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[EN] A new colorimetric system for NO(g) detection is described. The detection method is based on the aggregation of modified AuNPs through a Cu(I) catalyzed click reaction promoted by the in situ reduction of Cu(II) by NO ; We acknowledge the Spanish Government (MAT2009-14564-C04-03 and MAT2012-38429-C04-02) for financial support. A. M. is grateful to the Spanish Government for a fellowship. SCSIE (Universidad de Valencia) is gratefully acknowledged for all the equipment employed. ; Marti, A.; Costero Nieto, AM.; Gaviña Costero, P.; Parra Álvarez, M. (2015). Selective colorimetric NO(g) detection based on the use of modified gold nanoparticles using click chemistry. Chemical Communications. 51(15):3077-3079. https://doi.org/10.1039/c4cc10149a ; S ; 3077 ; 3079 ; 51 ; 15 ; Nagano, T. (1999). Practical methods for detection of nitric oxide. Luminescence, 14(6), 283-290. doi:10.1002/(sici)1522-7243(199911/12)14:6 283::aid-bio572>3.0.co;2-g ; L. J. Ignarro , Nitric Oxide: Biology and Pathobiology, Academic Press, San Diego, 2010 ; Ma, S., Fang, D.-C., Ning, B., Li, M., He, L., & Gong, B. (2014). The rational design of a highly sensitive and selective fluorogenic probe for detecting nitric oxide. Chem. Commun., 50(49), 6475-6478. doi:10.1039/c4cc01142b ; Kojima, H., Nakatsubo, N., Kikuchi, K., Kawahara, S., Kirino, Y., Nagoshi, H., … Nagano, T. (1998). Detection and Imaging of Nitric Oxide with Novel Fluorescent Indicators: Diaminofluoresceins. Analytical Chemistry, 70(13), 2446-2453. doi:10.1021/ac9801723 ; Chen, X., Tian, X., Shin, I., & Yoon, J. (2011). Fluorescent and luminescent probes for detection of reactive oxygen and nitrogen species. Chemical Society Reviews, 40(9), 4783. doi:10.1039/c1cs15037e ; Beltrán, A., Isabel Burguete, M., Abánades, D. R., Pérez-Sala, D., Luis, S. V., & Galindo, F. (2014). Turn-on fluorescent probes for nitric oxide sensing based on the ortho-hydroxyamino structure showing no interference with dehydroascorbic acid. Chemical Communications, 50(27), 3579. ...

3077 3079 51 15 ; S ; [EN] A new colorimetric system for NO(g) detection is described. The detection method is based on the aggregation of modified AuNPs through a Cu(I) catalyzed click reaction promoted by the in situ reduction of Cu(II) by NO We acknowledge the Spanish Government (MAT2009-14564-C04-03 and MAT2012-38429-C04-02) for financial support. A. M. is grateful to the Spanish Government for a fellowship. SCSIE (Universidad de Valencia) is gratefully acknowledged for all the equipment employed. Marti, A.; Costero Nieto, AM.; Gaviña Costero, P.; Parra Álvarez, M. (2015). Selective colorimetric NO(g) detection based on the use of modified gold nanoparticles using click chemistry. Chemical Communications. 51(15):3077-3079. https://doi.org/10.1039/c4cc10149a Nagano, T. (1999). Practical methods for detection of nitric oxide. Luminescence, 14(6), 283-290. doi:10.1002/(sici)1522-7243(199911/12)14:63.0.co;2-g L. J. Ignarro , Nitric Oxide: Biology and Pathobiology, Academic Press, San Diego, 2010 Ma, S., Fang, D.-C., Ning, B., Li, M., He, L., & Gong, B. (2014). The rational design of a highly sensitive and selective fluorogenic probe for detecting nitric oxide. Chem. Commun., 50(49), 6475-6478. doi:10.1039/c4cc01142b Kojima, H., Nakatsubo, N., Kikuchi, K., Kawahara, S., Kirino, Y., Nagoshi, H., … Nagano, T. (1998). Detection and Imaging of Nitric Oxide with Novel Fluorescent Indicators: Diaminofluoresceins. Analytical Chemistry, 70(13), 2446-2453. doi:10.1021/ac9801723 Chen, X., Tian, X., Shin, I., & Yoon, J. (2011). Fluorescent and luminescent probes for detection of reactive oxygen and nitrogen species. Chemical Society Reviews, 40(9), 4783. doi:10.1039/c1cs15037e Beltrán, A., Isabel Burguete, M., Abánades, D. R., Pérez-Sala, D., Luis, S. V., & Galindo, F. (2014). Turn-on fluorescent probes for nitric oxide sensing based on the ortho-hydroxyamino structure showing no interference with dehydroascorbic acid. Chemical Communications, 50(27), 3579. doi:10.1039/c3cc49555h Lv, X., ...

