冻干保护剂对HB有效组分脂质体包封率和粒径的影响论文.docVIP

　　冻干保护剂对HB有效组分脂质体包封率和粒径的影响论文 刘娟 胡水根卞俊 汪国华 柯乾坤 【摘要】 目的研究不同冻干保护剂种类和浓度对HB有效组分脂质体冻干前后包封率和平均粒径的影响。方法按16个处方制备了HB有效组分脂质体，采用荧光分光光度法测定包封率，用显微镜和数码图象分析软件测定了平均粒径，通过冻干前后脂质体包封率和粒径的比较优选出最佳的冻干保护剂。结果最佳冻干保护剂为甘露醇和二元保护剂蔗糖-甘氨酸，包封率达到69.91%和66.70%，外观效果良好，比例分别为，甘露醇∶PC∶CH∶HB = 4∶1∶0.5∶0.2；蔗糖∶甘氨酸∶PC∶CH∶HB = 4∶0.8∶1∶0.5∶0.2。结论 冻干保护剂可减少脂质体囊泡在冻干过程受到的破坏以及对脂质体包封率和粒径的影响。 【关键词】 脂质体 冻干保护剂 包封率 粒径 Abstract：ObjectiveTo study the effects of freeze-drying on the endcapsulation and vesicles size of HB liposome ulations of HB liposome ent efficiency ined by fluorospectrophotometry.The particle size of the preparation ined by microscope and digital imaging analysis softized lyoprotectent ent efficiency and particle size before and after freeze-drying.ResultsThe use of sucrose as a primary lyoprotectent and glycine as a supporting lyoprotectents and the use of mannitol provided the highest encapsulation rate and minimal change of HB liposomes.The results shoum formula e vesicles during freeze-drying and mininal the influences of encapsulation and particle size. Key e; Lyoprotectents; Entrapment efficiency； Particle size HB有效组分是从海洋湖沼类贝壳软体动物园背角无齿蚌anodonta mol·L-1氯化钠，0.2 mmol·L-1Na2HPO4·12H2O～0.2 mmol·L-1NaH2PO4·2H2O（81∶19），pH 7.4。 2 方法与结果 2.1 冻干保护剂的选择方案 实验处方设计PC∶CH∶HB=500 mg∶250 mg∶100 mg1 Suc∶PC∶CH∶HB =4∶1∶0.5∶0.22 Suc∶PC∶CH∶HB =2∶1∶0.5∶0.23 Gly∶PC∶CH∶HB = 4∶1∶0.5∶0.24 Gly∶PC∶CH∶HB = 2∶1∶0.5∶0.25 Man∶PC∶CH∶HB = 4∶1∶0.5∶0.26 Man∶PC∶CH∶HB = 2∶1∶0.5∶0.27 D-Sor∶PC∶CH∶HB = 4∶1∶0.5∶0.28 D-Sor∶PC∶CH∶HB = 2∶1∶0.5∶0.29 Tre∶PC∶CH∶HB=4∶1∶0.5∶0.210 Tre∶PC∶CH∶HB=2∶1∶0.5∶0.211 Suc∶Gly∶PC∶CH∶HB = 4∶0.8∶1∶0.5∶0.212 Suc∶Man∶PC∶CH∶HB = 4∶0.8∶1∶0.5∶0.213 Suc∶D-Sor∶PC∶CH∶HB = 4∶0.8∶1∶0.5∶0.214 Suc∶Tre∶PC∶CH∶HB = 4∶0.8∶1∶0.5∶0.215 Suc∶PVP∶PC∶CH∶HB = 4∶0.8∶1∶0.5∶0.216 PC∶CH∶HB = 1∶0.5∶0.2 2.2 HB有效组分脂质体的制备采用逆相蒸发法制备，取处方量的PC和CH溶于乙醚10 ml；另取HB、冻干保护剂、荧光素1ml（8 μg/ml） 溶于5 ml生理盐水中，将两溶液混合于茄形瓶中，探针超声30 s（每超声15 s，间歇4 s）；40℃下减压旋转蒸发除去乙醚，至成黏稠溶液后再加入5 ml生理盐水，探针超声60 s（每超声15s，间歇4s）；继续常压旋转蒸发1 h, 得HB有效组分脂质体混悬乳浊液。 2.3 冷冻干燥工艺取各处方脂质体混悬液1 ml，各3