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UNLOCKING THE POWER OF RETINOIDS

Cosmetologist Alexandra Calka considers tackling pigmentation with retinoids and liposomes

ALEXANDRA CALKA

Alexandra Calka is a cosmetologist with more than 12 years of experience in the industry and she holds a bachelor’s degree in cosmetology. She is the chief executive and educator at SkinEdu.co.uk and the owner of the multi-award-winning skin clinic Coco Beauty Clinic.

Skin problems, regardless of their nature, usually have a S complex pathogenesis. One such multifactorial problem is hyperpigmentation. Discolouration is a topic that constantly arises in our work, especially after the summer.

Over the past few years, I have had the opportunity to assist numerous patients facing the challenge of discolouration. Throughout this time, I have extensively explored various techniques and tools to address this issue, including chemical peels, microneedling, collaborative efforts with dermatologists, and laser therapy.

Unfortunately, I have found that therapies focused on removing the pigment did not yield the desired outcomes. It is likely that the inflammation triggered after these procedures led to the emergence of new discolouration. Instead, treatments specifically designed to brighten the skin, harmonise its colour, and minimise discolouration (without complete removal) proved to be significantly more effective.

ETIOLOGY OF SKIN DISCOLORATION

The causes of discolouration can be divided into two categories -endogenous (hormonal disorders, autoimmune diseases, inflammation) and exogenous (UV radiation, medications). In practice, however, both factors may overlap. 

The melanogenesis process is indeed complex, posing a challenge when attempting to halt melanin synthesis. However, this complexity also presents an opportunity to intervene in the process. In addition to traditional methods of exfoliation, the use of melanogenesis inhibitors can also contribute to the reduction of discolouration.

Melanogenesis inhibitors are substances that interfere with the production of melanin, the pigment responsible for skin colour. By targeting key enzymes or receptors involved in melanin synthesis, these inhibitors can help regulate the process and minimise excessive pigmentation.

Commonly used melanogenesis inhibitors include ingredients like hydroquinone, kojic acid, arbutin, liquorice extract, and vitamin C. These substances work by inhibiting specific enzymes involved in melanin synthesis, such as tyrosinase.

THE PATHOGENESIS OF HYPERPIGMENTATION

Melanogenesis is a complex process involving various enzymatic and chemical reactions. The enzymes tyrosinase, TRP-1, and TRP-2 play a crucial role in melanin synthesis. The transformation of tyrosinase into L-DOPA and DOPAquinone leads to the formation of eumelanin (found in black skin) and pheomelanin (found in fair skin). Melanin is primarily responsible for the pigmentation of human skin, eyes, and hair. Melanocytes in the epidermis produce melanin, which is then transported to neighbouring keratinocytes.

Under normal conditions, melanin production provides photo-protection to the skin by absorbing harmful UV radiation. However, excessive melanin production can lead to dermatological issues such as freckles, solar lentigo, and melasma. Therefore, controlling melanogenesis is important in managing these skin conditions.

By understanding the intricacies of melanogenesis, researchers have identified various melanogenesis inhibitors that can interrupt the process. These inhibitors target enzymes like tyrosinase, preventing the synthesis of melanin. This can help reduce excessive pigmentation and contribute to a more even skin tone.

In conclusion, the complexity of melanogenesis offers both challenges and opportunities in managing pigmentation issues. By utilising melanogenesis inhibitors and other treatments, it is possible to regulate melanin synthesis and address skin discolouration effectively.

WHY DOES DISCOLOURATION RETURN?

Discolouration may recur under the influence of re-stimulation by exogenous factors such as UV radiation or endogenous hormonal changes. Many years of experience in working with patients struggling with the problem of discolouration have shown me that pigmentation changes are very difficult to completely remove. The altered melanocyte metabolism and increased tyrosinase activity are difficult to reverse completely, and the effect visible in the form of a spectacular brightening is most often associated with the superficial removal of accumulated pigment. In the search for effective solutions in the fight against discolouration, products containing retinoids in liposomal form turned out to be very effective.