[EN] Two dansyl-modified beta-cyclodextrin derivatives (1 and 2) have been synthesized as host-guest sensory systems for the direct fluorescent detection of the peroxide explosives diacetone diperoxide (DADP) and triacetone triperoxide (TATP) in aqueous media. The sensing is based on the displacement of the dansyl moiety from the cavity of the cyclodextrin by the peroxide guest resulting in a decrease of the intensity of the fluorescence of the dye. Both systems showed similar fluorescent responses and were more sensitive towards TATP than DADP. ; We thank the Spanish Government (MAT2015-64139-C4-4-R) and Generalitat Valenciana (PROMETEOII/2014/047) for financial support. ; Almenar, E.; Costero, AM.; Gaviña, P.; Gil Grau, S.; Parra Álvarez, M. (2018). Towards the fluorogenic detection of peroxide explosives through host-guest chemistry. Royal Society Open Science. 5(4). https://doi.org/10.1098/rsos.171787 ; S ; 5 ; 4 ; Dubnikova, F., Kosloff, R., Almog, J., Zeiri, Y., Boese, R., Itzhaky, H., … Keinan, E. (2005). Decomposition of Triacetone Triperoxide Is an Entropic Explosion. Journal of the American Chemical Society, 127(4), 1146-1159. doi:10.1021/ja0464903 ; Fitzgerald, M., & Bilusich, D. (2011). Sulfuric, Hydrochloric, and Nitric Acid-Catalyzed Triacetone Triperoxide (TATP) Reaction Mixtures: An Aging Study. Journal of Forensic Sciences, 56(5), 1143-1149. doi:10.1111/j.1556-4029.2011.01806.x ; Matyáš, R., Pachman, J., & Ang, H.-G. (2009). Study of TATP: Spontaneous Transformation of TATP to DADP - Full Paper. Propellants, Explosives, Pyrotechnics, 34(6), 484-488. doi:10.1002/prep.200800043 ; Matyas, R., Pachman, J., & Ang, H.-G. (2008). Study of TATP: Spontaneous Transformation of TATP to DADP. Propellants, Explosives, Pyrotechnics, 33(2), 89-91. doi:10.1002/prep.200700247 ; Wang, J. (2007). Electrochemical Sensing of Explosives. Electroanalysis, 19(4), 415-423. doi:10.1002/elan.200603748 ; Bauer, C., Willer, U., Lewicki, R., Pohlkötter, A., Kosterev, A., Kosynkin, D., … Schade, W. (2009). A ...

[EN] A new chromo-fluorogenic probe, consisting of a biphenyl derivative containing both a silylbenzyl ether and a N,N-dimethylamino group, for NO2 detection in the gas phase has been developed. A clear colour change from colourless to yellow together with an emission quenching was observed when the probe reacted with NO2. A limit of detection to the naked eye of about 0.1 ppm was determined and the system was successfully applied to the detection of NO2 in realistic atmospheric conditions. ; We thank the Spanish Government (MAT2012‐38429‐C04) and Generalitat Valenciana (PROMETEOII/2014/047) for support. SCSIE (Universidad de Valencia) is gratefully acknowledged for all the equipment employed. We thank Dr. A. Múñoz from the CEAM (Valencia‐Spain) for her help for the development of the measures in real environment. ; Juarez, LA.; Costero, AM.; Sancenón Galarza, F.; Martínez-Máñez, R.; Parra Álvarez, M.; Gaviña Costero, P. (2015). A New Simple Chromo-fluorogenic Probe for NO2 Detection in Air. Chemistry - A European Journal. 21(24):8720-8722. https://doi.org/10.1002/chem.201500608 ; S ; 8720 ; 8722 ; 21 ; 24

