Tocophersolan CAS:9002-96-4 Promotes penetration + inhibits efflux, an efficacy enhancement solution that allows active ingredients to "penetrate and stay"
Publish Time:
2025-08-19
In the efficacy skincare arena, the 'actual effectiveness' of active ingredients is far more valuable than the 'added concentration'.
Many active ingredients struggle to deliver their intended effects due to poor skin penetration and insufficient retention, becoming a critical bottleneck for product effectiveness. Tocophersolan (TPGS), with its dual enhancement mechanism of 'promoting penetration + inhibiting efflux,' allows active ingredients to both penetrate and remain, redefining the delivery efficacy of active ingredients.
What is Tocophersolan?
Tocophersolan, also known as TPGS, Polyethylene Glycol 1000 Vitamin E Succinate, is a derivative of Vitamin E, formed by the esterification of hydrophilic polyethylene glycol (PEG) and lipophilic tocopherol succinate (TAS). This unique amphiphilic structure allows it to be both oil-friendly and water-embracing, easily breaking through skin absorption barriers.
As a 'senior ingredient' with over 70 years of safe application history, Tocophersolan's safety and suitability have been certified by multiple global authorities: it is not only included in the 'United States Pharmacopeia' and approved as a pharmaceutical excipient by the US FDA and China's NMPA, but also explicitly recognized by the European Food Safety Authority as a food ingredient for specific nutritional uses in children. Additionally, it has been confirmed safe for use in cosmetic formulations by the Cosmetic Ingredient Review (CIR) in the United States and is included in China's list of used cosmetic ingredients.
TPGS application in Medicines & Food product
Domestic and international literature confirms its efficacy-enhancing value:
Dual Enhancement: Allows active ingredients to 'penetrate and remain'
The difficulty in achieving efficacy with cosmetic active ingredients mainly faces three major challenges:
1. The lipophilic structure of the stratum corneum forms a physical barrier to hydrophilic active ingredients, resulting in low skin penetration rates;
2. The P-glycoprotein 'efflux pump' on cell membranes 'pumps out' active ingredients that enter the cell, leading to insufficient retention;
3. Traditional penetration enhancers such as ethanol come with irritation risks, making them undesirable for sensitive skin.
Tocophersolan is an 'all-around player' for solving these problems, with unique advantages:
1. Penetration Enhancement: Its amphiphilic structure enhances the fluidity of the skin's lipid bilayer, reduces interfacial tension, and promotes the penetration of active ingredients into cells, like opening a 'green channel' for them.
2. Retention Enhancement: It also inhibits the efflux action of P-glycoprotein, greatly increasing the retention of active ingredients within cells and improving bioavailability.
3. It is gentle, low-foaming, non-irritating, and has the skincare benefits of tocopherol itself. Its antioxidant properties can also protect easily degradable ingredients and increase the stability of formulations, making it suitable for all skin types.
Efficacy-enhancing value in multi-scene applications
1. Direct Proportion Compound: Amplifies the efficacy of active ingredients
In cosmetic applications, Tocophersolan can significantly amplify efficacy when compounded with active ingredients in proportion.
Experimental data shows that the combination of Tocophersolan + Resveratrol results in a skin retention amount that is 4 times , and a cell retention amount that is increased by 4.37 times 。
When paired with Glycyrrhiza glabra, its melanin inhibition effect far exceeds Bis-Diethoxy Diglycol Cyclohexane 1,4-Dicarboxylate, soybean lecithin, and other penetration enhancers.
2. Carrier Modification: Upgrades delivery efficacy
Using Tocophersolan to modify liposomes can also achieve enhanced delivery. At the same peptide concentration, the ability of its modified liposomes to inhibit melanin synthesis is 4 times above that of alcohol and aqueous solutions.
3. Solubilization
In addition, its solubilization ability is also excellent, and its low foaming properties make the product feel better to use.
With this 'efficacy-enhancing partner,' skincare products can truly achieve 'applied = absorbed = retained.' Today, Tocophersolan has become a key ingredient for many leading brands and is widely used in popular products for whitening, anti-wrinkle, and repair.
Please contact us for detailed information and samples.
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