛋黄卵磷脂和92%大豆卵磷脂包封时最高。丹参酮ⅡA脂质体采用薄膜分散法制备,并以50%大豆卵磷脂包封时的包封率最高,但远低于其他2种脂质体。结论含有多氢键的脂溶性雷公藤红素和不含氢键的水溶性丹参酮ⅡA磺酸钠适合逆向蒸发法制备其脂质体,而无氢键的脂溶性丹参酮ⅡA适合薄膜分散法。AIM To prepare the liposomes loaded with celastrol,tanshinone ⅡA and tanshinone ⅡA sodium sulfonate and to evaluate the effects of preparation technologies and entrapment materials on the encapsulation efficiencies. METHODS The liposomes for three constituents were prepared by film dispersion method and reverse phase evaporation method,respectively. 50% Lecithin high potency,80% egg yolk lecithin,92% lecithin high potency and complex phospholipid（ 5 ∶ 1 for ratio of dipalmitoyl phosphatidylcholine to 50% lecithin high potency）were served as entrapment materials. The encapsulation efficiencies were thus calculated based on the measured mean sizes and polydispersity of the liposomes. RESULTS Celastrol and tanshinone ⅡA sodium sulfonate liposomes accomplished by reverse phase evaporation method got the highest encapsulation efficiency when entrapped with 80% egg yolk lecithin and 92% lecithin high potency,respectively,which were higher than those prepared by film dispersion method. And celastrol liposomes exhibited an even superior performance than tanshinone ⅡA sodium sulfonate liposomes. Tanshinone Ⅱ A lipisome prepared by film dispersion method and then entrapped with50% lecithin high potency obtained its the highest value of encapsulation efficiency,which was much lower than those of another two liposomes. CONCLUSION Reverse phase evaporation method is appropriate for hydrophobic celastrol with multiple hydrogen bonds and hydrophilic sodium tanshinone ⅡA without hydrogen bonds to prepare their liposomes,while film dispersion method is applicable to hydrophobic tanshinone ⅡA without hydrogen bonds.

关 键 词：雷公藤红素 丹参酮ⅡA 丹参酮ⅡA磺酸钠 脂质体 包封率 制备工艺 包封材料 

分 类 号：R943[医药卫生—药剂学]