Controlled release of Captopril by regulating the pore size and morphology of ordered mesoporous silica

Abstract In order to control the release of water-soluble drug Captopril (CapH 2 ), a series of mesoporous silica materials has been prepared, using three kinds of surfactants C16TAB, C12TAB, and EO 20 PO 70 EO 20 , respectively. It has been found that the loading amount of the drug was related to the BET surface area of the mesoporous silica. MCM-41 16 with the highest surface area possesses the largest loading amount, which is up to 33.99 wt%. The loading and release kinetics (in vitro in simulated stomach fluid) showed that both of them were affected not only by the pore diameter but also by the morphologies of mesoporous silica materials. A rapid drug loading could be achieved either by enlarging pore sizes or by reducing particle sizes. And CapH 2 /SBA-15 delivery system with the largest pore diameter of 7.39 nm has exhibited the fastest release rate. While CapH 2 /MCM-41 12 system with the smallest pore diameter of 1.65 nm and sphere morphology (120–250 nm in size) has a faster release rate than that of CapH 2 /MCM-41 16 system with 2.17 nm pore diameter and rod-like morphology (ca. 20 μm in length). By comparing the release rate of CapH 2 /MCM-41 16 in a simulated stomach fluid with that in the proximal intestine fluid, it was found that the release media played a key role on the drug delivery profiles.

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

[2]  D. Zhao,et al.  A Fast Way for Preparing Crack-free Mesostructured Silica Monolith , 2003 .

[3]  A. Zukal,et al.  Mesoporous silica with controlled porous structure and regular morphology , 1999 .

[4]  J. S. Beck,et al.  Ordered mesoporous molecular sieves synthesized by a liquid-crystal template mechanism , 1992, Nature.

[5]  M. Jaroniec,et al.  Characterization of the Porous Structure of SBA-15 , 2000 .

[6]  D. Zhao,et al.  Rapid and high-capacity immobilization of enzymes based on mesoporous silicas with controlled morphologies. , 2003, Chemical communications.

[7]  L. Pellerito,et al.  Characterization of diorganotin(IV) complexes with captopril. The first crystallographically authenticated metal complex of this anti-hypertensive agent. , 2003, Journal of inorganic biochemistry.

[8]  Fredrickson,et al.  Triblock copolymer syntheses of mesoporous silica with periodic 50 to 300 angstrom pores , 1998, Science.

[9]  M. Vallet‐Regí,et al.  MCM-41 Organic Modification as Drug Delivery Rate Regulator , 2003 .

[10]  Gao Qing Lu,et al.  Modification of MCM-41 by Surface Silylation with Trimethylchlorosilane and Adsorption Study , 1998 .

[11]  K. Tsutsumi,et al.  Surface Functionalization and Stabilization of Mesoporous Silica Spheres by Silanization and Their Adsorption Characteristics , 2002 .

[12]  Jordan T. Watson,et al.  Catalytic activity of mesoporous silicate-immobilized chloroperoxidase , 2002 .

[13]  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.

[14]  B. K. Hodnett,et al.  Mechanistic and Structural Features of Protein Adsorption onto Mesoporous Silicates , 2002 .

[15]  J. B. Higgins,et al.  A new family of mesoporous molecular sieves prepared with liquid crystal templates , 1992 .

[16]  Luyan Zhang,et al.  Immobilization of enzymes in mesoporous materials: controlling the entrance to nanospace , 2004 .

[17]  C. Barbé,et al.  Silica Particles: A Novel Drug‐Delivery System , 2004 .

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

[19]  C. Mou,et al.  Extensive Void Defects in Mesoporous Aluminosilicate MCM-41 , 2000 .

[20]  Victor S-Y Lin,et al.  A mesoporous silica nanosphere-based carrier system with chemically removable CdS nanoparticle caps for stimuli-responsive controlled release of neurotransmitters and drug molecules. , 2003, Journal of the American Chemical Society.

[21]  K. Hidajat,et al.  Functionalized SBA-15 materials as carriers for controlled drug delivery: influence of surface properties on matrix-drug interactions. , 2005, Langmuir : the ACS journal of surfaces and colloids.

[22]  M. Vallet‐Regí,et al.  Mesoporous SBA-15 HPLC evaluation for controlled gentamicin drug delivery. , 2004, Journal of controlled release : official journal of the Controlled Release Society.

[23]  M. Lindén,et al.  Unusual, Vesicle-like Patterned, Mesoscopically Ordered Silica , 2003 .

[24]  A. O. Nur,et al.  Recent progress in sustained/controlled oral delivery of captopril: an overview. , 2000, International journal of pharmaceutics.

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

[26]  Victor S-Y Lin,et al.  A polyamidoamine dendrimer-capped mesoporous silica nanosphere-based gene transfection reagent. , 2004, Journal of the American Chemical Society.

[27]  S. J. Gregg,et al.  Adsorption Surface Area and Porosity , 1967 .

[28]  F. Caruso,et al.  Mesoporous Silica Particles as Templates for Preparing Enzyme‐Loaded Biocompatible Microcapsules , 2005 .

[29]  D. Zhao,et al.  High‐Yield Synthesis of Periodic Mesoporous Silica Rods and Their Replication to Mesoporous Carbon Rods , 2002 .

[30]  Yufang Zhu,et al.  Stimuli-responsive controlled drug release from a hollow mesoporous silica sphere/polyelectrolyte multilayer core-shell structure. , 2005, Angewandte Chemie.

[31]  M. Vallet‐Regí,et al.  Mesoporous MCM-41 as Drug Host System , 2003 .

[32]  Bradley F. Chmelka,et al.  Nonionic Triblock and Star Diblock Copolymer and Oligomeric Surfactant Syntheses of Highly Ordered, Hydrothermally Stable, Mesoporous Silica Structures , 1998 .

[33]  Larry A. Sklar,et al.  Control of Molecular Transport Through Stimuli‐Responsive Ordered Mesoporous Materials , 2003 .

[34]  P. Wright,et al.  Enzyme immobilisation using SBA-15 mesoporous molecular sieves with functionalised surfaces , 2001 .

[35]  D. Zhao,et al.  Multiphase assembly of mesoporous-macroporous membranes , 1999 .

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