Are in situ formulations the keys for the therapeutic future of S-nitrosothiols? - Université de Lorraine Access content directly
Journal Articles European Journal of Pharmaceutics and Biopharmaceutics Year : 2013

Are in situ formulations the keys for the therapeutic future of S-nitrosothiols?

Abstract

S-nitrosoglutathione (GSNO) and S-nitroso-N-acetylpenicillamine (SNAP) were formulated into in situ forming implants (ISI) and microparticles (ISM) using PLGA and either N-methyl-2-pyrrolidone (NMP) or triacetin. Physicochemical characterization was carried out, including the study of matrix structure and degradation. A strong correlation between drug hydrophobicity and the in vitro release profiles was observed: whatever the formulation, GSNO and SNAP were completely released after ca. 1 day and 1 week, respectively. Then, selected formulations (i.e., SNAP-loaded NMP formulations) demonstrated the ability to sustain the vasodilation effect of SNAP, as shown by monitoring the arterial pressure (telemetry) of Wistar rats after subcutaneous injection. Both ISI and ISM injections resulted in a 3-fold extended decrease in pulse arterial pressure compared with the unloaded drug, without significant decrease in the mean arterial pressure. Hence, the results emphasize the suitability of these formulations as drug delivery systems for S-nitrosothiols, widening their therapeutic potential.
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Dates and versions

hal-01273175 , version 1 (12-02-2016)

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Marianne Parent, Ariane Boudier, François Dupuis, Cécile Nouvel, Anne Sapin, et al.. Are in situ formulations the keys for the therapeutic future of S-nitrosothiols?. European Journal of Pharmaceutics and Biopharmaceutics, 2013, 85 (3), pp.640-649. ⟨10.1016/j.ejpb.2013.08.005⟩. ⟨hal-01273175⟩
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