喷雾干燥法制备水溶性白藜芦醇/HP-β-CD微胶囊
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摘要
利用羟丙基-β-环糊精(HP-β-CD)改善Res的水溶性,优化了喷雾干燥法制备Res/HP-β-CD微胶囊的工艺,采用UV、IR和SEM对Res/HP-β-CD微胶囊进行结构表征。结果表明,Res/HP-β-CD微胶囊的优化制备工艺为wReswHP-β-CD15(g/g),搅拌温度30℃,进料流量2.1mL/min,进风温度140℃,载药量15.18%,溶解度12.75g/L。UV、IR和SEM结果表明,Res与HP-β-CD通过氢键、疏水作用力等作用力形成Res/HP-β-CD微胶囊,并且粒径减少,提高了Res的水溶性。
Hydroxypropyl-β-cyclodextrin(HP-β-CD)was used to improve water solubility of Res.The preparation conditions of Res/HP-β-CD microcapsule by spray drying method were optimized,and Res/HP-β-CD microcapsule was confirmed by UV,IR and SEM.The results showed that optimum preparation conditions of Res/HP-β-CD microcapsule were mass ratio of Res to HP-β-CD for 1:5,stirring at 30 ℃,feed flow rate for 2.1 mL/min and inlet-air temperature for 140 ℃.The rate of drug-loading and the solubility of Res were 15.18% and12.75 g/L,respectively,under the optimum conditions.UV,IR and SEM tests of Res/HP-β-CD microcapsule demonstrated that the aqueous solubility of Res increased due to the microcapsule formation between Res and HP-β-CD by hydrogen bond and hydrophobic forces,and the decrease of particle size.
Hydroxypropyl-β-cyclodextrin(HP-β-CD)was used to improve water solubility of Res.The preparation conditions of Res/HP-β-CD microcapsule by spray drying method were optimized,and Res/HP-β-CD microcapsule was confirmed by UV,IR and SEM.The results showed that optimum preparation conditions of Res/HP-β-CD microcapsule were mass ratio of Res to HP-β-CD for 1:5,stirring at 30 ℃,feed flow rate for 2.1 mL/min and inlet-air temperature for 140 ℃.The rate of drug-loading and the solubility of Res were 15.18% and12.75 g/L,respectively,under the optimum conditions.UV,IR and SEM tests of Res/HP-β-CD microcapsule demonstrated that the aqueous solubility of Res increased due to the microcapsule formation between Res and HP-β-CD by hydrogen bond and hydrophobic forces,and the decrease of particle size.
引文
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[24]曾张福,方岩雄,纪红兵,等.喷雾干燥法制备β-环糊精/香兰素微胶囊[J].精细化工,2012,29(7):59-63.
[25]DIZAJ S M,VAZIFEHASL Z,SALATIN S,et al.Nanosizing of drugs:Effect on dissolution rate[J].Research in Pharmaceutical Sciences,2015,10(2):95-108.
[26]康秋红.难溶性药物STVNa混合溶剂增溶技术及制剂产品的开发[D].广州:华南理工大学,2015:5.
[2]王冠群,曲静然,丁烽,等.Mal-β-CD对黑胡椒精油的包合作用研究[J].食品与机械,2012,28(1):22-25.
[3]DUARTE A,MARTINHO A,NGELO LUS,et al.Resveratrol encapsulation with methyl-β-cyclodextrin for antibacterial and antioxidant delivery applications[J].LWT-Food Science and Technology,2015,63(2):1 254-1 260.
[4]HSU C M,YU S C,TSAI F J,et al.Enhancement of rhubarb extract solubility and bioactivity by 2-hydroxy-propyl-β-cyclodextrin[J].Carbohydrate Polymers,2013,98(2):1 422-1 429.
[5]孔祥珍,黄飞,周治彤,等.小麦醇溶蛋白自组装纳米粒子负载白藜芦醇的性质研究[J].中国粮油学报,2017,32(11):21-25.
[6]CHEN Bao-yuan,KUO Chia-Hung,LIU Yung-chuan,et al.Ultrasonic-assisted extraction of the botanical dietary supplement resveratrol and other constituents of polygonum cuspidatum[J].Journal of Natural Products,2012,75(10):1 810-1 813.
