Site-specific drug delivery systems within the gastro-intestinal tract: from the mouth to the colon.

Delivery of drugs by the oral route remains the most spread route to administer medicines to patients. The manuscript takes into consideration the most important organs of the digestive system (mouth, oesophagus, stomach, small intestine and colon), their size, physiology and transit patterns of dosage forms while travelling in the digestive tract. For each organ several strategies are considered, namely, adhesion, chemical modification of drug and/or excipient moieties, technological features of dosage forms (e.g. porosity, disintegration time), pH variations or transit times. The manuscript considers strategies that are commonly used in practice for long-term administration of drugs, without interfering with human physiology, and feasible industrially.

[1]  A. Wagstaff,et al.  Fentanyl Buccal Tablet , 2012, Drugs.

[2]  P. Minghetti,et al.  Buccoadhesive slow-release tablets of acitretin: design and `in vivo' evaluation , 1998 .

[3]  M. Salem,et al.  Mucoadhesive Dosage form of Lidocaine Hydrochloride: I. Mucoadhesive and Physicochemical Characterization , 2007, Drug development and industrial pharmacy.

[4]  P. Boesiger,et al.  Magnetic Resonance Imaging for the in Vivo Evaluation of Gastric-Retentive Tablets , 2003, Pharmaceutical Research.

[5]  J. Remon,et al.  In‐vitro Bioadhesion of a Buccal, Miconazole Slow‐release Tablet , 1993, The Journal of pharmacy and pharmacology.

[6]  J. Newton,et al.  Amylose as a coating for drug delivery to the colon: Preparation and in vitro evaluation using glucose pellets , 1996 .

[7]  Yun-jin Jung,et al.  Synthesis and Properties of Dextran–Nalidixic Acid Ester as a Colon-Specific Prodrug of Nalidixic Acid , 2001, Drug development and industrial pharmacy.

[8]  J. Jacobsen,et al.  Development and in vitro/in vivo testing of mucoadhesive buccal patches releasing benzydamine and lidocaine , 1996 .

[9]  D. Attwood,et al.  An evaluation of pectin as a carrier for drug targeting to the colon , 1993 .

[10]  Sanford Bolton,et al.  A Floating Controlled-Release Drug Delivery System: In Vitro-in Vivo Evaluation , 1993, Pharmaceutical Research.

[11]  J. Zhu,et al.  [Pharmacokinetics and pharmacodynamics of diltiazem floating tablets]. , 1992, Zhongguo yao li xue bao = Acta pharmacologica Sinica.

[12]  N. Peppas,et al.  Gastrointestinal transit and mucoadhesive characteristics of complexation hydrogels in rats. , 2006, Journal of pharmaceutical sciences.

[13]  H. Junginger,et al.  Buccal delivery of thiocolchicoside: in vitro and in vivo permeation studies. , 2003, International journal of pharmaceutics.

[14]  B. Mishra,et al.  Colon targeted delivery systems of metronidazole based on osmotic technology: development and evaluation. , 2008, Chemical & pharmaceutical bulletin.

[15]  A. Basit,et al.  An in vivo comparison of intestinal pH and bacteria as physiological trigger mechanisms for colonic targeting in man. , 2008, Journal of controlled release : official journal of the Controlled Release Society.

[16]  K. Sawant,et al.  Formulation, Characterization, and In Vitro Evaluation of Bioadhesive Gels Containing 5-Fluorouracil , 2008, Pharmaceutical development and technology.

[17]  J. Ali,et al.  Formulation and characterisation of a buccoadhesive erodible tablet for the treatment of oral lesions. , 1998, Die Pharmazie.

[18]  C. Rhodes,et al.  Development of a Novel Controlled-Release System for Gastric Retention , 1997, Pharmaceutical Research.

[19]  F. Sakr A programmable drug delivery system for oral administration. , 1999, International journal of pharmaceutics.

[20]  J. Siepmann,et al.  Floating matrix tablets based on low density foam powder: effects of formulation and processing parameters on drug release. , 2003, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[21]  Kinam Park,et al.  Gastric retention properties of superporous hydrogel composites. , 2000, Journal of controlled release : official journal of the Controlled Release Society.

[22]  Libo Yang,et al.  Colon-specific drug delivery: new approaches and in vitro/in vivo evaluation. , 2002, International journal of pharmaceutics.

[23]  A. Basit Advances in Colonic Drug Delivery , 2012, Drugs.

