大蒜素/海藻酸钠/明胶/壳聚糖复合微球的制备及性能

doi:10.16085/j.issn.1000-6613.2017-0245

摘要/Abstract

摘要： 以大蒜素为模型药物，采用复凝聚法制备了海藻酸钠/明胶/壳聚糖复合微球，考察了不同条件对微球溶胀性、载药性能和缓释性能等指标的影响。结果表明，明胶和海藻酸钠（质量比为1∶3）为2%，大蒜素投入量与混合胶比为1∶2时，制备的载药微球（DSGCM）外形规则，粒径分布在0.8～0.9mm之间，载药量为24.3%，包封率为69.4%，复合微球具有pH敏感性，在pH=7.4介质中微球溶胀率达到450%，药物释放过程符合Higuchi方程，明胶的加入可以延缓DSGCM复合微球的药物释放性能。

关键词: 大蒜素, 海藻酸钠, 明胶, 壳聚糖, 复合微球

Abstract: Sodium alginate/gelatin/chitosan composite microspheres were prepared by complex coacervation method using allicin as model drug. The effects of different conditions of swelling,drug loading and sustained release of DSGCM were investigated. The results showed that,when gelatin and sodium alginate(mass ratio 1∶3)was 2% and the allicin and the mix gel ratio was 1∶2,the preparation of DSGCM was spherical with particle sizes in the range of 0.8―0.9mm, and the drug loading and the entrapment efficiency were 24.3% and 69.4%,respectively. The composite microspheres was sensitive to pH,and the swelling rate of DSGCM was 450% in pH=7.4 media. The drug release process fitted well with the Higuchi equation kinetic model. The addition of gelatin could delay the drug release of DSGCM.

Key words: allicin, sodium alginate, gelatin, chitosan, composite microspheres

中图分类号:

TQ450.14

辛露露, 李付军, 薛飞, 张保华. 大蒜素/海藻酸钠/明胶/壳聚糖复合微球的制备及性能[J]. 化工进展, 2017, 36(10): 3826-3831.

XIN Lulu, LI Fujun, XUE Fei, ZHANG Baohua. Preparation and properties of allicin/sodium alginate/gelatin/chitosan composite microspheres[J]. Chemical Industry and Engineering Progress, 2017, 36(10): 3826-3831.

