复乳化-溶剂挥发法制备树舌多糖长循环热敏脂质体的方法研究及质量表征
|
摘要
目的建立树舌多糖长循环热敏脂质体的优选制备方法。方法通过对比薄膜分散法、乳化法溶剂挥发法、复乳化-溶剂挥发法三种方法制备树舌多糖长循环热敏脂质体的粒径、Zeta电位、包封率和载药量,对包封率和载药量最佳者的稳定性、形态和热敏特性进行表征。结果三种制备方法中,以复乳化-溶剂挥发法制备的树舌多糖热敏长循环热敏脂质体包封率和载药量最高(82.4%和7.2%),且其在28 d内稳定性良好,37℃时基本不释放,42℃时30 min内累计释药量到达90%以上。结论确立了复乳化-溶剂挥发法制备树舌多糖长循环热敏脂质体的处方和工艺,所制备的脂质体粒径均一,具有良好的热敏特性,可为进一步递药系统研究提供依据。
Objective To establish an optimal preparation method of polysaccharide long-circulating thermosensitive liposomes from Ganoderma lucidum polysaccharides. Methods The particle size,Zeta potential,entrapment efficiency and drug loading of Ganoderma lucidum polysaccharides long-circulating thermosensitive liposomes were characterized,which was prepared by comparing film dispersion method,emulsification solvent evaporation method and double emulsification solvent evaporation method. The stability,morphology and thermal sensitivity of polysaccharide long-circulating thermosensitive of liposomes with the best encapsulation efficiency and drug loading were characterized.Results Among the three preparation methods,the highest entrapment efficiency and drug loading capacity of thermosensitive long-circulating thermosensitive liposomes were prepared by double emulsification solvent evaporation method(82.4% and 7.2%). The liposomes had good stability in 28 d,and basically did not release at 37℃. The cumulative drug release reached more than 90% at 42℃.Conclusion The formulation and process of preparation of polysaccharide long-circulating thermosensitive liposomes from Ganoderma lucidum polysaccharides by double emulsification Ganoderma lucidum solvent evaporation method are established.The prepared liposomes has homogeneous particle size and good thermosensitive properties,which could provide a basis for further drug delivery system research.
Objective To establish an optimal preparation method of polysaccharide long-circulating thermosensitive liposomes from Ganoderma lucidum polysaccharides. Methods The particle size,Zeta potential,entrapment efficiency and drug loading of Ganoderma lucidum polysaccharides long-circulating thermosensitive liposomes were characterized,which was prepared by comparing film dispersion method,emulsification solvent evaporation method and double emulsification solvent evaporation method. The stability,morphology and thermal sensitivity of polysaccharide long-circulating thermosensitive of liposomes with the best encapsulation efficiency and drug loading were characterized.Results Among the three preparation methods,the highest entrapment efficiency and drug loading capacity of thermosensitive long-circulating thermosensitive liposomes were prepared by double emulsification solvent evaporation method(82.4% and 7.2%). The liposomes had good stability in 28 d,and basically did not release at 37℃. The cumulative drug release reached more than 90% at 42℃.Conclusion The formulation and process of preparation of polysaccharide long-circulating thermosensitive liposomes from Ganoderma lucidum polysaccharides by double emulsification Ganoderma lucidum solvent evaporation method are established.The prepared liposomes has homogeneous particle size and good thermosensitive properties,which could provide a basis for further drug delivery system research.
引文
[1] Chien RC,Yen MT,Tseng YH,et al. Chemical characteristics and anti-proliferation activities of Ganoderma tsugae polysaccharides[J]. Carbohydr Polym,2015,128(1):90-98.
[2] Li A,Shuai X,Jia Z,et al. Ganoderma lucidum polysaccharide extract inhibits hepatocellular carcinoma growth by downregulating regulatory T cells accumulation and function by inducing microRNA-125b[J]. J Transl Med,2015,13(1):100.
[3] Pattni BS,Chupin VV,Torchilin VP. New developments in liposomal drug delivery[J]. Chem Rev,2015,115(19):10938-10966.
[4]李端,罗文,张云飞,等.新型载水飞蓟宾热敏脂质体-微泡SonoVue复合体制备及质量分析[J].中国超声医学杂志,2015,31(3):250-253.
[5] Kneidl B,Peller M,Winter G,et al. Thermosensitive liposomal drug delivery systems:state of the art review[J].Int J Nanomedicine,2014,9(1):4387-4398.
[6]叶兆伟,承伟.脂质体包封率测定方法及影响因素[J].中国生物制品学杂志,2007,20(10):789-792.
[7] Jin YG,Deng YJ. Thermosensitive liposomes[J]. Chin J Mod Appl Pharm,1998,15(6):1-4.
[8] Chelvi TP,Ralhan R. Designing of thermosensitive liposomes from natural lipids for multimodality cancer therapy[J].Int J Hyperthermia,1995,11(5):685-695.
[2] Li A,Shuai X,Jia Z,et al. Ganoderma lucidum polysaccharide extract inhibits hepatocellular carcinoma growth by downregulating regulatory T cells accumulation and function by inducing microRNA-125b[J]. J Transl Med,2015,13(1):100.
[3] Pattni BS,Chupin VV,Torchilin VP. New developments in liposomal drug delivery[J]. Chem Rev,2015,115(19):10938-10966.
[4]李端,罗文,张云飞,等.新型载水飞蓟宾热敏脂质体-微泡SonoVue复合体制备及质量分析[J].中国超声医学杂志,2015,31(3):250-253.
[5] Kneidl B,Peller M,Winter G,et al. Thermosensitive liposomal drug delivery systems:state of the art review[J].Int J Nanomedicine,2014,9(1):4387-4398.
[6]叶兆伟,承伟.脂质体包封率测定方法及影响因素[J].中国生物制品学杂志,2007,20(10):789-792.
[7] Jin YG,Deng YJ. Thermosensitive liposomes[J]. Chin J Mod Appl Pharm,1998,15(6):1-4.
[8] Chelvi TP,Ralhan R. Designing of thermosensitive liposomes from natural lipids for multimodality cancer therapy[J].Int J Hyperthermia,1995,11(5):685-695.