Two new aryl carbinols (1 and 3) have been synthesised and characterised and their ability as OFF-ON probes for the chromogenic detection of the nerve agent simulant in acetonitrile has been tested. In addition compound 2 has been also studied. The carbinols suffered a phosphorylation reaction followed by an elimination process giving rise to the corresponding carbocations. This transformation of the carbinol into the carbocation is responsible for a significant color change. © The Royal Society of Chemistry and the Centre National de la Recherche Scientifique 2012. ; Financial support from the Spanish Government (project MAT2009-14564-C04-01) and the Generalitat Valencia (project PROMETEO/2009/016) is gratefully acknowledged. R. G. is grateful to the Spanish Ministry of Education and S. R. to Generalitat Valencia for their grants. ; Royo Calvo, S.; Gotor Candel, RJ.; Costero Nieto, AM.; Parra Álvarez, M.; Gil Grau, S.; Martínez Mañez, R.; Sancenón Galarza, F. (2012). Aryl carbinols as nerve agent probes. Influence of the conjugation on the sensing properties. New Journal of Chemistry. 36(12):1485-1489. https://doi.org/10.1039/c2nj40104e ; S ; 1485 ; 1489 ; 36 ; 12 ; Sadik, O. A., Land, W. H., & Wang, J. (2003). Targeting Chemical and Biological Warfare Agents at the Molecular Level. Electroanalysis, 15(14), 1149-1159. doi:10.1002/elan.200390140 ; Russell, A. J., Berberich, J. A., Drevon, G. F., & Koepsel, R. R. (2003). Biomaterials for Mediation of Chemical and Biological Warfare Agents. Annual Review of Biomedical Engineering, 5(1), 1-27. doi:10.1146/annurev.bioeng.5.121202.125602 ; Wang, H., Wang, J., Choi, D., Tang, Z., Wu, H., & Lin, Y. (2009). EQCM immunoassay for phosphorylated acetylcholinesterase as a biomarker for organophosphate exposures based on selective zirconia adsorption and enzyme-catalytic precipitation. Biosensors and Bioelectronics, 24(8), 2377-2383. doi:10.1016/j.bios.2008.12.013 ; Im, H.-J., & Song, K. (2009). Applications of Prompt Gamma Ray Neutron Activation Analysis: ...

Two triaryl methane cations have been used as probes for colorimetric detection of nerve agent simulants. Buffered mixed aqueous solutions of 1 and 2 showed bathochromic shifts in the presence of DCNP (diethylcyanophosphonate) and DCP (diethylchlorophosphate). The colour modulation can be observed to the naked eye. Appropriate mechanisms for the recognition event are proposed. © 2012 Elsevier Ltd. ; We thank the Spanish Government (projects MAT2009-14564-C01 and MAT2009-14564-C03) and the Generalitat Valenciana (project PROMETEO/2009/016) for support. R.G. is grateful to the Spanish Government for a fellowship. S.R. is grateful to the Generalitat Valenciana for a fellowship. SCSIE (Universidad de Valencia) is gratefully acknowledged for all the equipment employed. ; Gotor Candel, RJ.; Royo Calvo, S.; Costero Nieto, AM.; Parra Álvarez, M.; Gil Grau, S.; Martínez Mañez, R.; Sancenón Galarza, F. (2012). Nerve agent simulant detection by using chromogenic triaryl methane cation probes. Tetrahedron. 68(41):8612-8616. https://doi.org/10.1016/j.tet.2012.07.091 ; S ; 8612 ; 8616 ; 68 ; 41

