Development and evaluation of niacinamide transdermal formulation by artificial membrane permeability

Despite many efforts to improve the transdermal permeability of drugs, most of them are blocked by the skin barrier. Niacinamide (NAC) is a Biopharmaceutics Classification System class I drug with high aqueous solubility and intestinal permeability. Due to the high solubility and intestinal permeability of NAC, the development of new formulations is insufficient as transdermal, injection etc. Thus, this study aimed to develop the novel NAC formulation with improved skin permeability and secured stability. The NAC formulation approach is to first select a solvent that improves skin permeability, and then select a second penetration enhancer to determine the final formulation. All formulations were evaluated for skin permeability using an artificial membrane (Strat-M®).

The optimal formulation (non-ionic formulations (NF1) consisted of NAC/Tween®80 = 1:1 weight ratio in dipropylene glycol [DPG]) showed the highest permeability in all formulations in PBS buffer (pH 7.4). The thermal properties of NF1 were altered. Moreover, NF1 maintained a stable drug content, appearance, and pH value for 12 months. In conclusion, DPG had an excellent effect in increasing the NAC permeation, and Tween®80 played a boosting role. Through this study, an innovative NAC formulation was developed, and good results are expected for human transdermal research.

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Materials

Niacinamide 99.5% (nicotinamide, NAC), hexadecyltrimethylammonium bromide 98.0%, benzalkonium chloride 95.0%, alkyltrimethylammonium bromide 95.0%, dodecylamine 98.0%, cetylpyridinium chloride 98.0%, sodium dodecyl sulfate (SDS) 98.5%, Tween®80 (polysorbate 80), Tween®20 (polysorbate 20), Span®20 (sorbitan laurate), phosphate-buffered saline (PBS pH 7.4) powder, and Strat-M® Membrane (25mm) were purchased from Sigma-Aldrich Inc. (St. Louis, MO, USA). TEGOSOFT® CT was obtained from Evonik (Essen, Germany). Butylene glycol 99.0% (BG), dipropylene glycol 97.0% (DPG), and propylene glycol 99.0% (PG) were purchased from Samchun Pure Chemical Co., Ltd. (Pyeongtaek, Korea). Polyethylene glycol 400 was purchased from Junsei Chemical Co., Ltd. (Tokyo, Japan). Polyoxyethylene (160) and polyoxylpropylene (30) glycol (Kolliphor® P188), polyoxyethylene (196) and polyoxylpropylene (67) glycol (Kolliphor® P407), Polyethylene glycol 6000 (PEG6000), polyvinyl alcohol-polyethylene glycol graft copolymer (Kollicoat® IR), polyvinylpyrrolidone (Kollidon® K12), macrogol 15 hydroxystearate (Kolliphor® HS 15), polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus®), and D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) were obtained from BASF (Ludwigshafen, Germany). PVP/VA S-630 was obtained from ISP Technologies Inc. (Wayne, NJ, USA).

Jeong Sun Sohn, Jin-Seok Choi, Development and evaluation of niacinamide transdermal formulation by artificial membrane permeability, Saudi Pharmaceutical Journal, 2023, ISSN 1319-0164, https://doi.org/10.1016/j.jsps.2023.05.018.

See also the interesting video on Vitamin E TPGS: