CIESC Journal ›› 2013, Vol. 64 ›› Issue (1): 210-222.doi: 10.3969/j.issn.0438-1157.2013.01.023

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Oral colon-specific drug delivery system and its preparation

WU Qingxi, YAO Shanjing   

  1. Key Laboratory of Biomass Chemical Engineering of Ministry of Education, Department of Chemical and Biological Engineering, Zhejiang University, Hangzhou 310027, Zhejiang, China
  • Received:2012-04-26 Revised:2012-07-25 Online:2013-01-05
  • Supported by:

    supported by the National Natural Science Foundation of China (21036005) and the Key Doctoral Program of Special Fund of Higher Education of China (20110101130007).

Abstract: As the development and application of the fourth generation's drug dosage form, the oral colon-specific drug delivery system has the advantage of targeting orientation, increasing local drug concentration, acting on the lesion site directly, reducing drug dosage and side effect, etc.Aiming at the drug releasing mechanism, application and preparation technique, the research progress of this field is reviewed, so as to provide the theoretical basis and reference for the systematic research of the oral colon-specific drug delivery system.

Key words: colon-specific, drug delivery system, application, preparation

CLC Number: 

  • Q819
[1] Pinto J F.Site-specific drug delivery systems within the gastro-intestinal tract:from the mouth to the colon[J].International Journal of Pharmaceutics, 2010,395(1/2):44-52
[2] Jain S K, Jain A.Target-specific drug release to the colon[J].Expert Opinion on Drug Delivery, 2008,5(5):483-498
[3] Ratna V, Prabakaran L, Prushothaman M.Colon targeted drug delivery system—an overview[EB/OL].http://www.pharmainfo.net/reviews/colon-targeted-drug-delivery- system-overview
[4] Abraham C, Cho J H.Mechanisms of disease inflammatory bowel disease[J].New England Journal of Medicine, 2009,361(21):2066-2078
[5] Abraham C, Medzhitov R.Interactions between the host innate immune system and microbes in inflammatory bowel disease[J].Gastroenterology,2011,140(6):1729-1737
[6] Jung Y J, Kim Y M.What should be considered on design of a colon-specific prodrug?[J].Expert Opinion on Drug Delivery, 2010,7(2):245-258
[7] Kles K A, Vavricka S R, Turner J R, Musch M W, Hanauer S B, Chang E B.Comparative analysis of the in vitro prosecretory effects of balsalazide, sulfasalazine, olsalazine, and mesalamine in rabbit distal ileum[J].Inflammatory Bowel Diseases, 2005,11(3):253-257
[8] Friend D R, Chang G W.A colon-specific drug-delivery system based on drug glycosides and the glycosidases of colonic bacteria[J].Journal of Medicinal Chemistry, 1984,27(3):261-266
[9] Leopold C S, Friend D R.In vitro study drug for the assessment of poly(L-aspartic acid)as a drug carrier for colon-specific drug delivery[J].International Journal of Pharmaceutics, 1995,126(1/2):139-145
[10] Cui N, Friend D R, Fedorak R N.A budesonide prodrug accelerates treatment of colitis in rats[J].Gut., 1994,35(10):1439-1446
[11] Lee Y, Kim I H, Kim J, Yoon J H, Shin Y H, Jung Y, Kim Y M.Evaluation of dextran-flufenamic acid ester as a polymeric colon-specific prodrug of flufenamic acid, an anti-inflammatory drug, for chronotherapy[J].Journal of Drug Targeting, 2011,19(5):336-343
[12] Couto D, Ribeiro D, Freitas M, Gomes A, Lima J, Fernandes E.Scavenging of reactive oxygen and nitrogen species by the prodrug sulfasalazine and its metabolites 5-aminosalicylic acid and sulfapyridine[J].Redox Report, 2010,15(6):259-267
[13] Rajguru V V, Gaikwad P D, Bankar V H, Pawar S P.An overview on colonic drug delivery system[J].International Journal of Pharmaceutical Science Review and Research, 2011,2(6):197-204
[14] Ardusso M S, Manzo R H, Jimenez-Kairuz A F. Comparative study of three structurally related acid polyelectrolytes as carriers of basic drugs:carbomer, Eudragit l-100 and s-100[J].Supramolecular Chemistry, 2010,22(5):289-296
[15] Parakkal D, Thorpe M, Paver S, Ehrenpreis E, Hannon B. A comparison of dynamic systems models of gastrointestinal kinetics of controlled release multimatrix system 5-aminosalicylic acid(5-asa), lialda(tm)with pH-dependent, delayed release 5-asa(asacol(tm))[J].American Journal of Gastroenterology, 2010,105:S475
[16] Gao C S, Huang J, Jiao Y, Shan L, Liu Y, Li Y, Mei X G. In vitro release and in vivo absorption in beagle dogs of meloxicam from Eudragit(r)fs 30 d-coated pellets[J].International Journal of Pharmaceutics, 2006,322(1/2):104-112
[17] Malchow H, Gertz B.A new mesalazine foam enema(claversal foam)compared with a standard liquid enema in patients with active distal ulcerative colitis[J].Alimentary Pharmacology & Therapeutics, 2002,16(3):415-423
[18] Muzzalupo R, Tavano L, Cassano R, Trombino S, Cilea A, Picci N.Colon-specific devices based on methacrylic functionalized tween monomer networks:swelling studies and in vitro drug release[J].European Polymer Journal, 2010,46(2):209-216
[19] Kovacic B, Vrecer F, Planinsek O.Design of a drug delivery system with bimodal pH dependent release of a poorly soluble drug[J].Pharmazie, 2011,66(6):465-466
[20] Liu Hui(刘辉), Pan Weisan(潘卫三).The research progress of oral colon-specific drug delivery system[J].China Pharmacist(中国药师), 2008,11(2):167-169
[21] Wu B J, Shun N Y, Wei X L, Wu W.Characterization of 5-fluorouracil release from hydroxypropylmethylcellulose compression-coated tablets[J].Pharmaceutical Development and Technology, 2007,12(2):203-210
[22] Qi Meiling(齐美玲), Wang Peng(王鹏), Wu Dezheng(吴德政).Preparation of colonic delivery system for tinidazole[J].Chinese Journal of Pharmaceuticals(中国医药工业杂志), 2003,34(4):172-175
[23] Kshirsagar S J, Bhalekar M R.Design, development and in vitro-in vivo study of colon specific fast disintegrating tablet based on time dependent approach[J].Latin American Journal of Pharmacy, 2011,30(5):890-895
[24] Pedersen P J, Adolph S K, Subramanian A K, Arouri A, Andresen T L, Mouritsen O G, Madsen R, Madsen M W, Peters G H, Clausen M H.Liposomal formulation of retinoids designed for enzyme triggered release[J].Journal of Medicinal Chemistry, 2010,53(9):3782-3792
[25] Saffran M, Kumar G S, Savariar C, Burnham J C, Williams F, Neckers D C.A new approach to the oral-administration of insulin and other peptide drugs[J].Science, 1986,233(4768):1081-1084
[26] Sinha V R, Kumria R.Polysaccharide matrices for microbially triggered drug delivery to the colon[J].Drug Development and Industrial Pharmacy, 2004,30(2):143-150
[27] Wilson P J, Basit A W.Exploiting gastrointestinal bacteria to target drugs to the colon:an in vitro study using amylose coated tablets[J].International Journal of Pharmaceutics, 2005,300(1/2):89-94
[28] He W, Du Q, Cao D Y, Xiang B, Fan L F.Study on colon-specific pectin/ethylcellulose film-coated 5-fluorouracil pellets in rats[J].International Journal of Pharmaceutics, 2008,348(1/2):35-45