1485 1489 36 12 ; S ; Two new aryl carbinols (1 and 3) have been synthesised and characterised and their ability as OFF-ON probes for the chromogenic detection of the nerve agent simulant in acetonitrile has been tested. In addition compound 2 has been also studied. The carbinols suffered a phosphorylation reaction followed by an elimination process giving rise to the corresponding carbocations. This transformation of the carbinol into the carbocation is responsible for a significant color change. © The Royal Society of Chemistry and the Centre National de la Recherche Scientifique 2012. Financial support from the Spanish Government (project MAT2009-14564-C04-01) and the Generalitat Valencia (project PROMETEO/2009/016) is gratefully acknowledged. R. G. is grateful to the Spanish Ministry of Education and S. R. to Generalitat Valencia for their grants. Royo Calvo, S.; Gotor Candel, RJ.; Costero Nieto, AM.; Parra Álvarez, M.; Gil Grau, S.; Martínez Mañez, R.; Sancenón Galarza, F. (2012). Aryl carbinols as nerve agent probes. Influence of the conjugation on the sensing properties. New Journal of Chemistry. 36(12):1485-1489. https://doi.org/10.1039/c2nj40104e Sadik, O. A., Land, W. H., & Wang, J. (2003). Targeting Chemical and Biological Warfare Agents at the Molecular Level. Electroanalysis, 15(14), 1149-1159. doi:10.1002/elan.200390140 Russell, A. J., Berberich, J. A., Drevon, G. F., & Koepsel, R. R. (2003). Biomaterials for Mediation of Chemical and Biological Warfare Agents. Annual Review of Biomedical Engineering, 5(1), 1-27. doi:10.1146/annurev.bioeng.5.121202.125602 Wang, H., Wang, J., Choi, D., Tang, Z., Wu, H., & Lin, Y. (2009). EQCM immunoassay for phosphorylated acetylcholinesterase as a biomarker for organophosphate exposures based on selective zirconia adsorption and enzyme-catalytic precipitation. Biosensors and Bioelectronics, 24(8), 2377-2383. doi:10.1016/j.bios.2008.12.013 Im, H.-J., & Song, K. (2009). Applications of Prompt Gamma Ray Neutron Activation Analysis: Detection of Illicit ...

[EN] This critical review is focused on examples reported from 1947 to 2010 related to the design of chromo-fluorogenic chemosensors and reagents for explosives (141 references). © 2012 The Royal Society of Chemistry. ; Financial support from the Spanish Government (project MAT2009-14564-C04) and the Generalitat Valencia (project PROMETEO/2009/016) is gratefully acknowledged. Y.S. is grateful to the Spanish Ministry of Science and Innovation for her grant. ; Salinas Soler, Y.; Martínez Mañez, R.; Marcos Martínez, MD.; Sancenón Galarza, F.; Costero Nieto, AM.; Parra Álvarez, M.; Gil Grau, S. (2012). Optical chemosensors and reagents to detect explosives. Chemical Society Reviews. 41(3):1261-1296. https://doi.org/10.1039/c1cs15173h ; S ; 1261 ; 1296 ; 41 ; 3 ; Furton, K. (2001). The scientific foundation and efficacy of the use of canines as chemical detectors for explosives. Talanta, 54(3), 487-500. doi:10.1016/s0039-9140(00)00546-4 ; H�kansson, K., Coorey, R. V., Zubarev, R. A., Talrose, V. L., & H�kansson, P. (2000). Low-mass ions observed in plasma desorption mass spectrometry of high explosives. Journal of Mass Spectrometry, 35(3), 337-346. doi:10.1002/(sici)1096-9888(200003)35:3 337::aid-jms940>3.0.co;2-7 ; Walsh, M. (2001). Determination of nitroaromatic, nitramine, and nitrate ester explosives in soil by gas chromatography and an electron capture detector. Talanta, 54(3), 427-438. doi:10.1016/s0039-9140(00)00541-5 ; Sylvia, J. M., Janni, J. A., Klein, J. D., & Spencer, K. M. (2000). Surface-Enhanced Raman Detection of 2,4-Dinitrotoluene Impurity Vapor as a Marker To Locate Landmines. Analytical Chemistry, 72(23), 5834-5840. doi:10.1021/ac0006573 ; Yinon, J. (1982). Mass spectrometry of explosives: Nitro compounds, nitrate esters, and nitramines. Mass Spectrometry Reviews, 1(3), 257-307. doi:10.1002/mas.1280010304 ; Mathurin, J. C., Faye, T., Brunot, A., Tabet, J. C., Wells, G., & Fuché, C. (2000). High-Pressure Ion Source Combined with an In-Axis Ion Trap Mass Spectrometer. 1. ...