[24]  P. Giunchedi,et al.  Preparation, In Vitro Characterization and Preliminary In Vivo Evaluation of Buccal Polymeric Films Containing Chlorhexidine , 2008, AAPS PharmSciTech.

[25]  H. SEAGER,et al.  Drug‐delivery Products and the Zydis Fast‐dissolving Dosage Form * , 1998, The Journal of pharmacy and pharmacology.

[26]  H. Batchelor Bioadhesive Dosage Forms for Esophageal Drug Delivery , 2005, Pharmaceutical Research.

[27]  S. Bandari,et al.  Design and evaluation of polymeric coated minitablets as multiple unit gastroretentive floating drug delivery systems for furosemide. , 2009, Journal of pharmaceutical sciences.

[28]  S. Agarwal,et al.  Preparation and evaluation of bioerodible buccal tablets containing clotrimazole , 1996 .

[29]  Hoo-Kyun Choi,et al.  Preparation of buccal patch composed of carbopol, poloxamer and hydroxypropyl methylcellulose , 2003, Archives of pharmacal research.

[30]  Jason T McConville,et al.  Erosion Characteristics of an Erodible Tablet Incorporated in a Time-Delayed Capsule Device , 2005, Drug development and industrial pharmacy.

[31]  G. Fetih,et al.  Transbuccal permeation, anti-inflammatory activity and clinical efficacy of piroxicam formulated in different gels. , 2004, International journal of pharmaceutics.

[32]  S. Garg,et al.  Development and evaluation of a buccal bioadhesive system for smoking cessation therapy. , 2007, Die Pharmazie.

[33]  Jian-Hwa Guo Bioadhesive Polymer Buccal Patches for Buprenorphine Controlled Delivery: Formulation, In-vitro Adhesion and Release Properties , 1994 .

[34]  T. Vandamme,et al.  The use of polysaccharides to target drugs to the colon , 2002 .

[35]  R. Bodmeier,et al.  Floating or pulsatile drug delivery systems based on coated effervescent cores. , 1999, International journal of pharmaceutics.

[36]  O. Güven,et al.  Formulation and in Vitro–in Vivo Evaluation of Buccoadhesive Morphine Sulfate Tablets , 1994, Pharmaceutical Research.

[37]  V. Kadam,et al.  Mucoadhesive Bilayered Patches for Administration of Sumatriptan Succinate , 2008, AAPS PharmSciTech.

[38]  S. Prodduturi,et al.  Production and Characterization of Hot-Melt Extruded Films Containing Clotrimazole , 2003, Drug development and industrial pharmacy.

[39]  Kinam Park,et al.  Synthesis of superporous hydrogels: hydrogels with fast swelling and superabsorbent properties. , 1999, Journal of biomedical materials research.

[40]  A. Gazzaniga,et al.  Oral pulsatile delivery systems based on swellable hydrophilic polymers. , 2008, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[41]  C. T. Rhodes,et al.  Optimization of Sotalol Floating and Bioadhesive Extended Release Tablet Formulations , 1995 .

[42]  N. Shibata,et al.  Possibility of a patch system as a new oral delivery system. , 2003, International journal of pharmaceutics.

[43]  P. Malfertheiner,et al.  Lansoprazole Fast Disintegrating Tablet: A New Formulation for an Established Proton Pump Inhibitor , 2003, Digestion.

[44]  S. Bjerregaard,et al.  Cyclodextrin inclusion complexes of antimycotics intended to act in the oral cavity--drug supersaturation, toxicity on TR146 cells and release from a delivery system. , 1999, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[45]  B. Poli,et al.  Polyoxyethylene-poly(methacrylic acid-co-methyl methacrylate) compounds for site-specific peroral delivery. , 2000, International journal of pharmaceutics.

[46]  M. K. Chourasia,et al.  Pharmaceutical approaches to colon targeted drug delivery systems. , 2003, Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques.

[47]  L. Maggi,et al.  Formulation design and development to produce orodispersible tablets by direct compression , 2007 .

[48]  G. Bhat,et al.  The evaluation of a biodegradable dental chip containing chlorhexidine in chitosan base as a targeted drug delivery in the management of chronic periodontitis in patients , 2009 .