[29] Freire C, Podczeck F, Veiga F, Sousa J.Influence of the coating formulation on enzymatic digestibility and drug release from 5-aminosalicylic acid pellets coated with mixtures of high-amylose starch and surelease(r)intended for colon-specific drug delivery[J].Drug Development and Industrial Pharmacy, 2010,36(2):161-172
[30] Patel M M, Amin A F.Recent trends in microbially and/or enzymatically driven colon-specific drug delivery systems[J].Critical Reviews in Therapeutic Drug Carrier Systems, 2011,28(6):489-552
[31] Hu Z P, Mawatari S, Shimokawa T, Kimura G, Yoshikawa Y, Shibata N, Takada K.Colon delivery efficiencies of intestinal pressure-controlled colon delivery capsules prepared by a coating machine in human subjects[J].Journal of Pharmacy and Pharmacology, 2000,52(10):1187-1193
[32] Barakat N S, Al-Suwayeh S A, Taha E I, Yassin A.A new pressure-controlled colon delivery capsule for chronotherapeutic treatment of nocturnal asthma[J].Journal of Drug Targeting, 2011,19(5):365-372
[33] Elzatahry A A, Eldin M, Soliman E A, Hassan E A. Evaluation of alginate-chitosan bioadhesive beads as a drug delivery system for the controlled release of theophylline[J].Journal of Applied Polymer Science, 2009,111(5):2452-2459
[34] Rubinstein A, Tirosh B.Mucus gel thickness and turnover in the gastrointestinal-tract of the rat - response to cholinergic stimulus and implication for mucoadhesion[J].Pharmaceutical Research, 1994,11(6):794-799
[35] Sakhalkar H S, Hanes J, Fu J, Benavides U, Malgor R, Borruso C L, Kohn L D, Kujiaka D T, Goetz D J.Enhanced adhesion of ligand-conjugated biodegradable particles to colitic venules[J].Faseb Journal, 2005,19(3):792
[36] Li Zhongkun(李仲昆), Zou Heling(邹禾苓), Wang Heng(王珩), Jin Mei(靳梅), Li Bing(李冰).The preparation of cimetidine capsules for colon site-specific bioadhesive drug delivery system[J].Chinese Journal of Hospital Pharmacy(中国医院药学杂志), 2002,22(12):758-759
[37] Mahajan N, Sakarkar D, Manmode A, Pathak V, Ingole R, Dewade D.Biodegradable nanoparticles for targeted delivery in treatment of ulcerative colitis[J].Advanced Science Letters, 2011,4(2):349-356
[38] Rao S S, Ritschel W A.Development and in vitro/in vivo evaluation of a colonic release capsule of vasopressin[J].International Journal of Pharmaceutics,1992,86(1):35-41
[39] Semde R, Amighi K, Devleeschouwer M J, Moes A J.Studies of pectin hm/Eudragit(r)rl/Eudragit(r)ne film-coating formulations intended for colonic drug delivery[J].International Journal of Pharmaceutics, 2000,197(1-2):181-192
[40] Bott C, Rudolph M W, Schneider A R J, Schirrmacher S, Skalsky B, Petereit H U, Langguth P, Dressman J B, Stein J.In vivo evaluation of a novel pH- and time-based multiunit colonic drug delivery system[J].Aliment Pharmcol Ther., 2004,20(3):347-353
[41] Krishnamachari Y, Madan P, Lin S S.Development of pH- and time-dependent oral microparticles to optimize budesonide delivery to ileum and colon[J].International Journal of Pharmaceutics, 2007,338(1/2):238-247
[42] Chickpetty M S, Baswaraj R, Kumar G S.Development of novel combined time and pH-dependent based drug delivery systems for targeting 5-fluorouracil to the colon[J].Current Drug Delivery, 2011,8(5):566-574
[43] Jose S, Prema M T, Chacko A J, Thomas A C, Souto E B. Colon specific chitosan microspheres for chronotherapy of chronic stable angina[J].Colloids and Surfaces B-Biointerfaces, 2011,83(2):277-283