The synthesis, characterization and sensing features of a novel probe 1 for the selective chromogenic recognition of diisopropylfluorophosphate (DFP), a sarin and soman mimic, in 99:1 (v/ v) water/acetonitrile and in the gas phase is reported. Colour modulation is based on the combined reaction of phosphorylation of 1 and fluoride-induced hydrolysis of a silyl ether moiety. As fluoride is a specific reaction product of the reaction between DFP and the OH group, the probe shows a selective colour modulation in the presence of this chemical. Other nerve agent simulants, certain anions, oxidant species and other organophosphorous compounds were unable to induce colour changes in 1. This is one of the very few examples of a selective detection, in solution and in the gas phase, of a sarin and soman simulant versus other reactive derivatives such as the tabun mimic diethylcyanophosphate (DCNP). ; Financial support from the Spanish Government (Project MAT2012-38429-C04) is gratefully acknowledged. S. E. is grateful to the Generalitat Valenciana for his Santiago Grisolia fellowship. L. P. thanks the Universitat Politecnica de Valencia for his doctoral fellowship. ; El Sayed Shehata Nasr, S.; Pascual Vidal, L.; Agostini, A.; Martínez-Máñez, R.; Sancenón Galarza, F.; Costero Nieto, AM.; Parra Álvarez, M. (2014). A Chromogenic Probe for the Selective Recognition of Sarin and Soman Mimic DFP. ChemistryOpen. 3(4):142-145. https://doi.org/10.1002/open.201402014 ; S ; 142 ; 145 ; 3 ; 4

[EN] Mesoporous silica microparticles were prepared, loaded with the dye safranin O (M-Saf) or with the drug budesonide (M-Bud) and capped by the grafting of a bulky azo derivative. Cargo release from M-Saf at different pH values (mimicking those found in the gastrointestinal tract) in the absence or presence of sodium dithionite (a reducing agent mimicking azoreductase enzyme present in the colon) was tested. Negligible safranin O release was observed at pH 6.8 and 4.5, whereas a moderate delivery at pH 1.2 was noted and attributed to the hydrolysis of the urea bond that linked the azo derivative onto the external surface of the inorganic scaffold. Moreover, a marked release was observed when sodium dithionite was present and was ascribed to the rupture of the azo bond in the molecular gate. Budesonide release from M-Bud in the presence of sodium dithionite was also assessed by ultraviolet-visible spectroscopy and high performance liquid chromatography measurements. In addition, preliminary in vivo experiments with M-Saf carried out in mice indicated that the chemical integrity of the microparticles remained unaltered in the stomach and the small intestine, and safranin O seemed to be released in the colon. ; We thank the Spanish Government (projects MAT2015-64139-C4-4-R, MAT2015-64139-C4-2-R and MAT2015-64139-C4-1-R) and Generalitat Valenciana (project PROMETEOII/2014/047 and project AICO/2017/093) for financial support. ; Ferri, D.; Gaviña, P.; Parra Álvarez, M.; Costero, AM.; El Haskouri, J.; Amorós Del Toro, P.; Merino Sanjuán, V. (2018). Mesoporous silica microparticles gated with a bulky azo derivative for the controlled release of dyes/ drugs in colon. Royal Society Open Science. 5(8). https://doi.org/10.1098/rsos.180873 ; S ; 5 ; 8 ; Xu, X.-M., & Zhang, H.-J. (2016). miRNAs as new molecular insights into inflammatory bowel disease: Crucial regulators in autoimmunity and inflammation. World Journal of Gastroenterology, 22(7), 2206-2218. doi:10.3748/wjg.v22.i7.2206 ; DeFilippis, E. M., Longman, R., ...

This is the peer reviewed version of the following article: E. Garrido, M. Alfonso, B. Díaz de Greñu, B. Lozano-Torres, M. Parra, P. Gaviña, M. D. Marcos, R. Martínez-Máñez, F. Sancenón, Chem. Eur. J. 2020, 26, 2813, which has been published in final form at https://doi.org/10.1002/chem.201905688. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Self-Archiving. ; [EN] This work reports the synthesis, characterization, and sensing behavior of a hybrid nanodevice for the detection of the potent abuse drug 25I-NBOMe. The system is based on mesoporous silica nanoparticles, loaded with a fluorescent dye, functionalized with a serotonin derivative and capped with the 5-HT2A receptor antibody. In the presence of 25I-NBOMe the capping antibody is displaced, leading to pore opening and rhodamine B release. This delivery was ascribed to 5-HT2A receptor antibody detachment from the surface due to its stronger coordination with 25I-NBOMe present in the solution. The prepared nanodevice allowed the sensitive (limit of detection of 0.6 mm) and selective recognition of the 25I-NBOMe drug (cocaine, heroin, mescaline, lysergic acid diethylamide, MDMA, and morphine were unable to induce pore opening and rhodamine B release). This nanodevice acts as a highly sensitive and selective fluorometric probe for the 25I-NBOMe illicit drug in artificial saliva and in sweets. ; The authors thank the Spanish Government (projects RTI2018-100910-B-C41 (MCUI/AEI/FEDER, UE) and CTQ2017-87954-P) and the Generalitat Valencia (PROMETEO/2018/024) for support. E.G. is grateful to the Spanish MEC for her FPU grant. The authors also thank the Electron Microscopy Service at the UPV for support. ; Garrido-García, EM.; Alfonso-Navarro, M.; Díaz De Greñu-Puertas, B.; Lozano-Torres, B.; Parra Álvarez, M.; Gaviña, P.; Marcos Martínez, MD. (2020). Nanosensor for Sensitive Detection of the New Psychedelic Drug 25I-NBOMe. Chemistry - A European Journal. 26(13):2813-2816. ...