[7]SURGULADZE M A,BEZHUASHVILI M G.Impact of wine technology on the variability of resveratrol and piceids in Saperavi(Vitis vinifera,L.)[J].Annals of Agrarian Science,2016,15(1):137-140.
[8]MA Li-jie,LI Wang-ping,WANG Rui-xuan,et al.Resveratrol enhanced anticancer effects of cisplatin on non-small cell lung cancer cell lines by inducing mitochondrial dysfunction and cell apoptosis[J].International Journal of Oncology,2015,47(4):1 460-1 468.
[9]VANCAUWENBERGHE E,NOYER L,DEROUICHE S,et al.Activation of mutated TRPA1ion channel by resveratrol in human prostate cancer associated fibroblasts(CAF)[J].Molecular Carcinogenesis,2017,56(8):1 851-1 867.
[10]SELVARAJ S,MOHAN A,NARAYANAN S,et al.Dose-dependent interaction of trans-resveratrol with biomembranes:effects on antioxidant property[J].Journal of Medicinal Chemistry,2013,56(3):970-981.
[11]GOKCE E H,TUNCAY T S,EROGLU I,et al.Wound healing effects of collagen-laminin dermal matriximpregnated with resveratrol loaded hyaluronic acid-DPPC microparticles in diabetic rats[J].European Journal of Pharmaceutics&Biopharmaceutics,2017,119:17-27.
[12]YANG Yan-jing,HU Liang,XIA Ye-peng,et al.Resveratrol suppresses glial activation and alleviates trigeminal neuralgia via activation of AMPK[J].Journal of Neuroinflammation,2016,13(1):1-11.
[13]DAVIDOV-PARDO G,MCCLEMENTS D J.Resveratrol encapsulation:Designing delivery systems to overcome solubility,stability and bioavailability issues[J].Trends in Food Science&Technology,2014,38(2):88-103.
[14]LU Zhong,CHENG Bo,HU Ye-li,et al.Complexation of resveratrol with cyclodextrins:solubility and antioxidant activity[J].Food Chemistry,2009,113(1):17-20.
[15]ZHANG Xiao-ping,LE Yuan,WANG Jie-xin,et al.Resveratrol nanodispersion with high stability and dissolution rate[J].LWT-Food Science and Technology,2013,50(2):622-628.
[16]高欣,谢文利,朱江,等.纳米级白藜芦醇和白藜芦醇β-环糊精包合物生物利用度的比较研究[J].中草药,2011,42(5):966-968.
[17]孙希岚.白藜芦醇的分离纯化和溶解度的测定与关联[D].杭州:浙江大学,2008:44-45.
[18]施永清,郁莉萍,潘王盈,等.改性柚皮纤维大豆分离蛋白复合膜的制备[J].中国食品学报,2018,18(2):102-111.
[19]安伟娟.白藜芦醇分子环糊精包合物的研究[D].保定:河北农业大学,2009:31-33.
[20]KAUR K,UPPAL S,KAUR R,et al.Energy efficient,facile and cost effective methodology for formation of an inclusion complex of resveratrol with hp-β-CD[J].New Journal of Chemistry,2015,39(11):8 855-8 865.
[21]TROCHEPESQUEIRA E,PREZJUSTE I,NAVARRO-VZQUEZ A,et al.Aβ-cyclodextrin-resveratrol inclusion complex and the role of geometrical and electronic effects on its electronic induced circular dichroism[J].Rsc Advances,2013,3(26):10 242-10 250.
[22]TANG Bo,MA Li,WANG Huai-you,et al.Study on the supramolecular interaction of curcumin and betacyclodextrin by spectrophotometry and its analytical application[J].Journal of Agricultural and Food Chemistry,2002,50(6):1 355-1 361.
[23]张伟锋,罗新,王建辉,等.一种简便的环糊精超分子包结比测算新方法[J].食品与机械,2017,33(9):5-8.
[24]曾张福,方岩雄,纪红兵,等.喷雾干燥法制备β-环糊精/香兰素微胶囊[J].精细化工,2012,29(7):59-63.
[25]DIZAJ S M,VAZIFEHASL Z,SALATIN S,et al.Nanosizing of drugs:Effect on dissolution rate[J].Research in Pharmaceutical Sciences,2015,10(2):95-108.
[26]康秋红.难溶性药物STVNa混合溶剂增溶技术及制剂产品的开发[D].广州:华南理工大学,2015:5.