[44] Nunthanid J, Huanbutta K, Luangtana-Anan M, Sriamornsak P, Limmatvapirat S, Puttipipatkhachorn S. Development of time-, pH-, and enzyme-controlled colonic drug delivery using spray-dried chitosan acetate and hydroxypropyl methylcellulose[J].European Journal of Pharmaceutics and Biopharmaceutics, 2008,68(2):253-259
[45] Makhof A, Tozuka Y, Takeuchi H.pH-sensitive nanospheres for colon-specific drug delivery in experimentally induced colitis rat model[J].European Journal of Pharmaceutics and Biopharmaceutics, 2009,72(1):1-8
[46] Del Curto M D, Maroni A, Palugan L, Zema L, Gazzaniga A, Sangalli M E.Oral delivery system for two-pulse colonic release of protein drugs and protease inhibitor/absorption enhancer compounds[J].Journal of Pharmaceutical Sciences, 2011,100(8):3251-3259
[47] Bolourchian N, Dadashzadeh S.pH-independent release of propranolol hydrochloride from hpmc-based matrices using organic acids[J].Drug-Journal of Faculty of Pharmacy, 2008,16(3):136-142
[48] Nakase H, Okazaki K, Tabata Y, Uose S, Ohana M, Uchida K, Matsushima Y, Kawanami C, Oshima C, Ikada Y, Chiba T.Development of an oral drug delivery system targeting immune-regulating cells in experimental inflammatory bowel disease:a new therapeutic strategy[J].Journal of Pharmacology and Experimental Therapeutics, 2000,292(1):15-21
[49] Kong H, Kim H, Do H, Lee Y, Hong S, Yoon J H, Jung Y, Kim Y M.Structural effects of n-aromatic acyl-amino acid conjugates on their deconjugation in the cecal contents of rats:implication in design of a colon-specific prodrug with controlled conversion rate at the target site[J].Biopharmaceutics & Drug Disposition, 2011,32(6):343-354
[50] Udo K, Hokonohara K, Motoyama K, Arima H, Hirayama F, Uekama K.5-fluorouracil acetic acid/beta-cyclodextrin conjugates:drug release behavior in enzymatic and rat cecal media[J].International Journal of Pharmaceutics, 2010,388(1/2):95-100
[51] Lustrik M, Dreu R, Sibanc R, Srcic S.Comparative study of the uniformity of coating thickness of pellets coated with a conventional Wurster chamber and a swirl generator-equipped Wurster chamber[J].Pharmaceutical Development and Technology, 2012,17(3):268-276
[52] Zhou Jin(周进), Huang Weixing(黄卫星), Guan Yihao(官益豪), He Juanjuan(何娟娟).The applied research and equipment development of centrifugal fluidized bed[J].Chemical Equipment Technology(化工装备技术), 2005,26(2):5-9
[53] Sahni E, Chaudhuri B.Experimental and modeling approaches in characterizing coating uniformity in a pan coater:a literature review[J].Pharmaceutical Development and Technology, 2012,17(2):134-147
[54] Nukala R K, Boyapally H, Slipper I J, Mendham A P, Douroumis D.The application of electrostatic dry powder deposition technology to coat drug-eluting stents[J].Pharmaceutical Research, 2010,27(1):72-81
[55] Dixit R, Puthli S.Fluidization technologies:aerodynamic principles and process engineering[J].Journal of Pharmaceutical Sciences, 2009,98(11):3933-3960
[56] Xie Yuliang(谢瑜亮), Wang Mingjun(王明君), Yao Shanjing(姚善泾).Layer-by-layer self-assembly complex membrane composed of sodium cellulose sulfate-chitosan[J].Journal of Chemical Industry and Engineering(China)(化工学报), 2008,59(11):2910-2915
[57] Li Mingming(李鸣明), Yao Shanjing(姚善泾).Preparation and static contact angle measurement of NaCS/PDMDAAC polyelectrolyte complex membranes[J].CIESC Journal(化工学报), 2009,60(3):654-659
[58] Wang M, Xie Y, Zheng Q, Yao S.A novel, potential microflora-activated carrier for a colon-specific drug delivery system and its characteristics[J].Industrial & Engineering Chemistry Research, 2009,48(11):5276-5284