WHAT ARE LIPOSOMES?

For many years, professionals have been struggling with the problem of developing an efficient method of applying active substances to the skin. The lipophilic nature of the outer layers of the skin makes the penetration of many compounds into the skin difficult and sometimes even impossible, which is why some treatments for discolouration may be ineffective.

That’s why Alex Bangham’s discovery of the structure of the liposome was revolutionary. Liposomes are closed, spherical vesicle-shaped structures with sizes ranging from a few nanometers to one micrometre. In the lipid bilayer from which they are built, the polar heads of the phospholipids protrude outwards, and the hydrophobic carbohydrate chains are directed inwards. This structure of the liposome enables the transport of lipophilic compounds inside and hydrophilic compounds in the liposome core.

Liposomes are composed mostly of phospholipids and cholesterol, forming similar structures to cell membranes.

Liposomes have been used in the cosmetic and drug industries because they can carry and protect encapsulated substances, improve the solubility of certain substances, and provide controlled drug release.

After applying the preparation to the surface of the skin, several actions occur between the epidermal cells and liposomes, such as: -adsorption on the surface of keratinocytes and slow release of the active substance,

-lipid transfer between liposomes and keratinocyte cell membranes,

-endocytosis -absorption into the cell and release of the contained substance,

-fusion of lipids forming liposomes from the cell membrane,

-contact release -the release of active substances after contact between the liposome and the cell membrane.

LIPOSOMAL RETINOIDS IN DEPIGMENTING THERAPIES

Retinoids which are derivatives of vitamin A, are used to treat various pigmentation disorders like melasma and post-inflammatory hyperpigmentation. It causes inhibition of tyrosinase and epidermal melanin dispersion. Retinoids may also interfere with pigment transfer to keratinocytes and accelerate pigment loss by causing the epidermis to be shed more quickly. Retinoid use over a prolonged period causes increased stratum corneum compaction and decreased melanin content.

The most popular pigmentation treatment in both professional and home care is retinol. Retinol is highly sensitive to light and oxygen. Liposomes are an effective tool for the protection of retinol against oxidation by light, and the addition of sterols into liposomes can delay oxidation.

Thanks to the use of nanotechnology and the closure of retinoids in liposomes, the skin does not exfoliate rapidly and is not irritated, unlike peeling with a traditional form of retinol. Liposomal peeling works deeper, it releases more slowly and is less irritating.

Thanks to the use of a liposomal form of retinoids in professional treatments for pigmentation as well as in-home cosmetics, they gain in effectiveness. Thanks to adsorption, endocytosis, fusion and contact release properties pigmentation can be treated at all skin levels bringing spectacular results for longer.

SUMMARY

Hyperpigmentation is a complex skin condition that requires a comprehensive approach for effective treatment.

It is important to ensure that active ingredients can penetrate every layer of the skin to target the underlying causes of hyperpigmentation. In addition to exfoliating the already-formed pigment, it is crucial to inhibit the activity of tyrosinase, the enzyme involved in melanin synthesis.

Modern therapies often utilise retinoids enclosed in liposomes, which provide a safe and highly effective alternative to more invasive treatments. These liposomes help deliver the active ingredients directly to the target areas, maximising their effectiveness.

However, it is important to note that the treatment of hyperpigmentation requires regularity and consistency. Close cooperation between the cosmetologist and the patient is necessary, particularly in terms of home care, supplementation, and lifestyle adjustments. Following a disciplined skincare routine and adhering to the recommended treatments and guidelines will yield better results in managing hyperpigmentation.

In conclusion, treating hyperpigmentation requires a multifaceted approach that addresses both exfoliation and tyrosinase inhibition. Utilising advanced treatments such as liposomal retinoids can provide safe and effective results. However, the key to success lies in the regularity of treatments and the collaboration between the cosmetologist and the patient in terms of skincare and lifestyle maintenance. 

This article appears in November/December 2023

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This article appears in...
November/December 2023
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