[49]  A. Bernkop‐Schnürch,et al.  Preparation and characterisation of thiolated poly(methacrylic acid)-starch compositions. , 2004, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[50]  B. Conway,et al.  Strategies and therapeutic opportunities for the delivery of drugs to the esophagus. , 2008, Critical reviews in therapeutic drug carrier systems.

[51]  J Kristl,et al.  Optimisation of floating matrix tablets and evaluation of their gastric residence time. , 2000, International journal of pharmaceutics.

[52]  P. Giunchedi,et al.  Formulation and in vivo evaluation of chlorhexidine buccal tablets prepared using drug-loaded chitosan microspheres. , 2002, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[53]  A. Tiwary,et al.  Mucoadhesive Microspheres for Gastroretentive Delivery of Acyclovir: In Vitro and In Vivo Evaluation , 2008, The AAPS Journal.

[54]  M. K. Chourasia,et al.  Polysaccharides for Colon Targeted Drug Delivery , 2004, Drug delivery.

[55]  P. P. Bhatt,et al.  Evaluation of a mucoadhesive buccal patch for delivery of peptides: in vitro screening of bioadhesion. , 1998, Drug development and industrial pharmacy.

[56]  Carlo Rossi,et al.  Development of mucoadhesive patches for buccal administration of ibuprofen. , 2004, Journal of controlled release : official journal of the Controlled Release Society.

[57]  F. Vrečer,et al.  Physical and technological parameters influencing floating properties of matrix tablets based on cellulose ethers , 1998 .

[58]  A. Sakr,et al.  Development and evaluation of extended release bioadhesive sodium fluoride tablets. , 2005, International journal of pharmaceutics.

[59]  C. Lehr,et al.  Lectin-mediated drug targeting: history and applications. , 2004, Advanced drug delivery reviews.

[60]  P. Fine,et al.  Fentanyl buccal tablet. , 2008, Drugs of today.

[61]  Kinam Park,et al.  Gastric retentive drug-delivery systems. , 1998, Critical reviews in therapeutic drug carrier systems.

[62]  T. Nagai,et al.  Preparation of magnetic granules containing bleomycin and its evaluation using model esophageal cancer , 1997 .

[63]  A. Hoffman,et al.  Expandable gastroretentive dosage forms. , 2003, Journal of controlled release : official journal of the Controlled Release Society.

[64]  F. Alanazi,et al.  Formulation and physicochemical characterisation of buccoadhesive films containing ketorolac , 2007 .

[65]  Javed Ali,et al.  Floating drug delivery systems: A review , 2005, AAPS PharmSciTech.

[66]  Sanjay K. Jain,et al.  Target-specific drug release to the colon , 2008, Expert opinion on drug delivery.

[67]  XueTao Jiang,et al.  Design and evaluation of a dry coated drug delivery system with floating-pulsatile release. , 2008, Journal of pharmaceutical sciences.

[68]  L. Maggi,et al.  Preparation and evaluation of release characteristics of 3TabGum, a novel chewing device. , 2005, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[69]  G. Ceschel,et al.  Design and in vitro-in vivo evaluation of a bi-layered tablet containing benzocaine for local buccal administration , 2004 .

[70]  V. Sutariya,et al.  Development and Evaluation of Fast-Dissolving Film of Salbutamol Sulphate , 2005, Drug development and industrial pharmacy.

[71]  K. Järvinen,et al.  Precipitation complexation method produces cannabidiol/beta-cyclodextrin inclusion complex suitable for sublingual administration of cannabidiol. , 2007, Journal of pharmaceutical sciences.

[72]  A. Hoffman,et al.  Mucoadhesive drug carriers based on complexes of poly(acrylic acid) and PEGylated drugs having hydrolysable PEG-anhydride-drug linkages. , 2000, Journal of controlled release : official journal of the Controlled Release Society.

[73]  R. Fedorak,et al.  Targeted delivery, safety, and efficacy of oral enteric-coated formulations of budesonide. , 2005, Advanced drug delivery reviews.

[74]  J. Siepmann,et al.  Polymer blends for controlled release coatings. , 2008, Journal of controlled release : official journal of the Controlled Release Society.

[75]  H. Frijlink,et al.  Pulsatile drug delivery to ileo-colonic segments by structured incorporation of disintegrants in pH-responsive polymer coatings. , 2008, Journal of controlled release : official journal of the Controlled Release Society.

[76]  I. Wilding,et al.  Systemic Availability of the Active Metabolite Hydroxy‐Fasudil After Administration of Fasudil to Different Sites of the Human Gastrointestinal Tract , 2007, Journal of clinical pharmacology.

