星点设计-效应面法优化低密度脂蛋白纳米粒处方与制备工艺
Optimization of formulation and preparation process of low density lipoprotein nanoparticle by central composite design-response surface methodology
作者:张青;马伟从;张霞;蹇丹;毛声俊;
Author:
收稿日期: 年卷(期)页码:2013,28(01):-12-15
期刊名称:华西药学杂志
Journal Name:WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字:低密度脂蛋白;纳米粒;星点设计―效应面法;处方设计;制备工艺
Key words:
基金项目:国家重大新药创制科技重大专项课题靶向释药系统与新制剂技术平台的建设(立项编号:2009ZX09310-002)
中文摘要
目的研制低密度脂蛋白纳米粒,优选其处方与制备工艺。方法采用薄膜-超声法制备脂微乳,连接含载脂蛋白apoprotein B-100中、低密度脂蛋白受体结合域序列的合成肽制备纳米粒。以脂质浓度、超声功率及超声时间为考察因素,粒径为指标,采用星点设计-效应面法优化其处方及制备工艺。结果优选的脂质浓度为0.1%;超声功率为380 w,超声时间为6 h。制备的纳米粒平均粒径为27.7 nm,PDI为0.17,ζ-电位为-28.7 mV。结论采用星点设计-效应面法优化低密度脂蛋白纳米粒的处方与制备工艺,制备的纳米粒粒径与预测值接近,表明用该法优化其处方与制备工艺可行。
参考文献
[1]Owens MD,Baillie G,Halbert GW.Physicochemical properties ofmicroemulsion analogues of low density lipoprotein containing am-phiphatic apoprotein B receptor sequences[J].Int J Pharm,2001,228(1-2):109-117.
[2]Hayavi S,Baillie G,Owens MD,et al.Receptor dependent cellu-lar uptake of synthetic low density lipoprotein by mammalian cellsin serum-free tissue culture[J].J Pharm Pharmacol,2006,58(10):1337-1342.
[3]Nikanjam M,Blakely EA,Bjornstad KA,et al.Synthetic nano-low density lipoprotein as targeted drug delivery vehicle for glio-blastoma mulsiforme[J].Int J Pharm,2007,328(1):86-94.
[4]Nikanjam M,Gibbs AR,Hunt CA,et al.Synthetic nano-LDLwith paclitaxel oleate as targeted drug delivery vehicle for glio-blastoma mulsiforme[J].J Cont Rel,2007,124(3):163-171.
[5]Zhou P,Hatziieremia S,Elliott MA,et al.Uptake of synthetic lowdensity lipoprotein by leukemic stem cells-a potential stem celltargeted drug delivery strategy[J].J Cont Rel,2010,148(3):380-387.
[6]宋玉品,王敏亭,黄园,等.星点设计-效应面法优化醋酸地寒木松脂质纳米粒的制备工艺[J].华西药学杂志,2011,26(3):264-267.
[7]Havayi S,Halbert GW.Synthetic low-density lipoprotein,anovel biomimetic lipid supplernent for serurn-free tissue culture[J].Biotechnol Prog,2005,21(4):1262-1268.
【关闭】