Products Cited in Publications Worldwide Novel Naproxen Salts with Increased Skin Permeability

Novel Naproxen Salts with Increased Skin Permeability

Swiatek, Ewelina; Ossowicz-Rupniewska, Paula; Janus, Ewa; Nowak, Anna; Sobolewski, Peter; Duchnik, Wiktoria; Kucharski, Lukasz; Klimowicz, Adam

DOI: PMID:

Abstract

The paper presents the synthesis, full identification, and characterization of new salts-L-proline alkyl ester naproxenates [ProOR][NAP], where R was a chain from Et to Bu (including isopropyl). All obtained compounds were characterized by NMR (NMR), Fourier transform IR spectroscopy (FTIR), X-ray powder diffractometry (XRD), and in vitro dissolution studies. The sp. rotation, phase transition temperatures (m.p.), and thermal stability were also determined In addition, their lipophilicity, permeability, and accumulation in pigskin were determined Finally, toxicity against mouse L929 fibroblast cells was tested. The obtained naproxen derivatives showed improved solubility and higher absorption of drug mols. by biol. membranes. Their lipophilicity was lower and increased with the increase in the alkyl chain of the ester. The derivative with iso-Pr ester had the best permeability through pigskin. The use of L-proline iso-Pr ester naproxenate increased the permeation of naproxen through the skin almost four-fold. It was also shown that the increase in permeability is not associated with addnl. risk: all compounds had a similar effect on cell viability as the parent naproxen.

Keywords

amino acid ; ionic liquids ; naproxen ; nonsteroidal anti-inflammatory drug ; skin barrier ; transdermal drug delivery

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Naproxen

A29614822204-53-198%

Naproxen

211.0/1kg

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