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Ana Maria Orbesteanu, Mihaela Ionescu, Otilia Cinteza, Ioana Ailiesei, Radu Hertzog, Lavinia G. Hinescu, Constantin Mircioiu . Inclusion of oximes and pyridostigmine in nanosystems as a new method for improving their bioavailability. Current Health Sciences Journal , vol 41 (2), pp. 51-54, 2015.

Abstract: This research paper focuses on the possibility of improving the bioavailability of some of the most common antidotes for organophosphosphates poisoning: obidoxime, HI-6 and pyridostigmine. Silica nanoparticles were prepared by hydrolysis and condensation of tetraethylorthosilicate (TEOS) as precursor material. Alginate microparticles with pyridostigmine are are obtained by two different methods. External gelation technique (with heptane as the organic phase) was selected as the method of preparation for alginate microparticles, considering the solubility of the active ingredient and the nature of the polymer. Release study of oximes from silica nanoparticles was performed using HPLC method. Cell penetration capacity was studied by confocal microscopy. HPLC analysis shown that 0,3% obidoxime was released from the nanoparticles, while it did not indicate the presence of HI -6. Analysis by confocal microscopy of culture cells penetration by silica nanoparticles with fluorescein as a hydrophilic substance revealed aggregation of particles and their binding to the cell membranes. Because of their hydrophilic profile, antidotes for organophosphate poisoning have a low bioavailability. Thus, silica nanoparticles and alginate microparticles can be used as colloidal vectors for oximes and pyridostigmine, improving their bioavailability. Moreover, silica nanoparticles can penetrate the cell membrane, carrying the active substance to a specific site of action.

Keywords: oxime, pyridostigmine, silica nanoparticles, nanotechnology, confocal microscopy



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