Control-release microcapsule of famotidine loaded biomimetic synthesized mesoporous silica nanoparticles: Controlled release effect and enhanced stomach adhesion in vitro.

In the present work, control-release microcapsule of famotidine (FMT) loaded biomimetic synthesized mesoporous silica nanoparticles (B-MSNs) was developed, and controlled release effect and stomach adhesion of this formulation in vitro were mainly investigated. B-MSN was previously synthesized and it was amorphous mesoporous nanoparticles with helical channels. Cytotoxicity of B-MSN was studied using human breast cancer cells (MCF-7) and the result indicated that cytotoxicity of B-MSN can be neglected. After loading FMT into B-MSN, specific surface area, pore volume and pore diameter of B-MSN were obviously reduced. In vitro dissolution test showed that B-MSN had the ability to slow down FMT release for 15 min. In order to prolong controlled release effect and remained the advantage of B-MSN (improve drug stability due to its rigid silica framework), the combined application of control-release microcapsule (using cellulose and hydroxypropyl methylcellulose K15M as excipients) with B-MSN was designed. It was obvious that newly designed formulation significantly controlled FMT release with Fickian diffusion mechanism and showed enhanced stomach adhesion in vitro, which has significant value in widening the application of B-MSN in formulation design.

[1]  G. G. Stokes.  "J." , 1890, The New Yale Book of Quotations.

[2]  S. Che,et al.  Synthesis of amino group functionalized monodispersed mesoporous silica nanospheres using anionic surfactant , 2011 .

[3]  Siling Wang,et al.  Incorporation of indomethacin nanoparticles into 3-D ordered macroporous silica for enhanced dissolution and reduced gastric irritancy. , 2011, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[4]  E. Fattal,et al.  Alpha-cyclodextrin/oil beads as a new carrier for improving the oral bioavailability of lipophilic drugs. , 2007, Journal of controlled release : official journal of the Controlled Release Society.

[5]  V. Crocellà,et al.  Controlled release of metoprolol tartrate from nanoporous silica matrices , 2010 .

[6]  O. Terasaki,et al.  Molecular design of the surfactant and the co-structure-directing agent (CSDA) toward rational synthesis of targeted anionic surfactant templated mesoporous silica , 2007 .

[7]  Jianfeng Chen,et al.  Preparation and characterization of porous hollow silica nanoparticles for drug delivery application. , 2004, Biomaterials.

[8]  O. Terasaki,et al.  Carboxylic group functionalized ordered mesoporous silicas , 2011 .

[9]  P. Costa,et al.  Modeling and comparison of dissolution profiles. , 2001, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[10]  M. Kruk,et al.  Synthesis of Ultra-Large-Pore SBA-15 Silica with Two-Dimensional Hexagonal Structure Using Triisopropylbenzene As Micelle Expander , 2009 .

[11]  Qinfu Zhao,et al.  3D cubic mesoporous silica microsphere as a carrier for poorly soluble drug carvedilol , 2012 .

[12]  S. Che,et al.  Chiral mesoporous silica: chiral construction and imprinting via cooperative self-assembly of amphiphiles and silica precursors. , 2011, Chemical Society reviews.

[13]  Hongzhuo Liu,et al.  Biomimetic synthesized nanoporous silica@poly(ethyleneimine)s xerogel as drug carrier: characteristics and controlled release effect. , 2014, International journal of pharmaceutics.

[14]  Chaobo Xiao,et al.  ph-sensitive cationic guar gum/poly (acrylic acid) polyelectrolyte hydrogels: Swelling and in vitro drug release , 2007 .

[15]  Hsing-Wen Sung,et al.  In vivo evaluation of safety and efficacy of self-assembled nanoparticles for oral insulin delivery. , 2009, Biomaterials.

[16]  W. Pan,et al.  Biomimetic synthesized chiral mesoporous silica: Structures and controlled release functions as drug carrier. , 2015, Materials science & engineering. C, Materials for biological applications.

[17]  J. Koenderink.  Q… , 2014, Les noms officiels des communes de Wallonie, de Bruxelles-Capitale et de la communaute germanophone.

[18]  San-Yuan Chen,et al.  Nano-ferrosponges for controlled drug release. , 2007, Journal of controlled release : official journal of the Controlled Release Society.

[19]  Siling Wang,et al.  Folate-polyethyleneimine functionalized mesoporous carbon nanoparticles for enhancing oral bioavailability of paclitaxel. , 2015, International journal of pharmaceutics.

[20]  N. Peppas,et al.  Drug transport mechanisms and release kinetics from molecularly designed poly(acrylic acid-g-ethylene glycol) hydrogels. , 2006, Biomaterials.

[21]  Jing Wang,et al.  Facile synthesis of 3D cubic mesoporous silica microspheres with a controllable pore size and their application for improved delivery of a water-insoluble drug. , 2011, Journal of colloid and interface science.

[22]  Juan L. Vivero-Escoto,et al.  Mesoporous silica nanoparticles as controlled release drug delivery and gene transfection carriers. , 2008, Advanced drug delivery reviews.

[23]  I. Kangasniemi,et al.  Silica xerogel as an implantable carrier for controlled drug delivery--evaluation of drug distribution and tissue effects after implantation. , 2000, Biomaterials.

[24]  Yikun Gao,et al.  Exploitation of 3D face-centered cubic mesoporous silica as a carrier for a poorly water soluble drug: influence of pore size on release rate. , 2014, Materials science & engineering. C, Materials for biological applications.

[25]  Cecilia Sahlgren,et al.  Mesoporous silica nanoparticles in medicine--recent advances. , 2013, Advanced drug delivery reviews.

[26]  M. Vallet‐Regí,et al.  Influence of pore size of MCM-41 matrices on drug delivery rate , 2004 .

[27]  F. Hirayama,et al.  Evaluation of carboxymethyl-beta-cyclodextrin with acid function: improvement of chemical stability, oral bioavailability and bitter taste of famotidine. , 2010, International journal of pharmaceutics.

[28]  N. Najib,et al.  Characterization of famotidine polymorphic forms , 1997 .