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96 DERMOCOSMETICS


As a result, APPS was found to penetrate the dermis, functioning more effectively in the epidermis and dermis than other vitamin C derivatives, including ascorbyl glucoside (AG) and ascorbyl tetraisoparmitate (VC-IP) (Figure 2). Owing to this high performance,3 dermocosmetic products containing APPS have been developed for adoption in aesthetic medicine and beauty salons.


APPS and TPNa for acne care Millions of individuals worldwide suffer from acne, a prevalent dermatological ailment, increasing the demand for products that can successfully control and treat its symptoms. The factors associated with acne include environmental factors, such as UV radiation, air pollution, tobacco consumption, psychological stress, diverse microorganisms, and nutrition. Vitamins and their derivatives have the potential to counteract the oxidative stress and inflammation triggered by UV.4 For example, research indicates that TPNa


suppresses the inflammation caused by UV-B produced in cells under oxidative stress. To evaluate this, normal human epidermal keratinocytes were precultivated in growth media until confluent, after which TPNa, TAc, or dipotassium glycyrrhizinate (G2K), a commonly used anti-inflammatory drug, was added (Figure 3). Approximately 24 hours after administration, the cells were exposed to UV-B (60 mJ/cm2


),


and the culture medium was collected. The anti-inflammatory effects of secreted


prostaglandin E2 (PGE2), an inflammatory marker, were assessed using an enzyme-linked immunosorbent assay. TPNa was found to suppress PGE2 production, whereas TAc and G2K exhibited little to no suppressive activity (Figure 3). Owing to its strong anti-inflammatory effects,


TPNa is widely used in acne care products. Some dermatological clinics offer cosmetic treatments for acne in combination with oral medicinal care. Dr. Ikeno, a well-known dermatologist specializing in acne treatment, reported at the conference of the Society of Investigative Dermatology (SID) that TPNa had a significant effect on erythema in post-inflammatory acne lesions (efficacy rate of the acne symptoms: 1% TPNa lotion, 73.7%; vehicle lotion, 35.3%; 40 patients, 4-week-treatment).4 This might have been achieved by the high


anti-oxidative and anti-inflammatory effects of TPNa (Figure 3). It was formulated in a watery lotion formula (approximately 2%), which required a high solubility, since individuals with acne tend to not use oily formulations, such as creams. Figure 4A shows the significant example of acne patient using TPNa cosmetic lotion for one month. Dr. Ikeno found that TPNa- containing cosmetics are especially suited for initial acne care, treating erythema and inflammation. After this initial treatment, APPS plays a role in subsequent acne symptoms. Owing to their ability to scavenge oxidants on the skin, such as reactive oxygen species (ROS),3


ascorbyl


phosphate derivatives, including APPS, can be used to treat acne (Figure 4B). A previous clinical test report also revealed


PERSONAL CARE April 2025


Figure 1: The vitamin derivatives TPNa and APPS can penetrate the epidermis via the stratum corneum more effectively than vitamin C and E alone


that the combination of topical application and iontophoresis therapy with a 1% APPS lotion was effective for both acne and erythema around acne lesions. RGB analysis of the effects of APPS on acne lesions showed a reduction in inflammation to 67% of the initial inflammation at 2 months and 47% at 4 months, highlighting the rapid results of APPS compared to other provitamins.5


APPS and TPNa: Fine-line erasers for anti-ageing dermocosmetics products A common sign of ageing is crow’s feet around the eyes. Responses to a survey demonstrated that the eye area is prone to issues including fine lines (56.8%) and dryness (55.7%). Moisturizing the skin is one way to improve fine lines since wrinkles are mainly caused by the degradation of cellular matrix components,


80 70 60 50 40 30 20 10 0


-10 60.3 44.4


including collagens and elastins, due to photoageing induced by UV-A radiation. Free radicals, primarily ROS induced


by UV-A radiation, play important roles in photoageing. TPNa promotes ceramide synthesis and improves trans-epidermal water loss,6


whereas APPS improves skin dryness


through anti-oxidative efficacy.1,3 This suggests that both of the vitamin


derivatives established here may act as active anti-fine line ingredients by improving skin hydration. Wrinkles are more closely related to dermal structural ageing than to superficial hydration. At this point, APPS could be effective because it promotes collagen synthesis by permeating deep into the skin, where collagen-generating fibroblast cells exist.3 A previous study found that APPS suppresses superoxide production and


9.8 0.2


APPS 0.5%


APPS 1%


Ethyl As 1%


0.2


Ethyl As 2%


0.0


VC-IP 1%


0.0


VC-IP 3%


0.0


GO-VC 0.5%


0.0


GO-VC 1%


AG 2%


Figure 2: Graph showing the release of vitamin C (AsA) after 24 hours of topical application of vitamin C derivatives on the reconstructed skin model. Once applied onto the skin, the vitamin derivatives penetrate the skin and are digested by epidermal enzyme into vitamin C. Abbreviations; Ethyl As: ethyl vitamin C, VC-IP: ascorbyl tetraisoparmitate, GO-VC: caprylyl 2-glyceryl ascorbate and AG: ascorbyl glucoside


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Released ASA (nmol/wel)


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