Encapsulation of complementary model drugs in spray-dried nanostructured materials

Two model drugs of different physico-chemical and pharmaceutical properties (ibuprofen, acetaminophen) have been incorporated together or separately in silica-based microspheres using sol–gel and spray-drying processes. A variable amount of a neutral surfactant Brij-56© has also been added. The properties of the microspheres vary significantly depending on their composition. Three kinds of texture are identified: (1) silica containing spheroid nano-domains (formed by ibuprofen; diameters between 20 and 100 nm), (2) silica containing worm-like mesophases (formed by Brij-56© and both model drugs, typical correlation distances ~6 nm), (3) silica intimately mixed with the drug (acetaminophen) without visible phase-separation. The kinetics of drug release in simulated intestinal fluid strongly depend on these textures. The association of ibuprofen and acetaminophen in a single type of microsphere and without surfactant favours a concomitant release. Possible mechanisms of materials’ formation are discussed.

[1]  Keith Masters,et al.  Spray drying handbook , 1979 .

[2]  C. Brinker.  Sol-gel science , 1990 .

[3]  Yunfeng Lu,et al.  Aerosol-assisted self-assembly of mesostructured spherical nanoparticles , 1999, Nature.

[4]  D. Massiot,et al.  Morphological and textural control of spray-dried mesoporous silica-based spheresElectronic supplementary information (ESI) available: XRD patterns; 1H solid state NMR. See http://www.rsc.org/suppdata/jm/b4/b403201b/ , 2004 .

[5]  S. Lyonnard,et al.  Role of Interparticle Potential in Controlling the Morphology of Spray-Dried Powders from Aqueous Nanoparticle Sols , 2002 .

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

[7]  Yunfeng Lu,et al.  Evaporation-Induced Self-Assembly: Nanostructures Made Easy** , 1999 .

[8]  Peter York,et al.  The use of solubility parameters in pharmaceutical dosage form design , 1997 .

[9]  Chang Hyun Ko,et al.  Disordered molecular sieve with branched mesoporous channel network , 1996 .

[10]  Reinhard Vehring,et al.  Pharmaceutical Particle Engineering via Spray Drying , 2007, Pharmaceutical Research.

[11]  David Grosso,et al.  Aerosol Route to Functional Nanostructured Inorganic and Hybrid Porous Materials , 2011, Advanced materials.

[12]  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.

[13]  Xiangrong Song,et al.  Reversion of multidrug resistance by co-encapsulation of vincristine and verapamil in PLGA nanoparticles. , 2009, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[14]  K. Kosmidis,et al.  On the use of the Weibull function for the discernment of drug release mechanisms. , 2006, International journal of pharmaceutics.

[15]  F Langenbucher,et al.  Letters to the Editor: Linearization of dissolution rate curves by the Weibull distribution , 1972, The Journal of pharmacy and pharmacology.

[16]  M. Abdullah,et al.  Preparation of functional nanostructured particles by spray drying , 2006 .

[17]  C. Brinker,et al.  Sol-Gel Science: The Physics and Chemistry of Sol-Gel Processing , 1990 .

[18]  Chi-Hwa Wang,et al.  Mathematical modeling and simulation of drug release from microspheres: Implications to drug delivery systems. , 2006, Advanced drug delivery reviews.

[19]  P. Hildgen,et al.  Characteristics and properties of nanospheres co-loaded with lipophilic and hydrophilic drug models. , 2009, International journal of pharmaceutics.

[20]  A. Datye,et al.  Hexagonal Mesostructure in Powders Produced by Evaporation-Induced Self-Assembly of Aerosols from Aqueous Tetraethoxysilane Solutions , 2003 .

[21]  D. Durand,et al.  New insights into the formation of textures through spray-drying and self-assembly , 2007 .

[22]  C. Sanchez,et al.  Aerosol generated mesoporous silica particles , 2003 .

[23]  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.

[24]  Jun Liu,et al.  Mesoporous Silica Synthesized by Solvent Evaporation: Spun Fibers and Spray-Dried Hollow Spheres , 1997 .

[25]  J. Devoisselle,et al.  Drug nano-domains in spray-dried ibuprofen-silica microspheres. , 2012, Physical chemistry chemical physics : PCCP.