Influence of type and proportion of lyoprotectants on lyophilized ginsenoside Rg3 liposomes
Influence of type and proportion of lyoprotectants on lyophilized ginsenoside Rg3 liposomes
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DOI：
10.1111/jphp.12489
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发表时间：
2016-01-01
影响因子：
3.3
通讯作者：
Zhang, Di
中科院分区：
文献类型：
--
作者：
Li, Jianying;Hu, Meina;Zhang, Di
为了提高稳定性和保质期，制备了20(R)-人参皂苷Rg3脂质体(G-Rg3-LS)的冻干制剂。方法以葡萄糖、海藻糖、蔗糖、麦芽糖、乳糖、甘露醇、肌醇、羟丙基-环糊精和聚乙二醇为单一保护剂，比较它们对冻干G-Rg3-LS的保护作用。此外，还利用葡萄糖-甘露醇复合体确定了最佳冻干制剂。采用扫描电子显微镜、热重-差热分析、X射线衍射仪和傅立叶变换红外光谱仪对冻干脂质体或冻干保护剂的分析进行了进一步的研究。结果：当葡萄糖-甘露醇与磷脂的质量比为4：2：1(w/w)时，冻干的G-Rg3-LS外观良好，DRR高(86.52%，5.02%)，粒径变化小(45.83+/-0.50%)，复水重建时间短(8.3+/-1.5s)。各项指标均明显优于单一保护剂。结果表明，两种冻融保护剂复配时，能较好地保持葡萄糖的稳定作用和甘露醇的成型作用。新鲜制备的G-Rg3脂质体和冻干G-Rg3脂质体的细胞抑制实验表明，冷冻干燥不影响G-Rg3的生物活性。结论应用葡萄糖-甘露醇复合冻干剂可获得良好的G-Rg3冻干制剂。
ObjectivesTo improve stability and shelf life, lyophilized formulations of 20(R)-Ginsenoside Rg3 liposomes (G-Rg3-Ls) were prepared.MethodsGlucose, trehalose, sucrose, maltose, lactose, mannitol, inositol, hydroxypropyl--cyclodextrin and polyethylene glycol were used as single lyoprotectant and then compared in terms of their ability to protect lyophilized G-Rg3-Ls. Further, a glucose-mannitol complex was used to determine the optimal lyophilized preparation. The analysis of lyophilized liposomes or lyoprotectant was further investigated by scanning electron microscopy, thermogravimetry-differential thermal analysis, X-ray diffractometry and Fourier transform infrared spectroscopy. Cytotoxicity assay was used to assess the cyto-inhibition of freshly prepared and lyophilized liposomes.Key findingsWhen the ratio of glucose-mannitol to phospholipids was 4:2:1 (w/w) the lyophilized G-Rg3-Ls exhibited good appearance, high DRR (86.52%5.02%), small change in particle size (45.83 +/- 0.50%) and short rehydration reconstruction time (8.3 +/- 1.5s). All indices were considerably better than those of each single protective agent. Results indicated that when the two lyoprotectants were combined, the stabilizing effect of glucose and shaping effect of mannitol were well maintained. The cyto-inhibition of freshly prepared and lyophilized G-Rg3 liposomes showed that lyophilization did not affect the bioactivity of G-Rg3.ConclusionsThe application of glucose-mannitol composite lyoprotectants can obtain a good G-Rg3 lyophilized preparation.