Cosmoceuticals

DR AARTHI MARIA FRANCIS MBBS (INDIA) MASTERS IN ANTI-AGEING, AESTHETICS & REGENERATIVE MEDICINE (UCSI) DIPLOMA IN DERMATOLOGY (WALES) DIPLOMA IN AESTHETICS (USA) http://www.skinkl.com/







Coined by Dr. Albert Kligman - 1980 Active cosmetics that have positive effects on the skin that go beyond cleansing or moisturization.

“Biological actives” that have “antiaging” effects





Global Regulatory Bodies do not recognize any such category as "cosmeceuticals.“ A product can be a drug, a cosmetic, or a combination of both, but the term "cosmeceutical" has no meaning under the law".

ď ˝

ď ˝

ď ˝

largely aimed at the demographic working to mitigate the visible signs of aging, including lines, wrinkles, laxity, coarsening and skin discoloration.

Cosmeceuticals are largely designed to mitigate the visible due to external factors & chronological/intrinsic, aging.

Myriad ingredients have been studied to address matrix degradation, textural changes and hyperpigmentation.

ď ˝

ď ˝

Many single ingredients, as well as blends, are used to prevent this breakdown in younger individuals and stimulate repair and strengthening in the skin of older patients.

Ingredients: broad-spectrum sunscreens, antioxidants; matrix metalloproteinase inhibitors (MMPi), collagen & matrix producers; depigmenting agents and lately stem cells

   

  

Preventing ultraviolet (UV) damage Reducing free radical formation Improving the skin lipid barrier Brightening and unifying skin tone and color Improving texture Reducing pore size Reducing fine lines and wrinkles

 



4 FDA approved ingredients zinc oxide, titanium dioxide, avobenzone & ecamsule Block UVA and UVB

ď ˝

1.

2.

3.

Three categories: primary antioxidants, or electron donors; secondary antioxidants - chelate metal ions co-antioxidants - facilitate other antioxidants.

   

    

Resveratrol Silymarin Caffeine Coffea arabica extract Ergothioneine Green tea Genistein L-ascorbic acid (vitamin C) Glutathione



 



Resveratrol – potent FR scavenger, 17x greater antiO2 activity Green Tea – rich in polyphenols Glutathione – cellular detoxification & inhibits tyrosine kinase Caffeine – thermogenic, used in focal fat loss & rx of cellulite

 

 

MMP activity is necessary to rid the skin of spent protein fragments UV exposure, increases the activity of these enzymes, leading to the breakdown of healthy, necessary matrix components - acceleration of the appearance of wrinkling, laxity and other signs of premature skin aging.

An increase in MMP activity can be instigated with as little as 0.1 minimal erythema dose (MED) Supplementation with topical MMPi ingredients reduces breakdown of structural and adhesive proteins and strengthens and supports the ECM.

 



    

Retinoids Vitamin E (tocopherol, tocotrienols & tocopheryl acetate) Aloevera Soy extracts Resveratrol Beta-carotene Epigallocatechin gallate L-ascorbic acid



Aloevera – anti inflammatory

Vitamin E: - Lipophilic antioxidant - tocopherols are abundant forms - wound healing, ROS scavenger, Absorbs UVR, anti inflammatory 







stimulate the production of new collagen, elastin and other ECM components chains of amino acids in varying lengths and structures three main peptides : - neurotransmitter-affecting peptides - carrier peptides - signal peptides

Neurotransmitter-affecting Peptides 



Acetyl hexapeptide-8 inhibits the soluble N-ethylmaleimidesensitive factor attachment protein receptors (SNARE) complex.

In vivo studies found that applying acetyl hexapeptide-8 twice a day for 30 days resulted in a 30% decrease in the depth of dynamic wrinkles.

Carrier Peptides 





Copper peptides increase the uptake of copper by the cells when paired with a tripeptide (glycyl-L-histidyl-L-lysine).

Copper plays a role in collagen deposition through its activation of lysyl oxidase.

Research indicates that copper peptides strengthen the ECM by increasing the production of collagen, glycosaminoglycans and adhesive proteins.