参考文献

[1] 俞苗,刘烈刚.大蒜素[J].营养学报,2013(6):528-531.YU M,LIU L G.Allicin[J].Acta Nutrimenta Sinica,2013(6):528-531.
[2] ZHANG Z D,LI Y,JIAO Z K,et al.Effect of local application of allicin via gastroscopy on cell proliferation and apoptosis of progressive gastric carcinoma[J].Chin.J.Integ.Tradit.West Med.,2008,28:108-110.
[3] 王莹,刘博,宫月华,等.不同幽门螺杆菌菌株对大蒜素药物敏感性的差异及其与胃疾病的相关性[J].中国医科大学学报,2009,38(1):15-18.WANG Y,GONG Y H,YUAN Y.Difference in susceptibility of different genotypes of helicobacter pylori to allitridi and its relationship with gastric diseases[J].Journal of China Medical University,2009,38(1):15-18.
[4] 薛东齐,许向阳,姜景彬,等.大蒜素对番茄叶霉菌不同生理小种的抑制作用[J].河南农业科学,2016,45(2):71-76.XUE D Q,XU X Y,JIANG J B,et al.Inhibition of allicin on different races of tomato leaf mold[J].Journal of Henan Agricultural Sciences,2016,45(2):71-76.
[5] 潘兴寿,蓝景生,李天资,等.大蒜素治疗病毒性心肌炎疗效分析[J].右江医学,2010,38(2):120-122.PAN X S,LAN J S,LI T Z,et al.Analysis on the effect of garlicin for treating viral myocarditis[J].Youjiang Medical Journal,2010,38(2):120-122.
[6] 杨融辉,吴晗,张宁.大蒜素抗氧化活性及其生物效应的研究进展[J].东南大学学报(医学版),2015,34(6):1037-1040.YANG R H,WU H,ZHANG N.Research progress on antioxidant activity and biological effects of allicin[J].Journal of Southeast University(Medical Science Edition),2015,34(6):1037-1040.
[7] CLOVES A C,MELISSA C,DAVID M,et al.Antimalarial activity of allicin,a biologically active compound from garlic[J].Antimicrob Agents Chemother,2006,50(5):1731.
[8] ILIC D P,NIKOKLIC V D,NIKOLIC L B,et al.Thermal degradation,antioxidant and antimicrobial activity of the synthesized allicin and allicin incorporated in gel[J].Hem.Ind.,2010,64(2):85-91.
[9] ZHANG H,CHINGIN K,ZHU L,et al.Molecular characterization of ongoing enzymatic reactions in raw garlic cloves using extractive electrospray ionization mass spectrometry[J].Anal.Chem.,2015,87(5):2878-2883.
[10] 吴洁,杨静静.大蒜素/有机凹凸棒黏土/海藻酸钠/壳聚糖复合微球的制备及其性能[J].中国生化药物杂志,2011,32(6):433-436.WU J,YANG J J.Preparation and the drug loading properties of allicin/attapulgite/sodium alginate and chitosan composite microspheres[J].Chinese Journal of Biochemical Pharmaceutics,2011,32(6):433-436.
[11] LEE K Y,MOONEY D J.Alginate:properties and biomedical applications[J].Progress in Polymer Science,2012,37(1):106-126.
[12] 胡永利,张淑平.基于海藻酸钠抗菌材料制备及应用的研究进展[J].化工进展,2016,35(4):1126-1131.HU Y L,ZHANG S P.Progress in preparation and application of sodium alginate antibacterial materials[J].Chemical Industry and Engineering Progress,2016,35(4):1126-1131.
[13] 徐群娜,范倩倩,马建中,等.壳聚糖基纳米胶囊的制备及应用研究新进展[J].材料导报,2015,29(1):81-85,91.XU Q N,FAN Q Q,MA J Z,et al.Recent advances in preparation and application of chitosan-based nanocapsules[J].Materials Review,2015,29(1):81-85,91.
[14] 徐婷婷,李治方,吴洁,等.缓释铜的凹土/海藻酸钠复合微球的制备及性能测试[J].化工进展,2013,32(2):410-413.XU T T,LI Z F,WU J,et al.Investigation on the preparation and characterization of palygorskite/sodium alginate composite microspheres for the sustained releasing of Cu²⁺[J].Chemical Industry and Engineering Progress,2013,32(2):410-413.
[15] 吴慧玲,张淑平.海藻酸钠纳米复合材料的研究应用进展[J].化工进展,2014,33(4):954-959.WU H L,ZHANG S P.Progress in the application of sodium alginate/nanomaterial composites[J].Chemical Industry and Engineering Progress,2014,33(4):954-959.