This is the peer reviewed version of the following article: E. Añón, A. M. Costero, P. Amorós, J. El Haskouri, R. Martínez-Mánez, M. Parra, S. Gil, P. Gaviña, M. C. Terencio, M. Alfonso, ChemistrySelect 2020, 5, 3618., which has been published in final form at https://doi.org/10.1002/slct.202000417. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Self-Archiving. ; [EN] Osteoporosis is an illness which appears when the osteoblast/osteoclast activities are unbalanced taking place bone resorption (caused by osteoclasts) in higher extension than bone formation (induced by osteoblasts). Alendronate is one of the most used drugs for osteoporosis treatment despite its scarce bioavailability. Here we present the synthesis and characterization of mesoporous gated nanoparticles (two sets) for the controlled release of alendronate. The first set of nanoparticles (S1) were loaded with sulforhodamine B and capped with a peptide that could be selectively hydrolyzed by cathepsin K enzyme (overexpressed in osteoclasts). The second set (S2) was functionalized with aminopropyl moieties, loaded with nitrobenzofurazan labelled alendronate and capped with the same peptide. Both nanoparticles were internalized by RAW 264.7 macrophages (which could differentiate in osteoclasts) and were able to release its entrapped cargo in the presence of cathepsin K added in the macrophage lysates. Using S2 nanoparticles 4.2% of the total alendronate amount in contact with the cells is liberated inside them and could produce its therapeutic effect. ; We thank the Spanish Government (RTI2018-100910-B-C41, RTI2018-100910-B-C42 (MCUI/AEI/FEDER, UE)) and the Generalitat Valenciana (PROMETEU/2018/024) for support. SCSIE (Universitat de Valencia) is gratefully acknowledged for all the equipment employed. NMR was registered at the U26 facility of ICTS "NANBIOSIS" at the Universitat of Valencia. ; Añón, E.; Costero, AM.; Amorós Del Toro, P.; El Haskouri, J.; Martínez-Máñez, R.; Parra Álvarez, M.; Gil ...

58 69 281 ; S ; [EN] Magnetic mesoporous silica microparticles were loaded with safranin O (S1) and with hydrocortisone (S2) and the outer surface functionalized with a bulky azo derivative bearing urea moieties. Aqueous suspensions of both solids at pH 7.4 showed negligible payload release whereas a marked delivery was observed in the presence of sodium dithionite due to the rupture of the azo bonds. Besides, a moderate cargo release was observed at acidic pH due to the hydrolysis of the urea bonds that linked the azo derivative onto the external surface of the inorganic scaffolds. In vitro digestion models showed that S1 and S2 microparticles could be used for the controlled release of payload in the reducing colon environment (in which azoreductase enzymes are present). On the other hand, in vivo pharmacokinetic studies in rats showed that safranine O release from S1 microparticles was concentrated in colon. The performance of S2 microparticles for the treatment of colitis in rats (induced by oral administration of a 2,4,6-trinitrobenzenesulfonic acid solution) was tested. The controlled release of hydrocortisone from S2 in the colon of injured rats induced marked reduction in colon/body weight ratio and in clinical activity score. Also, histological studies showed a marked decrease in inflammation followed by intensive regeneration and almost normal mucosal structure of the individuals treated with S2. Besides, the use of a magnetic belt increased the therapeutic performances of S2 due to an enhanced retention time of the particles in the colon. We thank the Spanish Government (projects MAT2015-64139-C4-1-R and AGL2015-70235-C2-2-R (MINECO/FEDER)) and the Generalitat Valenciana (project PROMETEOII/2014/047) for support. AHT thanks to the Spanish MEC for his FPU grant. The authors also thank the Electron Microscopy Service at the Universitat Politecnica de Valencia for support. SCSIE (Universitat de Valencia) is also gratefully acknowledged for all the equipment employed. NMR was registered at the U26 ...