[77]  G. Ponchel,et al.  The Impact of Trimethyl Chitosan on In Vitro Mucoadhesive Properties of Pectinate Beads along Different Sections of Gastrointestinal Tract , 2007, Drug development and industrial pharmacy.

[78]  J. Remon,et al.  Spray-dried Amioca starch/Carbopol 974P mixtures as buccal bioadhesive carriers. , 2005, International journal of pharmaceutics.

[79]  S. A. Sande,et al.  Development of pectin matrix tablets for colonic delivery of model drug ropivacaine. , 2000, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[80]  Alfred Liang,et al.  Fast-dissolving intraoral drug delivery systems , 2001 .

[81]  Y. Kawashima,et al.  Hollow microspheres for use as a floating controlled drug delivery system in the stomach. , 1992, Journal of pharmaceutical sciences.

[82]  Fabiana Quaglia,et al.  Cyclodextrin-containing poly(ethyleneoxide) tablets for the delivery of poorly soluble drugs: potential as buccal delivery system. , 2006, International journal of pharmaceutics.

[83]  S. Chandran,et al.  Multiparticulate formulation approach to colon specific drug delivery: current perspectives. , 2006, Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques.

[84]  J. Fell,et al.  Targeting drugs to the colon: delivery systems for oral administration. , 1994, Journal of drug targeting.

[85]  J. H. Guo,et al.  The Effects of Backing Materials and Multilayered Systems on the Characteristics of Bioadhesive Buccal Patches , 1996, The Journal of pharmacy and pharmacology.

[86]  S. Mutalik,et al.  Development of mucoadhesive buccal films for the treatment of oral sub-mucous fibrosis: a preliminary study , 2009, Pharmaceutical development and technology.

[87]  Zhirong Zhang,et al.  Synthesis and characterization of HPMC derivatives as novel duodenum-specific coating agents , 2005, Archives of pharmacal research.

[88]  W. Sawicki Pharmacokinetics of verapamil and norverapamil from controlled release floating pellets in humans. , 2002, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[89]  F. Giordano,et al.  Time-dependent oral delivery systems for colon targeting , 1995 .

[90]  S. Al-suwayeh,et al.  In vitro and in vivo evaluation of floating controlled release dosage forms of verapamil hydrochloride , 2004 .

[91]  Xiaoling Li,et al.  Sublingual drug delivery. , 2008, Critical reviews in therapeutic drug carrier systems.

[92]  A. Mitra,et al.  Evaluation of a novel, natural oligosaccharide gum as a sustained-release and mucoadhesive component of calcitonin buccal tablets. , 1999, Journal of pharmaceutical sciences.

[93]  T. Velten,et al.  Drug delivery from the oral cavity: focus on a novel mechatronic delivery device. , 2008, Drug discovery today.

[94]  Kinam Park,et al.  Synthesis of fast-swelling, superporous sucrose hydrogels. , 2000 .

[95]  A. Gazzaniga,et al.  Oral delayed-release system for colonic specific delivery☆ , 1994 .

[96]  F. Otero-Espinar,et al.  In-vitro bioadhesion of carbopol hydrogels , 1996 .

[97]  D. Craig,et al.  Feasibility of a bioadhesive drug delivery system targeted to oesophageal tissue. , 2004, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[98]  R. Spiller,et al.  Pathological influences on colonic motility: implications for drug delivery , 1991 .

[99]  Alan F. Parr,et al.  Use of the InteliSite® Capsule to Study Ranitidine Absorption from Various Sites Within the Human Intestinal Tract , 1998, Pharmaceutical Research.

[100]  F. Vauzelle-Kervroedan,et al.  Pharmacokinetic Assessment of a Fast-release Orodispersible Tramadol Tablet Compared to a Conventional Tramadol Capsule , 2004, Arzneimittelforschung.

[101]  R. Bodmeier,et al.  Pulsatile drug-delivery systems. , 2001, Critical reviews in therapeutic drug carrier systems.

[102]  J. Newton,et al.  Amylose formulations for drug delivery to the colon: a comparison of two fermentation models to assess colonic targeting performance in vitro. , 2004, International journal of pharmaceutics.

[103]  Sanjay K. Jain,et al.  Perspectives of biodegradable natural polysaccharides for site-specific drug delivery to the colon. , 2007, Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques.