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Retinoids (Vitamin A)

Vitamin A has made its way into an increasing number of skincare products. Retinoids can be defined as the group of compounds that are based on a core structure of Vitamin A (all-trans-retinol) including its metabolites, as well as synthetically derived compounds that mimic naturally occurring retinol structures. Retinol is a milder version of retinoids and quite effective to reverse sun damage, ageing skin, treating acne and even psoriasis. While tretinoin must be prescribed by board certified dermatologists, retinol is over-the-counter product. Retinol is more active than retinyl palmitate and other ester forms of retinoids. 

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Vitamin A cannot be synthesised in the body, hence needs to be ingested or applied topically. 

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With regards to concentrations used within formulations, the following has been identified in research :

  • Retinol is clinically in low concentration 0.5 - 1%

  • Retinaldehyde is clinically effective at 0.05%

  • Retinyl palmitate requires a higher concentration of 2% to be clinically effective

 

Physical Characteristics

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Physical characteristics of vitamin A are:

  • Have a low stability when exposed to light, heat and oxygen

  • Hydrophobic/lipophilic agent, therefore, have the ability to morph themselves to diffuse through water soluble phases of the skin which can penetrate through both sebaceous glands and intracellularly

  • Can diffuse into the stratum corneum rapidly and then slow in pace when entering the epidermis and dermis

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Classification

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  • Metabolic Peeling Agent

  • Cosmeceutical ingredient

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Mechanism of Action

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Regulation of Epidermal Proliferation and Differentiation

  • Accelerate the shedding of corneocytes

  • Reduce the formation of comedones due to hyperplastic response

  • Regulates keratinocytes differentiation

  • Encourages differentiated cells to release more EGF (Epidermal Growth Factor) to continue the wound healing process and epidermal turnover

  • The stratum granulosum become thicker and keratinocyte size is enlarged with increase adhesion

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Up-Regulation of Collagen Synthesis

  • Stimulates the synthesis of TGF by both keratinocytes and macrophages

  • This stimulates collagen types I and III, and fibronectin synthesis by fibroblasts

  • Regulates the activation of MMP (matrix metalloproteinases) by inhibition of gene transcription of the keratinocytes

  • This results in a more organised, dense and parallel arrangement of collagen fibres

  • Collagen type VII production is also stimulated which forms the anchoring filaments of the dermo-epidermal junction

  • Glycosaminoglycans deposition also increases

 

Regulation of Angiogenesis

  • Regulates the response of Vascular Endothelial Growth Factor

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Regulation of Immune Responses

  • Modulation of neutrophil and leukotriene infiltration into tissues

 

Anti-Inflammatory Effects

  • Inhibits the mass infiltration of inflammatory mediators such as leukotrienes and leukocytes

  • Down regulate the inflammatory response initiated by Propionibacterium acnes​​​ (P. acnes)

  • Decreases levels of the pro inflammatory cytokine TNF

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Induction of Apoptosis

  • Help for the treating warts or any hyperproliferation on the skin

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Inhibits Tyrosinase Activity

  • Reduces pigmentary changes in the skin via reducing the expression of tyrosinase

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Mild Antibacterial Effects

  • Retinaldehyde

  • Against Gram positive bacteria such as P. acnes

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Clinical Indicators

It can be use in treating clinical conditions characterised by defective differentiation, DNA damage or those that require regulation, such as:

  • Photo-ageing

  • Acne

  • Thickened, rough skin texture such as warts, corn, callus

  • Vascular insufficiency

  • Thin skin

  • Post Inflammatory Hyperpigmentation

  • Melasma

  • Psoriasis

  • Dermatitis

  • Rosacea

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Contraindications

 

Vitamin A derivatives are contraindicated to

  • Pregnancy

  • Breastfeeding

  • Severe liver disorders

  • Photosensitising medication

  • Retinol based products must be ceased 3 days prior to and after chemical peeling procedures

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Application​

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Vitamin A derivatives is a powerful compound and can cause irritation, flaking and drying the skin. In contrary, that is the way it works. The safest way to use vitamin A product is by starting from the lowest percentage possible and build your skin tolerance up will eventually take you there. Apply every second or third night at first for one month before you use it more frequently. Then, when you go to the higher concentration, start applying every second or third night again and so on. If there are any irritation, just slow down with less application. 

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Vitamin A and it's derivatives must be use at night only. If use during day time, it will be deactivated by sun exposure and such a waste of your money. Since its exfoliate your skin while you are sleep at night, it'll cause your skin more sensitive to sunlight. Therefore, daily application of sunscreen is non-negotiable, otherwise, it will be pointless. 

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