Signal Peptides  



Signal peptides are used to instigate specific responses within the skin.

Palmitoyl pentapeptide-4 indicate an increase in the production of fibronectin, as well as a stimulation of types I and III collagen.

Palmitoyl oligopeptide is a long-chain peptide that stimulates the production of multiple dermal.

  



 

Dyschromia is due to degeneration of the vascular system and melanogenesis Hyperpigmentation & telengectasia UVR causes necrosis of endothelial cells, leading to dermal blood cell damage, capillary protects and promotes the collagen around damaged vessels by limiting inflammation and dilation.

Increased melanocytic activity & pigment deposits Worsened by hormonal shifts

   

    

Hydroquinone (HQ) Kojic acid Lactic acid L-ascorbic acid Retinoids Azelaic acid Arbutin Resorcinol derivatives Undecylenoyl phenylalanine



 



replenish the skin as it undergoes normal homeostasis and wound repair Animal/plant based Plant based – grape seed, lilac, swiss apple Prevent UV-induced oxidative stress, inhibit inflammation, neutralize free radicals and reverse the effects of photoaging.



  

 



Retinoid Drug Project – synthesis of Vit. A analogues, 1968 Not synthesized in the body Precursor – beta carotene Retinol is first oxidized into retinal, which is then oxidized into RA by dehydrogenases; Types: trans-retinol & cis-retinol Retinoic acid (RA) plays important roles in cell growth, differentiation, and organogenesis.

The RA interacts with retinoic acid receptor (RAR) and retinoic acid X receptor (RXR) which then regulate the target gene expression.



 



Light sensitive – polyene tail with carbon double bonds Low molecular weight Highly oil soluble Involved in cellular growth, cell surface alterations, apoptosis, immune response and modulation & epithelial growth

Natural • •

• •

Retinyl palmitate Retinol Retinaldehyde Tretinoin

Synthetic • •

•

Adapalene Tazarotene Isotretinoin





 



Natural retinoids, like tretinoin, activate all RARs, while synthetic retinoids activate only a targeted selection Therefore, synthetic retinoids cause less skin irritation Natural retinoids tend to break down immediately when exposed to light Retinaldehyde – more gentle, commonly used in eye creams Use pea sized amounts, at night, alongside moisturiser & sunscreen

   



 

Redness Peeling dryness Prickly sensation esp under sunlight Increased sensitivity – around eyes, alar nasi, mouth corners Initial worsening of breakouts Not to be used in pregnancy/BF

   

 

MDA Increases penetration of CP SM treatment Dermaroller Lasers Part of depigmenting preparations – obagi range, triluma, kligmans formula





 



Not synthesized by humans due to lacking enzymes L-ascorbic acid is the chemically active biological form Weak sugar acid, hydrophilic Low cutaneous bioavailability when taken orally Unstable when exposed to light

Mineral ascorbate (Mg Ascorbyl Phosphate)is suggested to be more stable ď ˝ Function: - donates electrons to neutralise ROS - Reconverts in the presence of glutathione - Potentiates action of vitamin E - Prevents DNA damage - Essential for collagen synthesis - Inhibits tyrosinase - Anti inflammatory ď ˝



   



FDA approved is 2% - 4% Tyrosine kinase inhibitor Mainly used to treat hyperpigmentation Part of triluma & kligmans formula produces a reversible depigmentation of the skin by inhibition of the enzymatic oxidation of tyrosine to 3,4-dihydroxyphenylalanine (dopa) and suppression of other melanocyte metabolic processes Side effects – ochronosis, rebound recalcitrant hyperpigmentation

AHA - fruits, milk, sugar - GA, LA, citric acid - Exfoliant, humectant, skin conditioning & pH adjusters - Endpoint: confluent erythema - Neutralised with bicarbonate ď ˝

ď ˝

-

-

BHA Bark of willow SA, Jessner Used in acne Anti seborrhea Ideal for exfoliation and regulate sebaceuos activity Endpoint: frosting Neutralised with water