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Use of LC ‐ MS analysis to elucidate by‐products of niacinamide transformation following in vitro skin permeation studies
Author(s) -
Sil B. C.,
Moore D. J.,
Lane M. E.
Publication year - 2018
Publication title -
international journal of cosmetic science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.532
H-Index - 62
eISSN - 1468-2494
pISSN - 0142-5463
DOI - 10.1111/ics.12486
Subject(s) - niacinamide , in vitro , chemistry , transformation (genetics) , permeation , biochemistry , chromatography , nicotinamide , membrane , enzyme , gene
Objective To explore and elucidate the formation of niacinamide ( NIA ) by‐products during in vitro skin permeation studies using liquid chromatography coupled to mass spectrometry ( LC ‐ MS ) analysis. Methods Porcine skin permeation studies of various NIA formulations were conducted using Franz diffusion cells for a period of 24 hours. NIA by‐products were identified by LC , extracted and further qualitatively analysed by LC ‐ MS . Results Analysis and characterisation of NIA by‐products using LC ‐ MS resulted in the identification of different molecular entities with similar structures to NIA . The most prevalent molecular specie in this study was 1,4,5,6‐tetrahydropyridine‐3‐carboxamide with the highest ion abundance. Other structural NIA analogues were also identified and reported, namely piperidine‐3‐carboxamide and 1,4‐dihydropyridine‐3‐carboxamide. None of these NIA derivatives were detected in stability studies of NIA in the medium used as the receptor phase, phosphate buffered saline ( PBS ), that had not been in contact with skin. Conclusion The comparatively low recovery of NIA following in vitro mass‐balance and permeation studies for pseudo‐finite and finite dosing of the active compared with infinite dosing is attributed to chemical derivatisation of the molecule during skin penetration. These findings reported here will allow the development of more sensitive methods to ensure full mass balance recovery of NIA following topical application of NIA preparations.