胰岛素缓控释制剂的研究进展
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摘要
糖尿病是目前患病率较高的疾病,皮下注射胰岛素是治疗糖尿病的主要方法。天然胰岛素属于多肽蛋白类药物,体内半衰期较短,维持长时间的稳态血药浓度,需要频繁给药,患者的顺应性低。将胰岛素包封在生物相容性好的材料中制成微球或原位植入系统,可在注射部位缓慢持续释放胰岛素,减少注射给药的次数,增加患者的依从性。分析了目前胰岛素注射缓控释制剂的设计思路及相关研究进展。
Diabetes is a disease with a high prevalence,and subcutaneous insulin injection is the main method for treating diabetes. Natural insulin belongs to polypeptide protein drugs,has a short half-life in vivo,requires frequent administration to maintain a long-term steady-state blood drug concentration,and has low patient compliance. Insulin is encapsulated in a biocompatible material to form a microsphere or in situ implantation system,so that insulin capsule can slowly and continuously release insulin at the injection site so as to reduce the number of jections and increase patient compliance. This article reviews the current design ideas and research progress of insulin injection controlled release preparations.
Diabetes is a disease with a high prevalence,and subcutaneous insulin injection is the main method for treating diabetes. Natural insulin belongs to polypeptide protein drugs,has a short half-life in vivo,requires frequent administration to maintain a long-term steady-state blood drug concentration,and has low patient compliance. Insulin is encapsulated in a biocompatible material to form a microsphere or in situ implantation system,so that insulin capsule can slowly and continuously release insulin at the injection site so as to reduce the number of jections and increase patient compliance. This article reviews the current design ideas and research progress of insulin injection controlled release preparations.
引文
[1]包星海，栾立标．对药物缓控释制剂的研究进展[J]．当代医药论丛，2017,15(23):36-37.
[2]李光华．微粒给药系统在体内分布的特点及制剂研究进展[J]．天津药学，2013,25(2):47-49.
[3]焦姣，蒋宫平，邓意辉．脂质体药物传递系统的50年发展历程概述[J]．沈阳药科大学学报，2014,31(9):738-754.
[4]张翠梅，李银莲．微粒给药系统的研究进展[J]．现代中西医结合杂志，2010,19(19):2463-2466.
[5]张煊，张华，王桂玲，等．正常大鼠静脉注射PEG包裹胰岛素脂质体的降血糖作用[J]．中国药学(英文版)，2004,13(1):28-31.
[6]韩凌，孙治国，鲁莹．抗肿瘤药物纳米粒载体的制备材料、包载药物及修饰方法[J]．药学实践杂志，2018,36(4):307-312.
[7]金红妍，李云飞，高钟镐．纳米粒载体研发及其对生物效应影响的研究进展[J]．中国药学杂志，2017,52(10):814-818.
[8]王颐婷．聚乙二醇/聚己内酯/聚乙烯亚胺载胰岛素纳米粒的制备及其体内外释放性质考察[D]．广州:南方医科大学，2016.
[9]赵莺歌．胰岛素/PLGA缓释纳米粒的研究[D]．石家庄:河北科技大学，2015.
[10]Zhang Z,Cai H,Liu Z,et al. Effective enhancement of hypoglycemic effect of insulin by liver-targeted nanoparticles containing cholic acid-modified chitosan derivative[J]. Mol Pharm,2016,13(7):2433-2442.
[11]Peng Q,Gong T,Zuo J,et al. Enhanced oral bioavailability of salvianolic acid B by phospholipid complex loaded nanoparticles[J]. Pharmazie,2008,63(9):661-666.
[12]Peng Q,Zhang Z,Sun X,et al. Mechanisms of phospholipid complex loaded nanoparticles enhancing the oral bioavailability[J]. Mol Pharm,2010,7(2):565-575.
[13]Peng Q,Zhang Z R,Gong T,et al. A rapid-acting,long-acting insulin formulation based on a phospholipid complex loaded PHBHHx nanoparticles[J]. Biomaterials,2012,3(5):1583-1588.
[14]吴蕾，朱雯婷，王俊，等．胰岛素缓释载体聚乙二醇—聚己内酯—聚甲基丙烯酸-N,N-二乙氨基乙酯的制备及评价[J]．南方医科大学学报，2017,37(7):975-982.
[15]方亮．药剂学[M]．北京:人民卫生出版社，2016.
[16]王峰，涂家生，张钧寿，等．PLGA微球控释系统的突释及其控制[J]．药学进展，2003,27(3):142-146.
[17]Kenneth D,Kathleen M,Campbell,et al. PEGylated insulin in PLGA microparticles. In vivo and in vitro analysis[J]. J Contr Rel,2005,104(3):447-460.
