Modulation of folic acid bioaccessibility by encapsulation in pH-responsive gated mesoporous silica particles

[EN] A study on the controlled release of folic acid (FA) from pH-responsive gated mesoporous silica particles (MSP) is reported. The MCM-41 support was synthesized using tetraethyl orthosilicate (TEOS) as hydrolytic inorganic precursor and the surfactant hexadecyltrimethylammonium bromide (CTAB) as porogen species. Calcination of the mesostructured phase resulted in the starting solid. This solid was loaded with FA to obtain the initial support S0. Moreover, this FA-loaded material was further functionalized with 3-[2-(2-aminoethylamino)ethylamino]propyltrimethoxysilane (N3) in order to obtain the gated polyamine-functionalised material S1. Solids S0 and S1 were characterized using standar…

Protective effect of mesoporous silica particles on encapsulated folates.

Mesoporous silica particles (MSPs) are considered suitable supports to design gated materials for the encapsulation of bioactive molecules. Folates are essential micronutrients which are sensitive to external agents that provoke nutritional deficiencies. Folates encapsulation in MSPs to prevent degradation and to allow their controlled delivery is a promising strategy. Nevertheless, no information exists about the protective effect of MSPs encapsulation to prevent their degradation. In this work, 5-formyltetrahydrofolate (FO) and folic acid (FA) were entrapped in MSPs functionalized with polyamines, which acted as pH-dependent molecular gates. The stability of free and entrapped vitamins af…

ChemInform Abstract: Crystal Structure and Magnetic Properties of α-Mn(H2PO2)2× H2O.

Abstract The crystal structure of α-Mn(H2PO2)2·H2O has been refined from X-ray powder diffraction data. The cell is monoclinic (space group P21/c, Z − 4) with α = 7.8601(3) A , b = 7.4411(3) A , c = 10.7717(4) A and β = 102.859(2)°. The structure was refined with the Rietveld refinement principles, using as starting model the parameters of the presumably isostructural compound Zn(H2PO2)2·H2O. The structure can be described as being formed by dimeric entities Mn2O2 of edge-sharing manganese octahedra. Each group is linked through Mn-O-P-O-Mn bridges to four other groups, resulting in a three-dimensional network. The thermal variation in the susceptibility shows a sharp peak at T = 6.5 K and …

Cathepsin-B Induced Controlled Release from Peptide-Capped Mesoporous Silica Nanoparticles

New capped silica mesoporous nanoparticles for intracellular controlled cargo release within cathepsin B expressing cells are described. Nanometric mesoporous MCM-41 supports loaded with safranin O (S1-P) or doxorubicin (S2-P) containing a molecular gate based on a cathepsin B target peptidic sequence were synthesized. Solids were designed to show "zero delivery" and to display cargo release in the presence of cathepsin B enzyme, which selectively hydrolyzed in vitro the capping peptide sequence. Controlled delivery in HeLa, MEFs WT, and MEFs lacking cathepsin B cell lines were also tested. Release of safranin O and doxorubicin in these cells took place when cathepsin B was active or presen…

Targeted-lung delivery of dexamethasone using gated mesoporous silica nanoparticles. A new therapeutic approach for acute lung injury treatment

Acute lung injury (ALI) is a critical inflammatory syndrome, characterized by increased diffuse inflammation and severe lung damage, which represents a clinical concern due to the high morbidity and mortality in critical patients. In last years, there has been a need to develop more effective treatments for ALI, and targeted drug delivery to inflamed lungs has become an attractive research field. Here, we present a nanodevice based on mesoporous silica nanoparticles loaded with dexamethasone (a glucocorticoid extensively used for ALI treatment) and capped with a peptide that targets the TNFR1 receptor expressed in pro-inflammatory macrophages (TNFR-Dex-MSNs) and avoids cargo leakage. TNFR-D…

Enhanced antifungal efficacy of tebuconazole using gated pH-driven mesoporous nanoparticles

Núria Mas,1–3 Irene Galiana,3 Silvia Hurtado,† Laura Mondragón,1–3 Andrea Bernardos,1–3 Félix Sancenón,1–3 María D Marcos,1–3 Pedro Amorós,4 Nuria Abril-Utrillas,5 Ramón Martínez-Máñez,1–3 José Ramón Murguía1,3 1Centro de Reconocimiento Molecular y Desarrollo Tecnológico (IDM), Centro Mixto Universidad Politécnica de Valencia, Universidad de Valencia, Valencia, Spain; 2Departamento de Química, Universidad Politécnica de Valencia, Valenci…

