Introduction

Ageing is an inevitable process in human life. However, the quest for youthful, healthy skin has been a driving force in human life and the field of cosmetic science. Nowadays, there has been spiking interest in moving towards natural remedies for skin rejuvenation as an alternative to synthetic chemicals and invasive procedures.

Human ageing is marked by wrinkles in the face, loss of elasticity, pigmentation, and more, but these are often influenced by factors such as environmental factors, sun exposure, time, genetics, pollution, and lifestyle choices. In searching for a remedy in a natural way, the grape seed extract garnered attention for its potential benefits in promoting skin health, and its combating natural signs in ageing processes.

This review aims to demonstrate the use of grape seed extract by exploring its bioactive components, mechanisms of action, benefits, and potential applications, providing a comprehensive understanding of how grape seed extract can be used in dermatology.

Historical context of grape seed for cosmetics

Vitis vinifera, commonly known as the grapevine, is native to southern Europe and Western Asia. Using grapes for cosmetic purposes dates back to Neolithic times and Greek philosophers believed that the extracts had healing powers.^1,2 

What are the active components in the grape seeds?

Grape seed extract is rich in various bioactive compounds which promote skin rejuvenation and other health conditions. The grapes have both phenolic and lipid components including flavanones, proanthocyanidins, anthocyanins, flavan-3-ols, stilbenes, flavanols, cinnamic acid derivatives, hydrobenzoic acid, fatty acids, phytosterols.

Among these, phenolic acids, flavonoids, anthocyanins, proanthocyanidins and stilbenes are considered major bioactive compounds in grapes.^3,4 These bioactive compounds contribute to health benefits, and they possess antioxidant, antimicrobial, anti-inflammatory, and anti-carcinogenic activities and have wide applications. The main bioactive components are as follows

• Proanthocyanidins: A powerful antioxidant, the most abundant and significant component, comprising up to 95% of the extract which helps in neutralizing free radicals, thereby reducing oxidative stress and preventing cellular damage, which is a major factor in skin ageing
• Flavonoids: Flavonoids, including catechins and epicatechins, enhance the skin's resilience to environmental damage and improve microcirculation, which helps in maintaining healthy skin tone and texture
• Polyphenols: Polyphenolic compounds such as resveratrol, offer anti-inflammatory and antimicrobial properties, further supporting skin health and potentially alleviating conditions like acne and rosacea

Benefits of grape seed extract

Grape seed extracts are widely recognized for their multiple benefits in promoting skin health and rejuvenation. Below are the key benefits that highlight its efficacy

• Neutralizing free radicals and protection against environmental damage
• Enhancing collagen production and stimulation of fibroblasts to maintain the skin integrity
• Anti-inflammatory effects by reduction of inflammation and alleviation of skin conditions like redness, swelling, and discomfort
• Improving skin hydration and elasticity which leads to softer, more supple skin, reducing dryness and rough texture
• Skin brightening and reducing hyperpigmentation by inhibiting the enzyme tyrosinase, which is involved in melanin production
• Improving blood circulation and cellular renewal helps to maintain a fresh and vibrant skin appearance
• Accelerates the skin’s natural healing processes by promoting cell regeneration and repair. Its role in collagen synthesis also aids in quicker recovery and better-quality healed skin and scar reduction

Mechanisms of action

The grape seed extract has been identified as a potential agent in the rejuvenation of skin health, particularly in maintaining skin elasticity, moisture content, and skin sebum content through various mechanisms. The main actions are through polyphenolic content including procyanidins, catechin, epicatechin, and gallic acid.

The bioactive components have

• Strong antioxidant protection and Free radicals’ activity
• Anti-inflammatory properties
• Collagen support⁵

Antioxidant and free radicals

The bioactive components increase the expression of decorin and biglycan, major proteins in the dermis which leads to skin elasticity. UV exposure generates reactive oxygen species (ROS), which lead to DNA damage, inflammation, and the breakdown of collagen. 

The oxidative stress damages the skin cells and tissues, and excessive production contributes to ageing. The antioxidant properties of grape seed extract are crucial in protecting the skin from oxidative stress, which is the causative factor in ageing and wrinkle formation in the skin by preserving the skin cells, integrity and function.

Grape seed extract contains high levels of proanthocyanidins, which neutralize free radicals, and reduce the reactive oxygen species and subsequent apoptosis in human keratinocytes exposed to UV radiation-induced skin damage.⁶

The grape seed inhibits the HYBID-mediated hyaluronan degradation which is the process implicated in skin wrinkling. The bioactive components from the grape seed extract by regulating the HYBID mRNA and protein expression, maintain the high -high-molecular-weight hyaluronan in the skin, contributing to hydration, firmness, and elasticity.⁷

Additionally, their ability to bind to bile acid and inhibit lipid digestion and absorption plays a role in preventing obesity and hyperlipidemia, indirectly supporting skin health by maintaining overall metabolic balance.₈ The synergistic effect of grape seed extract with other components in anti-ageing essences also repairs cells, improves metabolism, and activates aged cells, enhancing anti-oxidation and anti-ageing effects.⁹

Collagen synthesis

The collagen is a type of protein which makes up between 75% and 80% of your skin and these molecules are closely bound providing smooth, healthy, and highly elastic skin. Exposure to sunlight can break down the collagen bonds, which damages the appearance of the skin.