[16] 吴文果,刘伟,王士斌,等.海藻酸钙/聚精氨酸微胶囊的载药和缓释性能[J].化工进展,2014,33(5):1271-1275.WU WG,LIU W,WANG S B,et al.Drug loading and release of poly-L-arginine/calcium alginate microcapsules[J].Chemical Industry and Engineering Progress,2014,33(5):1271-1275.
[17] 贺宝元,张宝艳,李珊,等.载5-氟尿嘧啶壳聚糖/明胶微粒的制备及药物释放性能[J].化工进展,2016,35(7):2151-2155.HE B Y,ZHANG B Y,LI S,et al.Preparation of 5-fluorouracil loaded chitosan/gelatin particles and its' drug release properties[J].Chemical Industry and Engineering Progress,2016,35(7):2151-2155.
[18] 林粤顺,周新华,周红军,等.毒死蜱/羽毛蛋白/海藻酸钠复合微球的制备及其缓释性能[J].农药,2014,53(12):892-896,911.LIN Y S,ZHOU X H,ZHOU H J,et al.Preparation and slow-release performance of chlorpyrifos/feather keratin/sodium alginate microspheres[J].Agrochemicals,2014,53(12):892-896,911.
[19] 杨岚,王春华,林炜.明胶纳米颗粒的制备及应用进展[J].皮革科学与工程,2016,26(4):29-36.YANG L,WANG C H,LIN W.Advances in preparation and application of gelatin nanoparticles[J].Leather Science and Engineering,2016,26(4):29-36.
[20] 宋克东,虞泽,李瑞鹏,等.海藻酸钙/明胶微胶珠的制备、检测及神经干细胞相容性分析[J].高校化学工程学报,2015,29(5):1145-1153.SONG K D,YU Z,LI R P,et al.Preparation,characterization and neural stem cell biocompatibility of Ca-alginate-gelatin microbeads[J].Journal of Chemical Engineering of Chinese Universities,2015,29(5):1145-1153.
[21] 韩晓娜,黄国清,肖军霞.O-羧甲基壳聚糖/海藻酸钠微球的制备及取代度对微球溶胀性的影响[J].中国食品学报,2014,14(10):67-74.HAN X N,HUNG G Q,XIAO J X.Preparation of O-carboxymethyl chitosan/sodium alginate hydrogel beads and the effect of degree of substitution of O-carboxymethyl on the swelling properties of the beads[J].Journal of Chinese Institute of Food Science and Technology,2014,14(10):67-74.
[22] 刘云,张传杰,赵瑾朝,等.明胶/海藻酸钠(京尼平交联)互穿网络膜的制备与性能[J].复合材料学报,2015,32(4):997-1006.LIU Y,ZHANG C J,ZHAO J C,et al.Preparation and properties of gelatin/sodium alginate (cross-linked with genipin) interpenetrating polymeric network films[J].Acta Material Compositae Sinica,2015,32(4):997-1006.
[23] 李培培,李小芳,周维,等.魔芋葡甘聚糖-海藻酸钠载药凝胶微球的工艺研究[J].中药与临床,2015,6(6):19-22.LI P P,LI X F,ZHOU W,et al.Study on the preparation of drug-loaded gel microspheres using konjac glucomannan and sodium alginate[J].Pharmacy and Clinics of Chinese Materia Medica,2015,6(6):19-22.
[24] 张驰宇.pH敏感型海藻酸钙多孔凝胶微球的制备及溶胀性能的研究[J].功能材料,2010,41(12):2153.ZHANG C Y.Preparation and swelling property of pH-sensitive calcium alginate porous hydrogel microsphere[J].Journal of Functional Material,2010,41(12):2153.
[25] 刘伶俐,钱洋.pH 响应型壳聚糖-明胶水凝胶的制备研究[J].赤峰学院学报,2014,30(4):125-127.LIU L L,QIAN Y.Study on the preparation of pH responsive chitosan gel[J].Journal of Chifeng University (Natural Science Edition),2014,30(4):125-127.
[26] 黄正华,曹雁平,许朵霞,等.成胶条件对壳聚糖/海藻酸凝胶硬度的影响[J].中国食品学报,2015,15(2):163-167.CAO Z H,CAO Y P,XU D X,et al.The effects of gelling conditions on chitosan alginate gel rigidity[J].Journal of Chinese Institute of Food Science and Technology,2015,15(2):163-167.
[27] 吴洁,丁师杰,陈静,等.凹凸棒黏土对壳聚糖/海藻酸钠微球释放性能的影响[J].高校化学工程学报,2014,28(3):648-653.WU J,DING S J,CHEN J,et al.Effects of attapulgite on sustained release performance of chitosan/sodium alginate microspheres[J].Journal of Chemical Engineering of Chinese Universities,2014,28(3):648-653.
[28] 陈力,刘砚韬,黄亮,等.缓控释系统药物释放的数学模型研究进展[J].中国药业,2008,17(11):1-4.CHEN L,LIU Y T,HUANG L,et al.Research progress of mathematic model of sustained and controlled release system of drug release[J].China Pharmaceuticals,2008,17(11):1-4.