[18]杨辰辰．胰岛素长效释药系统在糖尿病治疗中的研究[D]．保定:河北大学，2017.
[19]魏刚，陆伟跃，郑俊民．温度敏感原位凝胶中药物的扩散行为[J]．药学学报，2004,39(3):232-235.
[20]张升，王利胜，赖宝林，等．温敏型原位凝胶的热力学及流变学性质研究[J]．中国医院药学杂志，2012,32(2):103-106.
[21]魏刚，徐晖，郑俊民．原位凝胶的形成机制及在药物控制释放领域的应用[J]．中国药学杂志，2003,38(8):564-568.
[22]李欣宇．泊洛沙姆温度敏感型原位凝胶的研制[D]．重庆:重庆医科大学，2008.
[23]Zhang L,Parsons D L. Navarre C,et al. Development and invitro evaluation of sustained release Poloxamer 407(P407)gel formulations of ceftiofur[J]. J Contr Rel,2002,85(1/2/3):73-81.
[24]印娜，秧茂盛．辅料泊洛沙姆407的作用与应用[J]．中国当代医药，2018,25(10):27-30.
[25]Ur-Rehman T,Tavelin S,Grbner G. Chitosan in situ gelation for improved drug loading and retention in poloxamer 407 gels[J]. Int J Pharm,2011,409(1):19-29.
[26]Barichello J M,Morishita M,Takayama K,et al. Absorption of insulin from pluronic F-127 gels following subcutaneous administration in rats[J]. Int J Pharm,1999,184(2):189-198.
[27]Kang F,Singh J. In vitro release of insulin and biocompatibility of in situ forming gel systems[J]. Int J Pharm,2005,304(1):83-90.
[28]Oak M,Singh J. Chitosan-zinc-insulin complex incorporated thermosensitive polymer for controlled delivery of basal insulin in vivo[J]. J Contr Rel,2012,163(2):145-153.
[29]高婷婷．温敏性羟丁基壳聚糖水凝胶用于胰岛素缓释载体研究[D]．青岛:中国海洋大学，2014.
[30]李臻益，胡晓玉，强琚莉，等．闭路智能胰岛素载药体系的研究进展[J]．有机化学，2018,38(1):29-39.
[31]唐富山，李锋，王竞，等．自组装短肽原位凝胶用作蛋白药物载体的初步研究[J]．中国药房，2009,20(7):522-525.
[32]Al-Achi A,Greenwood R. Erythrocytes as oral delivery systems for human insulin[J]. Drug Dev Ind Pharm,1998,24(1):67-72.
[33]Xia D,He H,Wang Y,et al. Ultrafast glucose-responsive,high loading capacity erythrocyte to self-regulate the release of insulin[J]. Acta Biomater,2018,69:301-312.
[34]Zhao F,Wu D,Yao D,et al. An injectable particle-hydrogel hybrid system for glucose-regulatory insulin delivery[J]. Acta Biomater,2017,64:334-345.
[35]Li X,Fu M,Wu J,et al. PH-sensitive peptide hydrogel for glucose-responsive insulin delivery[J]. Acta Biomater,2017,51:294-303.
[36]Sun L,Zhang X,Zheng C,et al. A p H gated,glucose-sensitive nanoparticle based on worm-likemesoporous silica for controlled insulin release[J]. J Phys Chem B,2013,117(14):3852-3860.
[2]李光华．微粒给药系统在体内分布的特点及制剂研究进展[J]．天津药学，2013,25(2):47-49.
[3]焦姣，蒋宫平，邓意辉．脂质体药物传递系统的50年发展历程概述[J]．沈阳药科大学学报，2014,31(9):738-754.
[4]张翠梅，李银莲．微粒给药系统的研究进展[J]．现代中西医结合杂志，2010,19(19):2463-2466.
[5]张煊，张华，王桂玲，等．正常大鼠静脉注射PEG包裹胰岛素脂质体的降血糖作用[J]．中国药学(英文版)，2004,13(1):28-31.
[6]韩凌，孙治国，鲁莹．抗肿瘤药物纳米粒载体的制备材料、包载药物及修饰方法[J]．药学实践杂志，2018,36(4):307-312.
[7]金红妍，李云飞，高钟镐．纳米粒载体研发及其对生物效应影响的研究进展[J]．中国药学杂志，2017,52(10):814-818.
[8]王颐婷．聚乙二醇/聚己内酯/聚乙烯亚胺载胰岛素纳米粒的制备及其体内外释放性质考察[D]．广州:南方医科大学，2016.
[9]赵莺歌．胰岛素/PLGA缓释纳米粒的研究[D]．石家庄:河北科技大学，2015.
[10]Zhang Z,Cai H,Liu Z,et al. Effective enhancement of hypoglycemic effect of insulin by liver-targeted nanoparticles containing cholic acid-modified chitosan derivative[J]. Mol Pharm,2016,13(7):2433-2442.