The grape seed’s proanthocyanidins stimulate the synthesis of collagen, which has been shown to bond with collagen fibres, and protect from degradation by enzymes like collagenases. This collagen synthesis action and protection of the existing collagen fibres enhances the skin elasticity and reduces the skin appearance of lines and wrinkles, which is a key indicator of youthful and healthy skin.

Application in skincare products

• Usage in creams and lotions: Grape seed extracts are the common ingredients in moisturizing creams and lotions. The fatty acids, such as linoleic acid, help to reinforce the skin barrier, maintaining hydration and preventing moisture loss
• Serums: The daily usage of serums typically contains higher concentrations of grape extracts compared to creams and lotions. They are designed for deeper penetration, allowing the active compounds to deliver more targeted benefits
• Face masks: The facet masks infused with grape extracts provide an intensive treatment that can boost skin radiance and hydration and nourishing ingredients deliver a concentrated dose of antioxidants and nutrients
• Sunscreens: The sunscreens incorporated with grape seed extracts enhance the skin's defence against UV radiation; well, it is not a replacement for traditional sun-blocking agents but provides additional protection by neutralizing free radicals generated by UV exposure

Complementary ingredients used with grape seed extract

To enhance the efficacy of skincare products, grape seed extracts are often combined with other beneficial ingredients. Its combination with other complementary ingredients and the ongoing innovations in formulation and delivery systems continue to enhance its effectiveness, making it a popular choice in the evolving landscape of skincare. The most common mix-ups are with hyaluronic acid, vitamin -C, Niacinamide, retinols are claimed to enhance the antioxidant synergy, moisture retention, brightening effect, and anti-ageing regimen.

Advantages of grape seed extract over the conventional treatments 

Clinical evidences

In one of the recent studies by Misbah et al, the development entailed extraction of grape seed extract from Vitis Vinifera shows a positive impact on slowing down skin ageing by countering the exogenous factors of oxidative stress and free radicals. The non-invasive technique from the study showed emulgel substantially reduced roughness, scaliness, winkles, and sebum content by 55%, 26%, 23.9% and 30.3% respectively enhancing elasticity and hydration by 50% and 32.2% respectively. It shows that it may be safe to incorporate bio-active botanical antioxidants for the evaluation of derma cosmetic benefits in the management of dehydrated and aged facial skin.¹⁰

The study by Kan Tao et al states that Protein phosphatase 2A (PP2A) is a master regulatory protein that plays a critical role in oxidative stress signalling. A novel grape seed extract called Activated Grape Seed Extract (AGSE), enriched for PP2A-activating flavonoids was demonstrated to have antioxidant and anti-inflammatory activities. The assessment of E-AGSE showed that it reduces wrinkling appearance, brightens the skin, and boosts hydration. It is also effective in sensitive skin, providing several benefits.¹¹

So far, the recent clinical evidence from human trials, animal studies, and in vitro research supports its efficacy in skin rejuvenation, demonstrating the tangible improvements in skin texture, elasticity, and reduction of wrinkles, enhanced collagen production, antioxidant activity, and anti-inflammatory effects. Future direction needs to augment the full potential of grape seed extracts and their applications in the field of dermatology.

Safety and adverse effects

Grape seed extracts are generally considered safe for both topical and oral use. However, understanding the toxicological profile is essential to ensure its safe application in skin care and therapeutic settings. Studies indicate that daily doses of up to 300 mg of grape seed extract are safe for most individuals, and must be supervised by a healthcare provider, which was commonly included in skincare products at concentrations ranging from 0.5% to 5%.

• Gastrointestinal disturbances: There may be some mild gastrointestinal issues such as nausea, stomach cramps, or diarrhoea when taking GSE orally
• Skin reactions: When taken topically, in rare conditions some may have redness, itching, and rash
• Interactions with medications: There may be a mild anticoagulant effect, which could potentially enhance the effects of blood-thinning medications and increase the risk of bleeding when taken orally
• Hormonal effects: Grape seed extract contains phytoestrogens with estrogen-like activity, generally beneficial but they might influence hormone-sensitive conditions
• Pregnancy and children: There is limited research on the safety of grape seed extract during pregnancy and breastfeeding and children

Summary

Grape seed extracts are renowned for their potent antioxidant, anti-inflammatory, and collagen-synthesis properties, making them a valuable ingredient in skin rejuvenation. The activities of proanthocyanidins, flavonoids, and others protect the skin from oxidative stress and enhance the skin's elasticity and hydration. Recent studies in the pharma world support its efficacy in reducing wrinkles, hyperpigmentation, and inflammation, with minimal side effects.

Its usage in various topical formulations like creams, serums, and grape seed extract offers a natural, effective alternative to conventional anti-ageing treatments, moreover, it aligns with growing trends in natural and sustainable skincare. The research should focus on optimizing the delivery systems, long-term effects and exploring synergistic combinations with other natural ingredients.