盐霉素纳米结构脂质载体冻干粉的制备
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摘要
目的制备盐霉素纳米结构脂质载体(Sal-NLCs)冻干粉。方法单因素考察冻干保护剂种类、剂量、加入方式、预冻方法等因素对Sal-NLCs粒径、多分散指数(PDI)和Zeta电位的影响,确定最佳冻干工艺,并测定Sal-NLCs冻干粉的制剂学性质进行考察。结果最佳冻干工艺:将5%的蔗糖冻干保护剂加入到制备好的Sal-NLCs溶液中,分别经-4℃、-20℃、-80℃预冻4 h、10 h、10 h,并冷冻干燥24 h。制备得到的冻干粉复溶后,粒径、PDI、Zeta电位及包封率较冻干前无明显变化。且冻干粉室温放置4周,体积不变,外观饱满紧凑。结论按照最佳冻干工艺制备的Sal-NLCs冻干粉性状稳定。
Objective To prepare salinomycin loaded nanostructured lipid carriers lyophilized powder.Methods The cryoprotector types,dosage,adding method was investigated by single factor method with particle size,Zeta potential and encapsulation efficiency of Sal-NLCs as evaluating indicator to determine the best freezedrying technology. The properties of Sal-NLCs freeze-dried powder was also studied. Results 5% of sucrose was added into the prepared Sal-NLCs solution. After a series of pre-freezing process,such as-4 ℃ for 4h,-20 ℃for 10 h,-80 ℃ for 10 h,the Sal-NLCs solution was transferred to freeze dryer immediately. The freeze dried powder prepared was well-stacked and there was no obvious change in particle size,Zeta potential and entrapment efficiency after rehydration. The powder still remained stable after it was placed at room temperature for 4 weeks.Conclusions The salinomycin loaded nanostructured lipid carriers lyophilized powder prepared by the optimum freeze-drying process are stable.
Objective To prepare salinomycin loaded nanostructured lipid carriers lyophilized powder.Methods The cryoprotector types,dosage,adding method was investigated by single factor method with particle size,Zeta potential and encapsulation efficiency of Sal-NLCs as evaluating indicator to determine the best freezedrying technology. The properties of Sal-NLCs freeze-dried powder was also studied. Results 5% of sucrose was added into the prepared Sal-NLCs solution. After a series of pre-freezing process,such as-4 ℃ for 4h,-20 ℃for 10 h,-80 ℃ for 10 h,the Sal-NLCs solution was transferred to freeze dryer immediately. The freeze dried powder prepared was well-stacked and there was no obvious change in particle size,Zeta potential and entrapment efficiency after rehydration. The powder still remained stable after it was placed at room temperature for 4 weeks.Conclusions The salinomycin loaded nanostructured lipid carriers lyophilized powder prepared by the optimum freeze-drying process are stable.
引文
[1]李秋艳,王敏,谢鹏,等.塞来昔布纳米结构脂质载体的制备及大鼠组织分布研究[J].中国药师,2016,19(2):277-281.
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[5]邱永宏,戈延茹,王成润,等.盐酸伊立替康脂质体冻干粉针的制备及其质量评价[J].江苏大学学报,2009,19(4):314-319.
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[9]杜周琦,李晓巍,赵秀峰,等.联合包载阿霉素和siRNA阳离子脂质体的制备及体外评价[J].沈阳药科大学学报,2016,33(11):839-843.
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[12]马艳红.制备米非司酮SLN冻干保护剂海藻糖作用显著[N].中国医药报,2005-08-11(A08)[2017-04-20].
[13]刘凯,孙进,何仲贵.新型纳米结构脂质载体系统的研究进展[J].沈阳药科大学学报,2008,25(3):236-242.
[14]陈锋,金日显,陈燕军.纳米结构脂质载体的研究进展[J].中国新药杂志,2008,17(6):456-460.
[15]Wanga M,Thanoua M.Targeting nanoparticles to cancer[J].Pharmacol Res,2010,62:90-99.
[16]宋时雨.PG脂质体的冻干工艺研究[D].武汉.华中科技大学,2012.
