Retinoids − natural and synthetic analogues of retinol (vitamin A) - provide numerous effects on human skin and are widely used in the treatment of various dermatological diseases.
Unlike drugs based on retinoids and vitamin A, in cosmetology and dermatology, retinoids are used mainly in the form of topical agents, most often in the form of creams or lotions.
Read the most up-to-date news from clinical trials on the effectiveness of retinoids on our estet-portal.com.
Vitamin A derivatives – main properties
Vitamin A (retinol) means all substances of animal origin that have the biological activity of the vitamin A complex. Among the most important forms of vitamin A are retinol, retinal, retinoic acid. Retinol is a fat-soluble vitamin found in animal products - milk, butter, eggs.
Synthetic retinoids have a therapeutic efficacy that is relative to vitamin A of animal or plant origin.
Unlike pharmacological products, which most often contain transretinoic acid (isotretinoin), cosmetic products contain retinoids with a less pronounced irritating effect - retinoic acid esters retinyl palmitate and retinyl acetate. Vitamin A itself is less commonly used – retinol. Both forms of vitamin A, retinol and retinoic acid, regulate many biological functions.
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Mechanism of action of retinoids
This process is associated with the activation of nuclear receptors with subsequent changes in the expression of a number of genes. The result of such exposure is a cascade of clinical, histological, immunological, biochemical and molecular changes that cover all living (including keratinized) skin cells. At the same time, it has been proven that retinoids act on skin cells both directly and indirectly through other cells.
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Topical (external) retinoids act through the RAR (retinoic acid receptors) and RXR (retinoid X receptors) receptors. RAR and RXR receptors have subtypes .alpha., .beta., .gamma. In human skin, RARγ and RXRα, but they are also associated with side effects when used (possibly itching, flushing).
RAR receptors provide a space for the formation of new synthetic retinoids with different or improved properties and stability. Cytoplasmic binding protein CRABP I and CRABP II (cellular retinoic acid binding protein) modulate the intracellular concentration of retinoic acid and affect its transport to the nucleus.
The effect of retinoids on the skin results in a range of clinical effects, including:
− change in skin color,
− accelerate regeneration,
− reduction of inflammatory processes,
− wrinkle smoothing,
− increase in elasticity and firmness,
Slight irritation and flaking of the skin may occur as side effects.
The effect of retinoids on skin cells
The development of the listed clinical effects is based on changes in skin cells controlled by retinoids. The most significant changes include:
1) Change in proliferation and differentiation of basal keratinocytes with inhibition of keratinization processes and acceleration of epidermal renewal.
2) Normalization of sebocyte proliferation with suppression of intracellular lipid synthesis, including triglycerides, fatty esters and acids.
3) Controlling the proliferation of hair follicle stem cells, stimulating the development of microcapillaries and improving blood supply to the hair papilla.
4) Modulation of the antigen representing the ability of cellular macrophages (Langerhans cells) to control the release of biologically active substances (interleukins, tumor necrosis factor, nitric oxide) involved in the inflammatory response.
5) Influence on the activity of tyrosinase - the enzyme responsible for the synthesis of melanin - in melanocytes.
6) Stimulation of fibroblast proliferation, collagen synthesis and suppression of the activity of enzymes (metalloproteinases) that destroy collagen, while simultaneously stimulating the synthesis of glycosaminoglycans - an important component of the dermal matrix.
Possibilities of using retinoids in dermatology
The implementation of these effects provides support for physiological processes in skin cells, as well as active recovery of soft tissues after injury and damage. Due to these properties, retinoids are widely used in the treatment of dermatological diseases such as psoriasis, acne, hyperkeratosis, eczema, burns and wounds.
In cosmetology, retinoid-based products are actively used to treat acne, as well as to prevent skin aging and fight age-related changes. Retinoid-based products used in cosmetology are called retinoivim cosmetic preparations.
Cosmetic applications for retinoids
Getting on the skin, retinoids are actively absorbed into the epidermis and dermis. The action of drugs in the epidermis is associated with the normalization of the processes of pigmentation and keratinization, in the dermis - with the restoration of the intercellular substance, protects the skin from age-related and photoaging. The penetration of retinoids into the hair follicles leads to the normalization of the activity of the sebaceous glands and contributes to the treatment of acne.
Proven effective photoaging prevention strategies
Given the less pronounced ability of retinoic acid esters to penetrate human skin, when creating retinoic cosmetics, it is very important to choose the right concentration of the active substance and the selection of auxiliary components (bases, emulsifiers, antioxidants, vitamins, plant extracts). Usually, the concentration of retinoids depends on the purpose of the product - it is higher in restorative and lower in preventive products.
With the correct application of these drugs, clinically positive results can be achieved in patients with various skin diseases.
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