Niacinamide: Vital Vitamin B3 Derivative for Radiant Skin

The vitamins are integral to the maintenance of good health, though needed in micro amounts. Likewise, the amide form of Vitamin B3 i.e., Niacinamide (pyridine-3-carboxamide) is involved in various critical biochemical reactions in the form of NAD+, NADH, NADP+, or NADPH. Aging skin cells lose NAD+ and NADPH; thus, supplementing aging skin cells with topical application of niacinamide provides visible benefits to the appearance of skin along with improvement of all skin functions that rely on the pathways involving the above co-factors.

The dermatological effects include a reduction in hyperpigmentation, pore size, sebum production, melanosome transfer, a decrease in fine lines and wrinkles, prevention of UV-induced immunosuppression, and an improvement in the skin barrier by increased ceramide and protein production. Considering its effectiveness in the management of various skin disorders, making topical formulations that enhance niacinamide permeation and retention in the cutaneous environment can be of immense benefit. Hence, the following considerations can be of vital significance in formulating optimal delivery systems for niacinamide formulations.

Choosing the right concentration of niacinamide

Skincare products frequently include niacinamide in concentrations ranging from 2% to 10%, with 5% being the most prevalent. However, several factors need to be taken into consideration while determining the optimal concentration of niacinamide to use in formulations. Amongst these, skin type and product type constitute major influencers.

Though niacinamide is well tolerated in topical applications, formulations intended for use by sensitive skin individuals might be restricted to 2%. On the other hand, higher concentrations of niacinamide, such as 5-10% can be used for individuals with dry or normal skin. Similarly, formulations with a higher concentration of niacinamide may be used for leave-on products, such as moisturizers or serums while rinse-off products like cleansers may be formulated with lower concentrations.

Striking the right pH balance

The efficacy of niacinamide is significantly affected by the pH of the formulation. Majorly, niacinamide retains its effectiveness in the 5-7 pH range. Thus, formulations with pH below or above this pH range are not ideally suited for harnessing the therapeutic effects of niacinamide. In a highly acidic environment, niacinamide can be converted to niacin, which can generate a “flushing" sensation due to its ability to dilate blood vessels, eliciting an irritation response.

Miscibility constraints with oil or silicone-based delivery systems

Since niacinamide has high water solubility (212.95 mg/mL), incorporating it into an oil or silicone-based product can be challenging. Due to miscibility issues, it might not be evenly dispersed within the formulation, resulting in uneven application and reduced or no efficacy of niacinamide. To overcome these issues, appropriate emulsion systems with optimal emulsifiers, and surfactants may be designed, or encapsulation of niacinamide within silicone delivery systems can be an effective alternative for formulating a stable, homogenous, and effective product.

The purity of the niacinamide cannot be compromised

The pharmaceutical grade of niacinamide which is used for formulation must be highly pure and free from impurities. The presence of nicotinic acid or nicotinic acid esters can result in itching, reddening, or other irritating effects, even at doses less than 1%. Further, any microbial or heavy metal contamination, which occurs due to a lack of quality control measures during the manufacturing process can be toxic to the skin or body.

Compatibility with other ingredients in the formulation

Though niacinamide is a stable active and can be safely used with other actives or excipients in formulation, the product’s overall efficacy may be affected by interaction amongst the versatile ingredients. For instance, niacinamide interaction with benzoyl peroxide can convert it into benzoic acid, which is less active in fighting acne. Similarly, alpha hydroxy acids (AHA) such as lactic acid and glycolic acid can reduce the pH, lowering the efficacy of niacinamide. Likewise, anti-aging formulations which use copper peptides can exhibit reduced efficacy when combined with niacinamide. At high concentrations, the combination of retinol with niacinamide may elicit irritation or sensitization reactions.

Overall, the topical application of effective and stable formulations of niacinamide can be a vital skincare regimen to maintain nourished skin and protect against environmental damage.