旋转中心组合设计法优化番茄红素纳米胶束的处方工艺
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摘要
目的利用旋转中心组合设计法(CCRD)优化番茄红素纳米胶束(LP-NM)的处方工艺。方法以酪蛋白-右旋糖酐接枝共聚物(CS-g-DX)为载体,采用乳化溶剂挥发法制备LP-NM;先以载药量(DL)及胶束粒径(Dr)为初步评价指标,进行单因素筛选确定影响LP-NM制备的主要因素;再以DL、Dr及多分散系数(PDI)为评价指标,采用CCRD优化LP-NM的处方工艺,对结果进行回归方程拟合,对最优条件进行预测分析。结果单因素筛选确定影响LP-NM制备的主要因素为酪蛋白浓度、乳化温度和载药比;各指标回归方程的拟合度较好;按处方优化得到的最佳条件制备LP-NM,各项指标的实测值与预测值接近。结论 CCRD可成功应用于LP-NM的处方工艺优化。
OBJECTIVE To optimize the formulation of lycopene-nanomicelles( LP-NM) using Central composite rotatable design method( CCRD). METHODS Casein-graft-dextran copolymer( CS-g-DX) was used as the carrier to prepare LP-NM by Emulsion solvent evaporation method. The main factors affecting the preparation of LP-NM were determined by Single factor screening with drug loading( DL) and particle size( Dr) as the preliminary evaluation indicators. CCRD was used to optimize the formulation process with DL,Dr and polydispersity coefficient( PDI) as the evaluation indicators. The data were imitated using regression equation,and the numerical optimization was performed. RESULTS Casein concentration,emulsifying temperature and the weight ratio of drug to casein were confirmed as the main factors affecting the preparation of LP-NM. LP-NM was prepared with optimum formulation,and the responses approached the prediction at the optimum. CONCLUSION CCRD can be successfully applied to the LP-NM prescription process optimization.
OBJECTIVE To optimize the formulation of lycopene-nanomicelles( LP-NM) using Central composite rotatable design method( CCRD). METHODS Casein-graft-dextran copolymer( CS-g-DX) was used as the carrier to prepare LP-NM by Emulsion solvent evaporation method. The main factors affecting the preparation of LP-NM were determined by Single factor screening with drug loading( DL) and particle size( Dr) as the preliminary evaluation indicators. CCRD was used to optimize the formulation process with DL,Dr and polydispersity coefficient( PDI) as the evaluation indicators. The data were imitated using regression equation,and the numerical optimization was performed. RESULTS Casein concentration,emulsifying temperature and the weight ratio of drug to casein were confirmed as the main factors affecting the preparation of LP-NM. LP-NM was prepared with optimum formulation,and the responses approached the prediction at the optimum. CONCLUSION CCRD can be successfully applied to the LP-NM prescription process optimization.
引文
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[2]Forssberg A,Lingen C,Ernster L,et al.Modification of X-irradiation syndrome by lycopene[J].Exp Cell Res,1959,16(1):7-14.
[3]Hu FL,Yi BW,Zhang WC,et al.Carotenoids and breast cancer risk:A meta-analysis and meta-regression[J].Breast Cancer Res Treat,2012,131(1):239-253.
[4]陈丽萍,何书英.番茄红素的抗氧化活性[J].华西药学杂志,2008,23(6):653-655.
[5]Clinton SK.Lycopene:Chemistry,biology,and implications for human health and disease[J].Nutr Rev,1998,56:35-51.
[6]徐向宏,何明珠.实验设计与Design-Expert、SPSS应用[M].北京:科学出版社,2010.
[7]Win K Y,Feng SS.Effects of particle size and surface coating on cellular uptake of polymeric nanoparticles for oral delivery of anticancer drugs[J].Biomaterials,2005,26(15):2713-2722.
[8]Nasir H,Vikas J,Alexander TF.Recent advances in the understanding of uptake of microparticulates across the gastrointestinal lymphatics[J].Adv Drug Deli Rev,2001,50(1-2):107-142.
[9]张培雯,黄园.载胰岛素纳米胶束的制备与表征[J].华西药学杂志,2014,29(5):487-490.