“New trends and strategies in the chemistry of advanced materials with relevance in biological systems, technique and environmental protection” 9th Edition, June 09-10, 2016
QUERCETIN ENCAPSULATION IN MAGNETIC SILICA NANOPARTICLES TARGETING IN VIVO APPLICATIONS Christiane M. NDAYa,b, Eleftherios HALEVASa,c, S. LAURENTd, Graham JACKSONb, George LITSARDAKISc, Athanasios SALIFOGLOUa a
Department of Chemical Engineering, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece b Department of Chemistry, University of Cape Town, 7700 Rondebosch, Cape Town, South Africa c Laboratory of Materials for Electrotechnics, Department of Electrical and Computer Engineering, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece d Department of General, Organic and Biomedical Chemistry, NMR and Molecular Imaging Laboratory, Faculty of Medicine and pharmacy, University of Mons, 7000 Mons, Belgium E-mail:
[email protected],
[email protected] Alzheimer’s disease (AD) is a progressive neurocognitive and functional deficiency disease, affecting 95% of the AD cases of >65 year old people [1,2]. As a progressive neurodegenerative disease, brain damage occurs along with β amyloid and tau protein accumulation, affecting the neuro-synaptic circuit of the patients [3,4,5]. Despite intensive research in the AD field, no cure has been found. Recently, greater attention has been focused on the advancement of naturally occurring antioxidant compounds, including quercetin. In the current work, efforts were made to synthesize quercetin-loaded magnetic PEGylated silica nanospheres with potentially enhanced magnetic and imaging characteristics. The new hybrid magnetic nanomaterials were fully characterized through elemental analysis, particle size, z-potential, FT-IR, thermogravimetric analysis, relaxivity measurements, TEM and SEM. Drug release studies were run using UV-visible spectroscopy. Furthermore, MRI properties and interactions of the quercetin magnetic nanocarriers with βamyloid peptide were demonstrated in rat hippocampal primary cell cultures. Overall, the findings suggested that: a) solubility and polydispersity improvement affected T1 and T2 relaxivity indicators, which are directly connected to MRI properties, b) magnetic physical properties were in line with differential magnetic efficacy profiles of the samples as the observed magnetic core of all samples maintained its size, and c) the biological activity profile of quercetin-loaded magnetic nanoparticles in a cellular neurodegenerative environment denotes the improved specificity of antioxidant reactivity counteracting oxidative stress reactivity. The new hybrid magnetic nanomaterials are expected to contribute to a) the achievement of improved targeted therapeutic activity, protection against QC degradation, pharmacokinetic optimization and control of its biodistribution, and b) decreased cytotoxicity as a result of a slower yet efficient QC release, counteracting induced Aβ toxic endpoints in neurodegenerative processes.
Acknowledgements The authors would like to acknowledge the Research Committee (RC) of Aristotle University of Thessaloniki, Greece. References 1. E. H. Kua, E. Ho, H. H. Tan, C. Tsoi, C. Thng, R. Mahendran, Psychogeriatrics 14 (2014) 196-201. 2. B. Boland, F. M. Platt, Best Pract. Res. Clin. Endocrinol. Metab. 29 (2015) 127-143. 3. P. A. Adlard, B. A. Tran, D. I. Finkelstein, P. M. Desmond, L. A. Johnston, A. I. Bush, G. F. Egan, Front Neurosci. 8 (2014) 327. 4. D. R. Thal, J. Attems, M. Ewers, J Alzheimers Dis. 42 (2014) Suppl 4:S421-S429. 5. G. K. Gouras, K. Willén, M. Faideau, Neurodegener. Dis. 13 (2014) 142-146.
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