Sol–gel one-pot synthesis in soft conditions of mesoporous silica materials ready for drug delivery system

The present work reveals a new and simple strategy, a one-step sol–gel procedure, to encapsulate a low water-soluble drug in silica mesostructured microparticles and to improve its release in physiological media. The synthesis of these new materials is based on the efficient solubilisation of a poorly water-soluble drug in surfactant micelles (Tween 80, a pharmaceutical excipient) which act as template for the silica network. A strict control of the sol–gel process and the parameters procedure in soft conditions (concentration, pH, temperature) was applied to reach the solubilisation limit of the drug in the micellar solution so as to optimise its encapsulation. Even if this one-pot procedure could appear limited by the low drug loading, it could provide an interesting alternative for the formulation of many recent highly active but very poorly soluble drugs.

[1]  G. Mul,et al.  Mesoporous silica material TUD-1 as a drug delivery system. , 2007, International journal of pharmaceutics.

[2]  M. Vallet‐Regí,et al.  A New Property of MCM-41: Drug Delivery System , 2001 .

[3]  G. Giammona,et al.  Mesoporous silicate as matrix for drug delivery systems of non-steroidal antinflammatory drugs , 2002 .

[4]  F. Renzo,et al.  Micelle-templated silicates as a test bed for methods of mesopore size evaluation , 1999 .

[5]  J. Devoisselle,et al.  Study of platelet behavior in vivo after endothelial stimulation with laser irradiation using fluorescence intravital videomicroscopy and PEGylated liposome staining. , 2002, Microvascular research.

[6]  J. Devoisselle,et al.  The potential of ordered mesoporous silica for the storage of drugs: the example of a pentapeptide encapsulated in a MSU-tween 80. , 2003, Chemphyschem : a European journal of chemical physics and physical chemistry.

[7]  T. Coradin,et al.  Stability of Mesoporous Oxide and Mixed Metal Oxide Materials under Biologically Relevant Conditions , 2007 .

[8]  J. Devoisselle,et al.  Inclusion of ibuprofen in mesoporous templated silica: drug loading and release property. , 2004, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[9]  Jenny Andersson,et al.  Influences of Material Characteristics on Ibuprofen Drug Loading and Release Profiles from Ordered Micro- and Mesoporous Silica Matrices , 2004 .

[10]  J. H. De Boer,et al.  Studies on Pore Systems in Catalysts , 1965 .

[11]  C. E. Efstathiou,et al.  Micellar acid-base potentiometric titrations of weak acidic and/or insoluble drugs. , 1993, Journal of pharmaceutical and biomedical analysis.

[12]  Raymond C Rowe,et al.  Handbook of Pharmaceutical Excipients , 1994 .

[13]  J. Devoisselle,et al.  Characterization of a phospholipid bilayer entrapped into non-porous silica nanospheres , 2004 .

[14]  Jean-Marie Devoisselle,et al.  Solid-State NMR Study of Ibuprofen Confined in MCM-41 Material , 2006 .

[15]  J. Devoisselle,et al.  Tuning nanophase separation and drug delivery kinetics through spray drying and self-assembly , 2010 .

[16]  J. Xiong,et al.  Solid state NMR perspective of drug-polymer solid solutions: a model system based on poly(ethylene oxide). , 2004, International journal of pharmaceutics.

[17]  J. Devoisselle,et al.  Synthesis and characterisation of ibuprofen-anchored MCM-41 silica and silica gel , 2003 .

[18]  I. Kangasniemi,et al.  In vitro evaluation of sol-gel processed spray dried silica gel microspheres as carrier in controlled drug delivery. , 2000, International journal of pharmaceutics.

[19]  E. Säilynoja,et al.  In vitro release of heparin from silica xerogels. , 2001, Biomaterials.

[20]  J. Devoisselle,et al.  Liposil, a promising composite material for drug storage and release. , 2007, Journal of controlled release : official journal of the Controlled Release Society.

[21]  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.

[22]  P. Kooyman,et al.  A new synthesis of mesoporous MSU-X silica controlled by a two-step pathway , 2000 .

[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]  R. Liu.  Water-insoluble drug formulation , 2000 .

[25]  M. Vallet‐Regí,et al.  Bioceramics and pharmaceuticals: A remarkable synergy , 2007 .

[26]  J. Broekhoff.  Studies on pore systems in catalysts: XIII. Pore distributions from the desorption branch of a nitrogen sorption isotherm in the case of cylindrical pores B. Applications , 1968 .

[27]  J. Dressman,et al.  Influence of physicochemical properties on dissolution of drugs in the gastrointestinal tract. , 1997, Advanced drug delivery reviews.

[28]  Gary Martin,et al.  Surfactant Systems: Their Chemistry, Pharmacy and Biology , 1984 .

[29]  R. Liu.  Water-Insoluble Drug Formulation, Second Edition , 2008 .

[30]  K. Unger,et al.  The use of porous and surface modified silicas as drug delivery and stabilizing agents , 1983 .