Hydrolysis of DCNP (a Tabun mimic) catalyzed by mesoporous silica nanoparticles

[EN] The hydrolysis of diethylcyanophosphonate, DCNP (a Tabun simulant) in the presence of mesoporous silica nanoparticles (MSN) has been studied in acetonitrile:water (99.5:0.5 v/v) mixtures using 31P NMR as a suitable technique to follow the DCNP hydrolysis. MSN alone was not capable to induce DCNP hydrolysis, yet MSN in combination with the presence of the bases potassium carbonate, triethylamine or DABCO enhanced DCNP degradation. When MSN was used combined with K2CO3, a hydrolysis of ca. 95% of the initial DCNP after 60 min was observed. In the presence of DABCO, MSN was able to induce the hydrolysis of ca. 90% of DCNP after the same time. However, the DCNP hydrolysis using MSN in the …

Stability of different mesoporous silica particles during an in vitro digestion

Mesoporous silica materials have the ability to entrap drugs, nutrients and functional biomolecules and can be able to act as smart delivery systems capable to control and target the release of their cargo in a particular part of the gastrointestinal tract when administrated orally. However, the aptness of these encapsulation supports in in vivo oral controlled release relies on their chemical stability through the digestive tube. In this context, we have evaluated the stability of four different mesoporous silica particles, frequently used as encapsulating supports, during an in vitro digestion process comprising buccal, stomach and intestinal phases. Results showed that after 4 h of diges…

Poly(N-isopropylacrylamide)-gated Fe3O4/SiO2 core shell nanoparticles with expanded mesoporous structures for the temperature triggered release of lysozyme

Core-shell nanoparticles comprised of Fe3O4 cores and a mesoporous silica shell with an average expanded pore size of 6.07 nm and coated with a poly(N-isopropylacrylamide) (PNIPAM) layer (CS MSNs EP PNIPAM) were prepared and characterized. The nanoparticles was loaded with (Ru(bipy)3 2+) dye or an antibacterial enzyme, lysozyme, to obtain CS MSNs EP PNIPAM Ru(bipy)3 2+ and CS MSNs EP PNIPAM Lys, respectively. The lysozyme loading was determined to be 160 mg/g of nanoparticle. It was seen that Ru(bipy)3 2+ and lysozyme release was minimal at a room temperature of 25 ºC while at physiological temperature (37 º C), abrupt release was observed. The applicability of the CS MSNs EP PNIPAM Lys was…

Heterogeneous Gold Catalyst: Synthesis, Characterization, and Application in 1,4-Addition of Boronic Acids to Enones

The new 1 wt % Au/TiO2–UVM-7 catalyst was prepared and fully characterized. This heterogeneous catalyst proved to be active, selective and recyclable for the unprecedented gold-catalyzed 1,4-addition of various functionalized arylboronic acids to 2-cyclohexen-1-one and other selected enones using toluene as a solvent. The gold-based catalyst was recycled two times and played an active role in this reaction, and the nature of the solvent determined a remarkable change in the products’ selectivities.

An aptamer-gated silica mesoporous material for thrombin detection.

An aptamer-capped mesoporous material for the selective and sensitive detection of &-thrombin in human plasma and serum has been prepared and characterised.

Tetrathiafulvalene-Capped Hybrid Materials for the Optical Detection of Explosives

[EN] Mesoporous silica microparticles capped with TTF moieties and containing a ruthenium dye in the pores were used for the turn-on optical detection of the nitroaromatic explosives Tetryl and TNT via a selective pore uncapping and release of the entrapped dye.

Temperature-controlled release by changes in the secondary structure of peptides anchored onto mesoporous silica supports

Changes in the conformation of a peptide anchored onto the external surface of mesoporous silica nanoparticles have been used to design novel temperature-controlled delivery systems.

New Insights of Oral Colonic Drug Delivery Systems for Inflammatory Bowel Disease Therapy

[EN] Colonic Drug Delivery Systems (CDDS) are especially advantageous for local treatment of inflammatory bowel diseases (IBD). Site-targeted drug release allows to obtain a high drug concentration in injured tissues and less systemic adverse effects, as consequence of less/null drug absorption in small intestine. This review focused on the reported contributions in the last four years to improve the effectiveness of treatments of inflammatory bowel diseases. The work concludes that there has been an increase in the development of CDDS in which pH, specific enzymes, reactive oxygen species (ROS), or a combination of all of these triggers the release. These delivery systems demonstrated a th…

Encapsulation of folic acid in different silica porous supports: A comparative study.

Although folic acid is essential to numerous bodily functions, recent research indicates that a massive exposition to the vitamin could be a double-edged sword. In this study, the capacity of different caped mesoporous silica particles (i.e. Hollow Silica Shells, MCM-41, SBA-15 and UVM-7) to dose FA during its passage through the gastrointestinal tract has been evaluated. Results confirmed that the four capped materials were capable to hinder the delivery of FA at low pH (i.e. stomach) as well as able to deliver great amounts of the vitamin at neutral pH (i.e. intestine). Nevertheless, the encapsulation efficiency and the deliver kinetics differed among supports. While supports with large p…

Organic-Inorganic Hybrid Mesoporous Materials as Regenerable Sensing Systems for the Recognition of Nitroaromatic Explosives

[EN] Fluorescent organic-inorganic mesoporous hybrid materials have been prepared and characterised, and their behaviour against nitroaromatic explosives have been tested. MCM-41 silica was used as an inorganic scaffold and pyrene (P derivative containing trialkoxysilane moieties), dansyl and fluorescein (D and F derivatives also containing trialkoxysilane groups, respectively) fluorophores have been anchored on hybrid materials by a co-condensation method to obtain a homogenous distribution of dyes into the pores of the support. Six sensing materials have been prepared, of which SP, SD, SF were hydrophilic and SPh, SDh, SFh were hydrophobic. Template-free hydrophilic materials (SP, SD, SF)…

Selective and Sensitive Chromofluorogenic Detection of the Sulfite Anion in Water Using Hydrophobic Hybrid Organic-Inorganic Silica Nanoparticles

[EN] In water and wine: Chromofluorogenic detection of the sulfite anion in pure water was accomplished by using a new hybrid organic-inorganic material that contained a probe entrapped in hydrophobic biomimetic cavities. This material was used for the detection of sulfite in red wine. Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Enzyme-Responsive Controlled Release Using Mesoporous Silica Supports Capped with Lactose

Controlled delivery using oligonucleotide-capped mesoporous silica nanoparticles.

Transition metal derivatives of low oxidation state phosphorus oxoacids: synthetic pathways and structural studies

Abstract A general synthetic approach intended to rationalize the solution preparative chemistry of transition metal phosphites and hypophosphites is presented. As previously shown for other derivatives containing also tetrahedral or pseudotetrahedral oxoanions, the hydrolytic processes affecting the cationic moieties play a determinant role on the very nature of the final solid. In fact, despite the limited number of donor atoms in the anions, the crystal chemistry of these compounds is quite intricate because of both the variety of possible cationic aggregates and the many ways to interconnect them through pseudotetrahedral anionic groups.

ChemInform Abstract: Transition Metal Derivatives of Low Oxidation State Phosphorus Oxoacids: Synthetic Pathways and Structural Studies

Abstract A general synthetic approach intended to rationalize the solution preparative chemistry of transition metal phosphites and hypophosphites is presented. As previously shown for other derivatives containing also tetrahedral or pseudotetrahedral oxoanions, the hydrolytic processes affecting the cationic moieties play a determinant role on the very nature of the final solid. In fact, despite the limited number of donor atoms in the anions, the crystal chemistry of these compounds is quite intricate because of both the variety of possible cationic aggregates and the many ways to interconnect them through pseudotetrahedral anionic groups.

Hybrid materials with nanoscopic anion-binding pockets for the colorimetric sensing of phosphate in water using displacement assays

Mesoporous amino-functionalised solids containing certain dyes have been used as suitable anion hosts in displacement assays for the colorimetric signalling of phosphate in water. Amoros del Toro, Pedro Jose, Pedro.Amoros@uv.es

Enhanced Efficacy and Broadening of Antibacterial Action of Drugs via the Use of Capped Mesoporous Nanoparticles

[EN] A novel nanodevice consisting of mesoporous nanoparticles loaded with vancomycin and capped with epsilon-poly-L-lysine (epsilon-PL) was prepared and its interaction with different Gram-negative bacteria studied. A remarkable improvement in the efficacy of the antimicrobial drug epsilon-PL and a broadening of the antimicrobial spectrum of vancomycin is demonstrated.

Atrane complexes chemistry as a tool for obtaining trimodal UVM-7-like porous silica

[EN] The use of atrane complexes as hydrolytic precursors enables the homogeneous incorporation of manganese (25Si/Mn48) throughout the porous walls of the nanoparticles of a surfactant-templated bimodal mesoporous silica (UVM-7). The subsequent leaching of the manganese nanodomains allows adding controlled microporosity to the host silica framework. The resulting final silica material presents three pore systems structured at different length scales: interparticle textural-type macroporosity (ca. 43.2nm), ordered intraparticle mesoporosity (ca. 2.63nm; after template removal), and well-dispersed microporosity (< 2nm; as consequence of the lixiviation of the Mn-rich domains). The good dispe…

A photoactivated molecular gate.

Light-controlled gate: A novel capped silica nanoscopic mesoporous hybrid material for photo-driven cargo release applications has been designed and prepared. The capped system, which shows a zero release, contains a photo-cleavable bulky o-methoxybenzylamine derivative. Upon irradiation at 254¿nm, photo-degradation of the o-methoxybenzylamine framework and the subsequent delivery of a fluorescent cargo were observed