Abstract

Niacinamide (NIA) is the amide form of vitamin B3 and has been widely used in pharmaceutical and personal care formulations. Previously, we reported a comparative study of NIA permeation from neat solvents using the Skin Parallel Artificial Membrane Permeability Assay (PAMPA) and mammalian skin. A good correlation between NIA permeation in the different models was found. In the present work, ten binary and ternary systems were evaluated for their ability to promote NIA delivery in the Skin PAMPA model, porcine skin and human epidermis. Penetration enhancement was evident for binary systems composed of propylene glycol and fatty acids in human skin studies. However, propylene glycol and oleic acid did not promote enhancement of NIA compared with other systems in the Skin PAMPA model. A good correlation was obtained for permeation data from Skin PAMPA and porcine skin. However, data from the Skin PAMPA model and from human skin could only be correlated when the PG-fatty acid systems were excluded. These findings add to our knowledge of the potential applications of Skin PAMPA for screening dermal/transdermal preparations.

Highlights

  • Niacinamide (NIA) is the water-soluble form of vitamin B3 (Figure 1)

  • The results obtained in this study suggested that the Skin Parallel Artificial Membrane Permeability Assay (PAMPA) model is not a suitable model for screening such combinations

  • The influence of binary and ternary solvents on the in vitro permeation of NIA was assessed in the Skin PAMPA model, porcine skin and heat separated human epidermis

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Summary

Introduction

Niacinamide (NIA) is the water-soluble form of vitamin B3 (Figure 1). The authors assessed the corneocyte maturity and surface area from NIA treated and untreated (control) areas, as well as trans-epidermal water loss (TEWL). The thickness of the SC before and after the application of NIA was determined using confocal Raman spectroscopy (CRS). The NIA treatment decreased TEWL values, increased the thickness of the SC, and larger and more mature corneocytes were found in the treated versus control sites. Pre-coated PAMPA Plates (Pion Inc. PN120657), hydration solution, stirring disks and a Gut-BoxTM device were o2b.2t.aMineisdcifbriolimty panIOd NStaIbnicli.tByiSllteurdicieas, MA, USA. Were analyzed using the HPLC method validated earlier with a Kinetix® 5 mm Phenyl-Hexyl 250 × 4.6 mm reversed column (Phenomenex, Macclesfield, UK) with water:methanol (80:20) as the mobile. The column temperature was set to 30 ◦C and the UV detection wavelength was 263 nm [8]

The Skin PAMPA Permeation Studies
Permeation Studies in Porcine and Human Skin
Data Analysis
Stability Determination
Skin PAMPA Permeation Studies
Porcine Skin Permeation and Mass Balance Studies
Conclusions
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