[17]刘娟,胡水根,卞俊,等.冻干保护剂对HB有效组分脂质体包封率和粒径的影响[J].时珍国医国药,2007,18(9):2119-2121.
[18]苏树强,华泽钊,丁志华,等.冻干保护剂和复溶水溶液对HBIa脂质体包封率的影响[J].中国新药杂志,2004,13(9):809-812.
[19]邓礼荷,韦敏燕,汤晨懿,等.冻干工艺及保护剂对羟基喜树碱脂质体质量的影响[J].中国医药工业杂志,2012,43(1):30-34.
[20]Zhang W,Li X,Ye T,et al.Design,characterization,and in vitro cellular inhibition and uptake of optimized genistein-loaded NLC for the prevention of posterior capsular opacification using response surface methodology[J].Int J Pharm,2013,454(1):354-366.
[2]黄龙,王毅,汪翼.盐霉素抗肿瘤机制的相关研究进展[J].中南医学科学杂志,2016,44(1):117-120.
[3]方亮.药剂学[M].8版.北京:人民卫生出版社,2016:329.
[4]周晖,邱立朋,闫笑笑,等.奥沙利铂纳米结构脂质载体的制备及表征[J].药学学报,2010,45(9):1177-1182.
[5]邱永宏,戈延茹,王成润,等.盐酸伊立替康脂质体冻干粉针的制备及其质量评价[J].江苏大学学报,2009,19(4):314-319.
[6]张洪记.多西他赛冻干脂质体的研究[D].镇江:江苏大学,2011.
[7]唐文雅,宋艳志,邓意辉.脂质体冻干保护剂的种类及其作用机制研究进展[J].沈阳药科大学学报,2012,29(7):560-569.
[8]杨柳,姚瑰玮,王秀玲,等.替尼泊苷冻干粉针剂的处方及冻干工艺研究[J].中国抗生素杂志,2014,39(3):224-228.
[9]杜周琦,李晓巍,赵秀峰,等.联合包载阿霉素和siRNA阳离子脂质体的制备及体外评价[J].沈阳药科大学学报,2016,33(11):839-843.
[10]Mitri K,Shegokar R,Gohla S,et al.Lipid nanocarriers for dermal delivery of lutein:preparation,characterization,stability and performance[J].Int J Pharm,2011,414(1/2):267-275.
[11]P uglia C,Damiani E,Offerta A,et al.Evaluation of nanostructured lipid carriers(NLC)and nanoemulsions as carriers for UV-filters:characterization,in vitro penetration and photostability studies[J].Eur J Pharm Sci,2014,51:211-217.
[12]马艳红.制备米非司酮SLN冻干保护剂海藻糖作用显著[N].中国医药报,2005-08-11(A08)[2017-04-20].
[13]刘凯,孙进,何仲贵.新型纳米结构脂质载体系统的研究进展[J].沈阳药科大学学报,2008,25(3):236-242.
[14]陈锋,金日显,陈燕军.纳米结构脂质载体的研究进展[J].中国新药杂志,2008,17(6):456-460.
[15]Wanga M,Thanoua M.Targeting nanoparticles to cancer[J].Pharmacol Res,2010,62:90-99.
[16]宋时雨.PG脂质体的冻干工艺研究[D].武汉.华中科技大学,2012.
[17]刘娟,胡水根,卞俊,等.冻干保护剂对HB有效组分脂质体包封率和粒径的影响[J].时珍国医国药,2007,18(9):2119-2121.
[18]苏树强,华泽钊,丁志华,等.冻干保护剂和复溶水溶液对HBIa脂质体包封率的影响[J].中国新药杂志,2004,13(9):809-812.
[19]邓礼荷,韦敏燕,汤晨懿,等.冻干工艺及保护剂对羟基喜树碱脂质体质量的影响[J].中国医药工业杂志,2012,43(1):30-34.
[20]Zhang W,Li X,Ye T,et al.Design,characterization,and in vitro cellular inhibition and uptake of optimized genistein-loaded NLC for the prevention of posterior capsular opacification using response surface methodology[J].Int J Pharm,2013,454(1):354-366.