用于构建可溶性微针的基质材料及其复合材料<sup>*</sup>

doi:10.11896/j.issn.1005-023X.2017.019.018

Abstract
Figure/Table
References
Related Citation (15)

Download:

Full Text ( PDF ) (1333KB)
Export: BibTeX | EndNote (RIS)

Abstract As a novel transdermal drug delivery system, dissolvable microneedle has broken the limitations of traditional transdermal formulations which are not able to deliver macromolecular. Besides the aspect of macromolecular delivery, dissolvable microneedles have numerous advantages including small enough to avoid causing pain, minimal skin trauma, no bleeding or introduction of pathogens, good biocompatibility, easy to self-administration, etc. The study of dissolvable microneedle has recently become a hot topic. The choice of matrix materials directly affects the preparation process of microneedle, as well as the properties of skin puncturing and drug releasing. This paper introduces the research status of dissolvable microneedle, classifies and introduces the matrix materials, then summarizes the use of their compounds. The properties of ductile materials and brittle materials and their synergistic effects after composite are introduced as well. Finally, the existing problems and research directions in this field are discussed.

Key words： dissolvable microneedle material classification composite ductile material brittle material

Published: 07 May 2018

CLC number:	R944.9
	TB332

	Service
	E-mail this article
	Add to my bookshelf
	Add to citation manager
	E-mail Alert
	RSS
	Articles by authors
	ZHANG Jie
	MA Fengsen
	ZHAN Haohui
	HUANG Yingcong

Cite this article:

ZHANG Jie,MA Fengsen,ZHAN Haohui, et al. Matrix Materials and Their Composites for Dissolvable Microneedle Construction: a Review[J]. Materials Reports, 2017, 31(19): 129-134.

URL:

http://www.mater-rep.com/EN/10.11896/j.issn.1005-023X.2017.019.018 OR http://www.mater-rep.com/EN/Y2017/V31/I19/129