[EN] Magnetic mesoporous silica microparticles were loaded with safranin O (S1) and with hydrocortisone (S2) and the outer surface functionalized with a bulky azo derivative bearing urea moieties. Aqueous suspensions of both solids at pH 7.4 showed negligible payload release whereas a marked delivery was observed in the presence of sodium dithionite due to the rupture of the azo bonds. Besides, a moderate cargo release was observed at acidic pH due to the hydrolysis of the urea bonds that linked the azo derivative onto the external surface of the inorganic scaffolds. In vitro digestion models showed that S1 and S2 microparticles could be used for the controlled release of payload in the reducing colon environment (in which azoreductase enzymes are present). On the other hand, in vivo pharmacokinetic studies in rats showed that safranine O release from S1 microparticles was concentrated in colon. The performance of S2 microparticles for the treatment of colitis in rats (induced by oral administration of a 2,4,6-trinitrobenzenesulfonic acid solution) was tested. The controlled release of hydrocortisone from S2 in the colon of injured rats induced marked reduction in colon/body weight ratio and in clinical activity score. Also, histological studies showed a marked decrease in inflammation followed by intensive regeneration and almost normal mucosal structure of the individuals treated with S2. Besides, the use of a magnetic belt increased the therapeutic performances of S2 due to an enhanced retention time of the particles in the colon. ; We thank the Spanish Government (projects MAT2015-64139-C4-1-R and AGL2015-70235-C2-2-R (MINECO/FEDER)) and the Generalitat Valenciana (project PROMETEOII/2014/047) for support. AHT thanks to the Spanish MEC for his FPU grant. The authors also thank the Electron Microscopy Service at the Universitat Politecnica de Valencia for support. SCSIE (Universitat de Valencia) is also gratefully acknowledged for all the equipment employed. NMR was registered at the U26 facility of ICTS ...

[EN] Magnetic micro-sized mesoporous silica particles were used for the preparation of a gated material able to release an entrapped cargo in the presence of an azo-reducing agent and, to some extent, at acidic pH. The magnetic mesoporous microparticles were loaded with safranin O and the external surface was functionalized with an azo derivative 1 (bearing a carbamate linkage) yielding solid S1. Aqueous suspensions of S1 at pH 7.4 showed negligible safranin O release due to the presence of the bulky azo derivative attached onto the external surface of the inorganic scaffold. However, in the presence of sodium dithionite (azoreductive agent), a remarkable safranin O delivery was observed. At acidic pH, a certain safranin O release from S1 was also found. The pH-triggered safranin O delivery was ascribed to the acid-induced hydrolysis of the carbamate moiety that linked the bulky azo derivatives onto the mesoporous inorganic magnetic support. The controlled release behavior of S1 was also tested using a model that simulated the gastro intestinal tract. ; We thank the Spanish Government (projects MAT2015-64139-C4-1-R and AGL2015-70235C2-2-R (MINECO/FEDER)) and the Generalitat Valenciana (project PROMETEOII/2014/047) for support. AHT thanks to the Spanish MEC for his FPU grant. The authors also thank the Electron Microscopy Service at the Universitat Politecnica de Valencia for support. SCSIE (Universitat de Valencia) is also gratefully acknowledged for all the equipment employed. NMR was registered at the U26 facility of ICTS "NANBIOSIS" at the Universitat de Valencia. The authors thanks L.A. Villaescusa for his helpful discussion about the 1H-NMR analysis of the composition of loaded and functionalized supports. ; Teruel, AH.; Coll Merino, MC.; Costero, AM.; Ferri, D.; Parra Álvarez, M.; Gaviña, P.; Gonzalez -Alvarez, M. (2018). Functional magnetic mesoporous silica microparticles capped with an azo-derivative: A promising colon drug delivery device. Molecules. 23(2). https://doi.org/10.3390/molecules23020375 ; S ...