Encapsulation of fluorogenic probes and pharmacologically active molecules into nanoparticles for enhancing cellular uptake

Abstract : Polymeric nanoparticles have been considered to have the potential to improve drug delivery to the desired site of action and to enable delivery of poorly soluble, poorly absorbed or unstable drugs. In this work, two types of active substances have been chosen for encapsulation in polymeric nanoparticles: fluorogenic probes for intracellular targeting of the reduced glutathione (GSH), namely ortho-phthaldialdehyde (OPA) and naphthalene-2,3-dicarboxaldehyde (NDA), as well as salmon calcitonin (sCT) which is a polypeptide hormone. The probe or sCT-loaded nanoparticles were obtained using a simple or double emulsion solvent evaporation method, respectively. The obtained nanoparticles were thoroughly characterized, e.g. in terms of the size, zeta potential, encapsulation efficiency, drug (probe) release, cytotoxicity or microscopic morphology and thermal properties. NDA-loaded nanoparticles were incubated with yeast cells and intracellular NDA-GSH adduct levels increased by about 9-times in comparison with the free probe. In the case of sCT, the in vivo study was conducted in rats, and it was demonstrated that after subcutaneous injection of sCT-loaded nanoparticles, elevated serum sCT levels could be sustained for 3 days. In conclusion, the active molecules incorporated in polymeric nanoparticles achieved the better cellular uptake (NDA) and bioavailability (sCT) that the non encapsulated ones.
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Eliza Anna Martenka. Encapsulation of fluorogenic probes and pharmacologically active molecules into nanoparticles for enhancing cellular uptake. Human health and pathology. Université Henri Poincaré - Nancy 1, 2009. English. ⟨NNT : 2009NAN10065⟩. ⟨tel-01748351⟩

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