[11]Peng Q,Gong T,Zuo J,et al. Enhanced oral bioavailability of salvianolic acid B by phospholipid complex loaded nanoparticles[J]. Pharmazie,2008,63(9):661-666.
[12]Peng Q,Zhang Z,Sun X,et al. Mechanisms of phospholipid complex loaded nanoparticles enhancing the oral bioavailability[J]. Mol Pharm,2010,7(2):565-575.
[13]Peng Q,Zhang Z R,Gong T,et al. A rapid-acting,long-acting insulin formulation based on a phospholipid complex loaded PHBHHx nanoparticles[J]. Biomaterials,2012,3(5):1583-1588.
[14]吴蕾，朱雯婷，王俊，等．胰岛素缓释载体聚乙二醇—聚己内酯—聚甲基丙烯酸-N,N-二乙氨基乙酯的制备及评价[J]．南方医科大学学报，2017,37(7):975-982.
[15]方亮．药剂学[M]．北京:人民卫生出版社，2016.
[16]王峰，涂家生，张钧寿，等．PLGA微球控释系统的突释及其控制[J]．药学进展，2003,27(3):142-146.
[17]Kenneth D,Kathleen M,Campbell,et al. PEGylated insulin in PLGA microparticles. In vivo and in vitro analysis[J]. J Contr Rel,2005,104(3):447-460.
[18]杨辰辰．胰岛素长效释药系统在糖尿病治疗中的研究[D]．保定:河北大学，2017.
[19]魏刚，陆伟跃，郑俊民．温度敏感原位凝胶中药物的扩散行为[J]．药学学报，2004,39(3):232-235.
[20]张升，王利胜，赖宝林，等．温敏型原位凝胶的热力学及流变学性质研究[J]．中国医院药学杂志，2012,32(2):103-106.
[21]魏刚，徐晖，郑俊民．原位凝胶的形成机制及在药物控制释放领域的应用[J]．中国药学杂志，2003,38(8):564-568.
[22]李欣宇．泊洛沙姆温度敏感型原位凝胶的研制[D]．重庆:重庆医科大学，2008.
[23]Zhang L,Parsons D L. Navarre C,et al. Development and invitro evaluation of sustained release Poloxamer 407(P407)gel formulations of ceftiofur[J]. J Contr Rel,2002,85(1/2/3):73-81.
[24]印娜，秧茂盛．辅料泊洛沙姆407的作用与应用[J]．中国当代医药，2018,25(10):27-30.
[25]Ur-Rehman T,Tavelin S,Grbner G. Chitosan in situ gelation for improved drug loading and retention in poloxamer 407 gels[J]. Int J Pharm,2011,409(1):19-29.
[26]Barichello J M,Morishita M,Takayama K,et al. Absorption of insulin from pluronic F-127 gels following subcutaneous administration in rats[J]. Int J Pharm,1999,184(2):189-198.
[27]Kang F,Singh J. In vitro release of insulin and biocompatibility of in situ forming gel systems[J]. Int J Pharm,2005,304(1):83-90.
[28]Oak M,Singh J. Chitosan-zinc-insulin complex incorporated thermosensitive polymer for controlled delivery of basal insulin in vivo[J]. J Contr Rel,2012,163(2):145-153.
[29]高婷婷．温敏性羟丁基壳聚糖水凝胶用于胰岛素缓释载体研究[D]．青岛:中国海洋大学，2014.
[30]李臻益，胡晓玉，强琚莉，等．闭路智能胰岛素载药体系的研究进展[J]．有机化学，2018,38(1):29-39.
[31]唐富山，李锋，王竞，等．自组装短肽原位凝胶用作蛋白药物载体的初步研究[J]．中国药房，2009,20(7):522-525.
[32]Al-Achi A,Greenwood R. Erythrocytes as oral delivery systems for human insulin[J]. Drug Dev Ind Pharm,1998,24(1):67-72.
[33]Xia D,He H,Wang Y,et al. Ultrafast glucose-responsive,high loading capacity erythrocyte to self-regulate the release of insulin[J]. Acta Biomater,2018,69:301-312.
[34]Zhao F,Wu D,Yao D,et al. An injectable particle-hydrogel hybrid system for glucose-regulatory insulin delivery[J]. Acta Biomater,2017,64:334-345.
[35]Li X,Fu M,Wu J,et al. PH-sensitive peptide hydrogel for glucose-responsive insulin delivery[J]. Acta Biomater,2017,51:294-303.
[36]Sun L,Zhang X,Zheng C,et al. A p H gated,glucose-sensitive nanoparticle based on worm-likemesoporous silica for controlled insulin release[J]. J Phys Chem B,2013,117(14):3852-3860.
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