[59] Yu C Y, Yin B C, Zhang W, Cheng S X, Zhang X Z, Zhuo R X.Composite microparticle drug delivery systems based on chitosan, alginate and pectin with improved pH-sensitive drug release property[J].Colloids and Surfaces B-Biointerfaces, 2009,68(2):245-249
[60] Sierra-Pallares J, Marchisio D L, Parra-Santos M T, Garcia-Serna J, Castro F, Cocero M J.A computational fluid dynamics study of supercritical antisolvent precipitation:mixing effects on particle size[J].AIChE Journal, 2012,58(2):385-398
[61] Akamatsu K, Ikeuchi Y, Nakao A, Nakao S.Size-controlled and monodisperse enzyme-encapsulated chitosan microspheres developed by the SPG membrane emulsification technique[J].Journal of Colloid and Interface Science, 2012,371:46-51
[62] Xie Y, Wang M, Yao S.Preparation and characterization of biocompatible microcapsules of sodium cellulose sulfate/chitosan by means of layer-by-layer self-assembly[J].Langmuir,2009,25(16):8999-9005
[63] Kobayashi I, Vladisavljevic G T, Uemura K, Nakajima M.CFD analysis of microchannel emulsification:droplet generation process and size effect of asymmetric straight flow-through microchannels[J].Chemical Engineering Science,2011,66(22):5556-5565
[64] Zhu Liying(朱丽英).Study on colon-specific drug delivery carrier based on chitosan and sodium cellulose sulfate[D].Hangzhou:Zhejiang University, 2011
[65] Zhu L, Lin D, Yao S.Biodegradation of polyelectrolyte complex films composed of chitosan and sodium cellulose sulfate as the controllable release carrier[J].Carbohydrate Polymers, 2010,82(2):323-328
[66] Chen H L, Wu J, Sun M, Guo C Y, Yu A H, Cao F L, Zhao L Y, Tan Q, Zhai G X.N-trimethyl chitosan chloride-coated liposomes for the oral delivery of curcumin[J].Journal of Liposome Research, 2012,22(2):100-109
[67] Subhabrota M, Souvik R, Subhadeep C.Preparation and gamma scintigraphic evaluation of colon specific pellets of ketoprofen prepared by powder layering technology[J].Daru-Journal of Pharmaceutical Sciences, 2011,19(1):47-56
[68] Shah N, Shah T, Amin A.Polysaccharides:a targeting strategy for colonic drug delivery[J].Expert Opinion on Drug Delivery, 2011,8(6):779-796
[69] Krishnaiah Y, Seetha D A, Nageswara R L, Reddy P, Karthikeyan R S, Satyanarayana V.Guar gum as a carrier for colon specific delivery:influence of metronidazole and tinidazole on in vitro release of albendazole from guar gum matrix tablets[J].Journal of Pharmacy and Pharmaceutical Sciences, 2001, 4(3):235-243
[70] Yadav V J, Ahad H A, Sreeramulu J, Himabindu V. Fabrication and comparative evaluation of glipizide, aloe barbadensis miller mucilage, guar gum and ispaghula husk-based controlled release matrix tablets[J].Indian Journal of Pharmaceutical Sciences, 2009,71(2):166
[71] Salunkhe K S, Kulkarni M V.Formulation and in-vitro evaluation of dextrin matrix tablet of ibuprofen for colon specific drug delivery[J].Pakistan Journal of Pharmaceutical Sciences, 2008,21(1):17-20
[72] Amrutkar J R, Gattani S G.Chitosan-chondroitin sulfate based matrix tablets for colon specific delivery of indomethacin[J].AAPS PharmSciTech, 2009,10(2):670-677
[73] Di Pretoro G, Zema L, Palugan L, Wilson D I, Rough S L, Gazzaniga A.Optimisation and scale-up of a highly-loaded 5-asa multi-particulate dosage form using a factorial approach[J].European Journal of Pharmaceutical Sciences, 2012,45(1/2):158-168
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