NMR imaging of chitosan and carboxymethyl starch tablets: swelling and hydration of the polyelectrolyte complex.

The hydration and swelling properties of the tablets made of chitosan, carboxymethyl starch, and a polyelectrolyte complex of these two polysaccharides have been studied by NMR imaging. We studied the effect of pH and ionic strength on the swelling of the tablets and on the diffusion of fluid into the tablets in water and simulated physiological fluids. The pH value of the fluids exerts a more significant effect than their ionic strengths on the swelling of the tablets. The tablets are compared also with those made of cross-linked high amylose starch. The formation of complex helps to keep the integrity of the tablets in various media and render a slow and restricted swelling similar to that of the tablets of the cross-linked high amylase starch, which is significantly lower than the swelling of chitosan and of carboxymethyl starch. The capacities to modulate the release rate of drugs in different media are discussed by comparing the matrices and evaluating the preparation process of the complex. A sustained release of less soluble drugs such as aspirin in gastrointestinal fluids can be provided by the complex, due to the ionic interaction and hydrogen bonding between the drug and the biopolymer complex.

[1]  B. Luppi,et al.  Chitosan/pectin polyelectrolyte complexes: selection of suitable preparative conditions for colon-specific delivery of vancomycin. , 2008, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[2]  M. Mateescu,et al.  Carboxymethyl high amylose starch (CM-HAS) as excipient for Escherichia coli oral formulations. , 2005, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[3]  P. Dewick Essentials of Organic Chemistry: For Students of Pharmacy, Medicinal Chemistry and Biological Chemistry , 2006 .

[4]  H. Pörtner,et al.  Simultaneous observations of haemolymph flow and ventilation in marine spider crabs at different temperatures: a flow weighted MRI study. , 2001, Magnetic resonance imaging.

[5]  Robert Gurny,et al.  Structure and interactions in chitosan hydrogels formed by complexation or aggregation for biomedical applications. , 2004, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[6]  A. Domb,et al.  Chitosan chemistry and pharmaceutical perspectives. , 2004, Chemical reviews.

[7]  Xiao Xia Zhu,et al.  NMR imaging of high-amylose starch tablets. 2. Effect of tablet size. , 2002, Biomacromolecules.

[8]  S. Baumgartner,et al.  Quantitative evaluation of polymer concentration profile during swelling of hydrophilic matrix tablets using 1H NMR and MRI methods. , 2005, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[9]  Kshirsagar Drug delivery systems , 2000 .

[10]  C. Fyfe,et al.  Investigation of Hydrogel Formation from Hydroxypropylmethylcellulose (HPMC) by NMR Spectroscopy and NMR Imaging Techniques , 1997 .

[11]  M. Mateescu,et al.  The influence of protonation ratio on properties of carboxymethyl starch excipient at various substitution degrees: Structural insights and drug release kinetics. , 2010, International journal of pharmaceutics.

[12]  X. Zhu,et al.  NMR spectroscopy and imaging studies of pharmaceutical tablets made of starch , 2009 .

[13]  Y Wang,et al.  Chitosan-DNA nanoparticles as gene carriers: synthesis, characterization and transfection efficiency. , 2001, Journal of controlled release : official journal of the Controlled Release Society.

[14]  V. Lenaerts,et al.  Cross-linked high amylose starch derivatives as matrices for controlled release of high drug loadings. , 2001, Journal of controlled release : official journal of the Controlled Release Society.

[15]  R. Marchessault,et al.  Membrane formation and drug loading effects in high amylose starch tablets studied by NMR imaging. , 2008, Biomacromolecules.

[16]  M. Mateescu,et al.  Carboxymethyl high amylose starch for F4 fimbriae gastro-resistant oral formulation. , 2007, International journal of pharmaceutics.

[17]  Hoo-Kyun Choi,et al.  Preparation of an extended-release matrix tablet using chitosan/Carbopol interpolymer complex. , 2008, International journal of pharmaceutics.

[18]  J. Swarbrick,et al.  Encyclopedia of Pharmaceutical Technology , 2006 .

[19]  D. Wong Mechanism and Theory in Food Chemistry , 1989 .

[20]  M. Mateescu,et al.  Carboxymethyl high amylose starch: Chitosan self-stabilized matrix for probiotic colon delivery. , 2008, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[21]  Karsten Mäder,et al.  Pharmaceutical applications of magnetic resonance imaging (MRI). , 2005, Advanced drug delivery reviews.

[22]  M. Mateescu,et al.  Cross-linked high amylose starch derivatives for drug release. II. Swelling properties and mechanistic study. , 2004, International journal of pharmaceutics.

[23]  Yu Juan Wang,et al.  Polyelectrolyte complex of carboxymethyl starch and chitosan as drug carrier for oral administration , 2011 .

[24]  C. Goodman United States Pharmacopeial Convention , 1988 .

[25]  K. Jain,et al.  Drug delivery systems - an overview. , 2008, Methods in molecular biology.

[26]  Xiao Xia Zhu,et al.  NMR imaging of high-amylose starch tablets. 1. Swelling and water uptake. , 2002, Biomacromolecules.

[27]  Miqin Zhang,et al.  Chitosan-based hydrogels for controlled, localized drug delivery. , 2010, Advanced drug delivery reviews.

[28]  Wei Zhang,et al.  The synergetic bone-forming effects of combinations of growth factors expressed by adenovirus vectors on chitosan/collagen scaffolds. , 2009, Journal of controlled release : official journal of the Controlled Release Society.

[29]  J. Hadgraft,et al.  Modified-Release Drug Delivery Technology , 2002 .

[30]  X. Zhu,et al.  NMR imaging study of cross-linked high-amylose starch tablets — The effect of drug loading , 2010 .

[31]  I. C. Sinka,et al.  NMR imaging of density distributions in tablets. , 2006, International journal of pharmaceutics.

[32]  M. Mateescu,et al.  Influence of Drying Procedure and of Low Degree of Substitution on the Structural and Drug Release Properties of Carboxymethyl Starch , 2010, AAPS PharmSciTech.

[33]  Xiao Xia Zhu,et al.  Imaging of high-amylose starch tablets. 3. Initial diffusion and temperature effects. , 2005, Biomacromolecules.

[34]  G. Kaur,et al.  Colon Delivery of Budesonide: Evaluation of Chitosan–Chondroitin Sulfate Interpolymer Complex , 2010, AAPS PharmSciTech.

[35]  L. Cartilier,et al.  Cross-linked amylose as matrix for drug controlled release. X-ray and FT-IR structural analysis , 1998 .

[36]  H. Pörtner,et al.  In vivo MR spectroscopy and MR imaging on non-anaesthetized marine fish: techniques and first results. , 2002, Magnetic resonance imaging.

[37]  Gautam Sen,et al.  A Novel Polymeric Biomaterial Based on Carboxymethylstarch and its Application in Controlled Drug Release , 2009 .