1 Gerstel M S, Place V A. Drug delivery device: US, 3964482[P].1976-06-22.
2 Kim Y C, Park J H, Prausnitz M R. Microneedles for drug and vaccine delivery[J]. Adv Drug Delivery Rev,2012,64(14):1547.
3 Matsuo K, Hirobe S, Yokota Y, et al. Transcutaneous immunization using a dissolving microneedle array protects against tetanus, diphtheria, malaria, and influenza[J]. J Controlled Release,2012,160(3):495.
4 Matsuo K, Yokota Y, Zhai Y, et al. A low-invasive and effective transcutaneous immunization system using a novel dissolving microneedle array for soluble and particulate antigens[J]. J Controlled Release,2012,161(1):10.
5 Demuth P C, Garcia-Beltran W F, Ai-Ling M L, et al. Composite dissolving microneedles for coordinated control of antigen and adjuvant delivery kinetics in transcutaneous vaccination[J]. Adv Funct Mater,2013,23(2):161.
6 Park Y H, Ha S K, Choi I, et al. Fabrication of degradable carboxymethyl cellulose (CMC) microneedle with laser writing and replica molding process for enhancement of transdermal drug delivery[J]. Biotechnol Bioprocess Eng,2016,21(1):110.
7 Ito Y, Maeda T, Fukushima K, et al. Permeation enhancement of ascorbic acid by self-dissolving micropile array tip through rat skin[J]. Chem Pharmaceutical Bull,2010,58(4):458.
8 Lee K, Lee C Y, Jung H. Dissolving microneedles for transdermal drug administration prepared by stepwise controlled drawing of mal-tose[J]. Biomaterials,2011,32(11):3134.
9 Zhu Z, Luo H, Lu W, et al. Rapidly dissolvable microneedle patches for transdermal delivery of exenatide[J]. Pharmaceutical Res,2014,31(12):3348.
10 Liu S, Quan Y S, Fumio K, et al. Preparation and characterization of novel hyaluronic acid microneedles for insulin transdermal delivery[J]. J Shenyang Pharmaceutical University,2010,27(1):6(in Chinese).
刘姝, 权英淑, 神山文男, 等. 新型经皮传递胰岛素透明质酸微针制剂的制备及性能考察[J]. 沈阳药科大学学报,2010,27(1):6.
11 Liu S, Jin M N, Quan Y S, et al. The development and characteristics of novel microneedle arrays fabricated from hyaluronic acid, and their application in the transdermal delivery of insulin[J]. J Controlled Release,2012,161(3):933.
12 Liu S, Wu D, Quan Y S, et al. Improvement of transdermal delivery of exendin-4 using novel tip-loaded microneedle arrays fabricated from hyaluronic acid[J]. Mol Pharm,2016,13(1):272.
13 Ye Y, Wang J, Hu Q, et al. Synergistic transcutaneous immunotherapy enhances antitumor immune responses through delivery of checkpoint inhibitors[J]. ACS Nano,2016,10(9):8956.
14 Zhang Y, et al. Thrombin-responsive transcutaneous patch for auto-anticoagulant regulation[J]. Adv Mater,2017,29(4):1604043.
15 Ito Y, Murakami A, Maeda T, et al. Evaluation of self-dissolving needles containing low molecular weight heparin (LMWH) in rats[J]. Int J Pharmaceutics,2008,349(1-2):124.
16 Tsioris K, Raja W K, Pritchard E M, et al. Fabrication of silk microneedles for controlled-release drug delivery[J]. Adv Funct Mater,2012,22(2):330.
17 Lee J W, Choi S O, et al. Dissolving microneedle patch for transdermal delivery of human growth hormone[J]. Small,2011,7(4):531.
18 Chan C, Caffarel-Salvador E, Brady A J, et al. Hydrogel-forming microneedle arrays allow detection of drugs and glucose in vivo: Potential for use in diagnosis and therapeutic drug monitoring[J]. PLOS ONE,2015,10(12):e0145644.
19 Caffarel-Salvador E, Tuan-Mahmood T M, Mcelnay J C, et al. Potential of hydrogel-forming and dissolving microneedles for use in paediatric populations[J]. Int J Pharm,2015,489(1-2):158.
20 Lutton R E, Larraneta E, Kearney M C, et al. A novel scalable manufacturing process for the production of hydrogel-forming microneedle arrays[J]. Int J Pharm,2015,494(1):417.
21 Cha K J, Kim T, Park S J, et al. Simple and cost-effective fabrication of solid biodegradable polymer microneedle arrays with adjustable aspect ratio for transdermal drug delivery using acupuncture microneedles[J]. J Micromech Microeng,2014,24(11):115015.
22 Park J H, et al. Polymer particle-based micromolding to fabricate novel microstructures[J]. Biomed Microdevices,2007,9(2):223.
23 Dangol M, Yang H, Li C G, et al. Innovative polymeric system (IPS) for solvent-free lipophilic drug transdermal delivery via dissolving microneedles[J]. J Controlled Release,2016,223:118.
24 Kim J D, et al. Droplet-born air blowing: Novel dissolving microneedle fabrication[J]. J Controlled Release,2013,170(3):430.
25 Liu S, Jin M N, Quan Y S, et al. Transdermal delivery of relatively high molecular weight drugs using novel self-dissolving microneedle arrays fabricated from hyaluronic acid and their characteristics and safety after application to the skin[J]. Eur J Pharmaceutics Biopharmaceutics, 2014,86(2):267.
26 Sullivan S P, Murthy N, Prausnitz M R. Minimally invasive protein delivery with rapidly dissolving polymer microneedles[J]. Adv Mater,2008,20(5):933.
27 Lee J W, Park J H, Prausnitz M R. Dissolving microneedles for transdermal drug delivery[J]. Biomaterials,2008,29(13):2113.
28 Martin C J, Allender C J, Brain K R, et al. Low temperature fabrication of biodegradable sugar glass microneedles for transdermal drug delivery applications[J]. J Controlled Release, 2012,158(1):93.
29 Donnelly R F, Morrow D I, Singh T R, et al. Processing difficulties and instability of carbohydrate microneedle arrays[J]. Drug Deve-lopment Ind Pharmacy,2009,35(10):1242.
30 Gao Z P, Yue T L, Yuan Y H, et al. Research progress on producing technology and the applied characteristics of fructose[J]. J Northwest Sci-Tech University of Agriculture and Forestry (Nat Sci Ed),2003,31(s1):187(in Chinese).
高振鹏, 岳田利, 袁亚宏, 等. 果糖生产技术和应用研究进展[J]. 西北农林科技大学学报(自然科学版),2003,31(s1):187.
31 Mcgrath M G, Vucen S, Vrdoljak A, et al. Production of dissolvable microneedles using an atomised spray process: Effect of microneedle composition on skin penetration[J]. Eur J Pharmaceutics Biopharmaceutics,2014,86(2):200.
32 Peng Y F, Zhou Y B, Li Q, et al. Application prospect of trehalose[J]. China Food Additives, 2009(1):42(in Chinese).
彭亚锋, 周耀斌, 李勤, 等. 海藻糖的特性及其应用[J]. 中国食品添加剂,2009(1):42.
33 Vrdoljak A, et al. Induction of broad immunity by thermostabilised vaccines incorporated in dissolvable microneedles using novel fabrication methods[J]. J Controlled Release,2016,225:192.
34 Choi H J, Yoo D G, Bondy B J, et al. Stability of influenza vaccine coated onto microneedles[J]. Biomaterials,2012,33(14):3756.
35 Lee K, Jung H. Drawing lithography for microneedles: A review of fundamentals and biomedical applications[J]. Biomaterials,2012,33(30):7309.
36 Chu L Y, Prausnitz M R. Separable arrowhead microneedles[J]. J Controlled Release,2011, 149(3):242.
37 Wei P P. Extraction and preparation of raffinose from defatted wheat germ[D]. Wuxi: Jiangnan University,2011(in Chinese).
魏培培. 脱脂麦胚中棉子糖的提取制备[D]. 无锡:江南大学,2011.
38 Zhang Y K, Jin J S. A kind of functional cosmetic ingredient—Hya-luronic acid[J]. China Surfactant Detergent Cosmetics,2004,34(2):111(in Chinese).
张延坤, 金京顺. 一种功能性化妆品原料——透明质酸[J]. 日用化学工业,2004, 34(2):111.
39 Bian J, Zhou Y P. Clinical application of hyaluronic acid [J]. Chin J Injury Repair Wound Healing (Electron Ed),2008,3(5):60(in Chinese).
卞靖, 周业平. 透明质酸的临床应用[J]. 中华损伤与修复杂志(电子版),2008,3(5):60.
40 Lu L, Leng Y, Chen Y. An experiment study on wound healing with exogenous hyaluronic acid[J]. Chin J Plastic Surgery,2000(1):30(in Chinese).
吕洛, 冷永成,陈玉林. 透明质酸对创面愈合胶原代谢影响的实验研究[J]. 中华整形外科杂志, 2000(1):30.
41 Katsumi H, Liu S, Tanaka Y, et al. Development of a novel self-dissolving microneedle array of alendronate, a nitrogen-containing bisphosphonate: Evaluation of transdermal absorption, safety, and pharmacological effects after application in rats[J]. J Pharmaceutical Sci,2012,101(9):3230.
42 Monkare J, Reza Nejadnik M, Baccouche K, et al. IgG-loaded hyaluronan-based dissolving microneedles for intradermal protein deli-very[J]. J Controlled Release,2015,218:53.
43 Gao C M, Liu M Z, Lv S Y, et al. Preparation of sodium alginate hydrogel and its application in drug release[J]. Prog Chem,2013,25(6):1012(in Chinese).
高春梅, 柳明珠, 吕少瑜, 等. 海藻酸钠水凝胶的制备及其在药物释放中的应用[J]. 化学进展,2013,25(6):1012.
44 Yusuf K, Demir Z A, Oya Kerimoglu. Sodium alginate microneedle arrays mediate the transdermal delivery of bovine serum albumin[J]. Plos One,2013,8(5):1224.
45 Li H P, Li B, et al. Advances in characterization of amylose and amylopectin starch[J]. Food Sci,2010,31(11):273(in Chinese).
李海普, 李彬, 等. 直链淀粉和支链淀粉的表征[J]. 食品科学,2010,31(11):273.
46 Wendorf J R, Ghartey-Tagoe E B, Williams S C, et al. Transdermal delivery of macromolecules using solid-state biodegradable microstructures[J]. Pharmaceutical Res,2010,28(1):22.
47 Hassan C M, Stewart J E, Peppas N A. Diffusional characteristics of freeze/thawed poly(vinyl alcohol) hydrogels: Applications to protein controlled release from multilaminate devices[J]. Eur J Pharmaceutics Biopharmaceutics,2000,49(2):161.
48 Dou X W. Preparation of phase transition hydrogel microneedle arrays for transdermal delivery of insulin[D]. Shanghai: Shanghai Jiao Tong University,2009(in Chinese).
窦学文. 用于胰岛素透皮给药的相转化水凝胶微针点阵的制备[D]. 上海:上海交通大学, 2009.
49 Fukushima K, Ise A, Morita H, et al. Two-layered dissolving microneedles for percutaneous delivery of peptide/protein drugs in rats[J]. Pharmaceutical Res,2010,28(1):7.
50 Hiraishi Y, Nakagawa T, Quan Y S, et al. Performance and characteristics evaluation of a sodium hyaluronate-based microneedle patch for a transcutaneous drug delivery system[J]. Int J Pharmaceutics,2013,441(1-2):570.
51 Hou J. The study on insoluble silk microneedle[D]. Suzhou:Soochow University,2014(in Chinese).
侯静. 不溶化丝素微针的制备与研究[D]. 苏州:苏州大学,2014.
52 Yu J. Synthesis and characterization of polvglycolicacid[D]. Wuhan: Wuhan University of Technology,2006(in Chinese).
于娟. 聚羟基乙酸(PGA)的合成及性能表征[D]. 武汉:武汉理工大学,2006.
53 Wang Z Y, Zhao Y M. Polyglycolic acid biodegradable polymer[J]. Guangzhou Chem, 2004,29(1):50(in Chinese).
汪朝阳, 赵耀明. 聚乙醇酸类生物降解高分子[J]. 广州化学,2004,29(1):50.
54 Park J H, Allen M G, Prausnitz M R. Biodegradable polymer microneedles: Fabrication, mechanics and transdermal drug delivery[J]. J Controlled Release,2005,104(1):51.
55 Yu D M, Cao Y M. Absorbable polymer polyglycolic acid[J]. New Chem Mater,1996(1):17(in Chinese).
于德梅, 曹有名. 可吸收性聚合物聚乙醇酸[J]. 化工新型材料,1996(1):17.
56 Park J H, et al. Polymer microneedles for controlled-release drug delivery[J]. Pharmaceutical Res,2006,23(5):1008.
57 Kim M, Jung B, Park J H. Hydrogel swelling as a trigger to release biodegradable polymer microneedles in skin[J]. Biomaterials,2012,33(2):668.
58 Wang D G, Zhen H, Hu Y J, et al. Biocompatibility study of implantation and degradation products of polyvinyl alcohol[J]. Beijing Biomed Eng,1996(3):165(in Chinese).
王定国, 郑华, 胡颖嘉, 等. 聚乙烯醇体内植入和降解产物生物相容性研究[J]. 北京生物医学工程,1996(3):165.
59 Donnelly R F, Majithiya R, Singh T R, et al. Design, optimization and characterisation of polymeric microneedle arrays prepared by a novel laser-based micromoulding technique[J]. Pharmaceutical Res,2011,28(1):41.
60 Robinson B V, Sullivan F M, Borzelleca J F, et al. PVP, a critical review of kinetics and toxicology of polyvinylpyrrolidone (povidone)[M].Boca Raton: Crc Press,1990.
61 Feng Y. Optimization of microneedles and application in the modle drug[D]. Shanghai: Shanghai Jiao Tong University,2013(in Chinese).
冯艳. 微针的处方优化及其在模型药物中的应用[D]. 上海:上海交通大学,2013.
62 Raphael A P, Prow T W, Crichton M L, et al. Targeted, needle-free vaccinations in skin using multilayered, densely-packed dissolving microprojection arrays[J]. Small,2010,6(16):1785.
63 Donnelly R F, Mccrudden M T, Zaid Alkilani A, et al. Hydrogel-forming microneedles prepared from "super swelling" polymers combined with lyophilised wafers for transdermal drug delivery[J]. PLOS ONE,2014,9(10):e111547.
64 Wang Q Q, Ma T, Li J C, et al. The preparation of the dissolving microneedle array of macromolecular drugs through percutaneous release[J]. J Bengbu Medical College,2016,41(4):523(in Chinese).
王清清, 马涛, 李见春, 等. 应用于大分子药物经皮释药的可溶微针贴片制备[J]. 蚌埠医学院学报,2016,41(4):523.
65 Chu L Y, Choi S O, Prausnitz M R. Fabrication of dissolving polymer microneedles for controlled drug encapsulation and delivery: Bubble and pedestal microneedle designs[J]. J Pharmaceutical Sci,2010,99(10):4228.
66 Wu Z Z, et al. The fabrication and optimization of complex hyaluronic acid microneedles[J]. Prog Modern Biomed,2016,16(2):206(in Chinese).
吴造展, 尹芹, 陈丽竹, 等. 复合透明质酸微针制剂的制备及优化[J]. 现代生物医学进展, 2016,16(2):206.
67 Wu X X, Cao Y J, Gui S Y. Preparation of self-dissolving microneedles and its influence on transdermal delivery of sinomenine hydrochloride gel[J]. Anhui Medical Pharmaceutical J,2015(6):1035(in Chinese).
吴星星, 曹英骥, 桂双英. 自溶性微针的制备及其对盐酸青藤碱凝胶透皮性能的影响[J]. 安徽医药,2015(6):1035.
68 Lu Y, Mantha S N, Crowder D C, et al. Microstereolithography and characterization of poly(propylene fumarate)-based drug-loaded microneedle arrays[J]. Biofabrication,2015,7(4):045001.
69 Ke C J, Lin Y J, Hu Y C, et al. Multidrug release based on microneedle arrays filled with pH-responsive PLGA hollow microspheres[J]. Biomaterials,2012,33(20):5156.
70 Guo T, Zhang Y T, Zhao J H, et al. Application of lipid carriers combining microneedle in transdermal drug delivery[J]. J Chin Pharmaceutical Sci,2015,50(13):1085(in Chinese).
郭腾, 张永太, 赵继会, 等. 脂质载体结合微针在经皮给药中的应用[J]. 中国药学杂志, 2015,50(13):1085.
71 Fukuoka E, et al. Some physicochemical properties of glassy indomethacin[J]. Chem Pharmaceutical Bull,1986,34(10):4314.