Active Skin Care Ingredients

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Active Skin Care Ingredients

• Peter T Pugliese, M.D
• Circadia by Dr Pugliese
• Reading, Pa

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What is Active?
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What is Active?
An Active Ingredient is any substance that is
capable of restoring the skin to normal or near
normal condition.
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Conditions for Using Actives

• First they must be safe. (Noli nocere).
• Second they must be physiologically compatible.
• Third they must be effective at low levels.

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Conditions cont

• The ingredient must be able to penetrate the
  skin to a predetermined desire level.
• The product must be tested for efficacy and
  safety with documented supportive data.
• The ingredient must not have a drug status.

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Classification of Actives

• Moisturizers
• Exfoliators
• Proliferators
• Collagen and Elastin Builders
• Enzyme inhibitors
• Antioxidants (includes DNA protectors)
• Anti-glycation agents
• Anti-inflammatory agents

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Moisturizers

• Moistuization can only occur from within the
  skin!
• Moisturizers only slow water loss from leaving
  the skin.
• Effective moisturizers slow water loss from 25
  to 50 . Greater reduction in water loss is not
  good for the skin, and can damage skin.

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Some Moisturizers

• Petrolatum (Vaseline)
• Waxes ( sterates, cetyl alcohol, beeswax)
• Saccharide isomerate (excellent climate control)
• Glycols ( glycerin, propylene glycol) are really
  humectants, that is they absorb water.
• Jojoba oil (liquid wax)
• Silicones ( many types)

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Process of water reaching the stratum corneum
Water is transferred from the capillaries to the
epidermis
Water if formed here
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Mechanism of Moisturizers
Water out
Moisturizer
Water blocked
Water back in
Water up
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Exfoliators

• Exfoliators are agents that remove stratum
  corneum cells, chemically, or mechanically.
• To exfoliate they must break the desmosome bonds.
• The two methods used are protein denaturation and
  enzymatic.

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Protein Denaturation

• Protein denaturation involves chemicals that can
  partially, or fully alter a protein. For example,
  egg albumin when placed in an acid solution such
  as vinegar will coagulate. This is an
  irreversible change.
• Chemicals can be acid, or alkaline depending on
  the protein.

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Examples of Acids and Alkali

• Alpha hydroxy acids such as lactic, glycolic,
  malic, or Beta hydroxy acids such as salicylic.
• Acids are proton donors, that is they denature by
  adding atoms that cross link, or dissolve.
• Alkali such as sodium hydroxide, or calcium
  carbonate are just the opposite. They attract
  protons and most often will dissolve proteins.

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The Target is The Desmosome
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An Other View of a Desmosome
An adjacent cell is on this side and would
contain all the proteins shown in the area marked
cytoplasm in the diagram. The action of acids
and alkali are on the desmoglein and desmocollin.
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Exfloliating Enzymes

• Enzymes are proteins that act on specific
  substances to alter them in some way.
• Enzymes can join substances or take then apart.
• Enzymes act on specific parts of a substance.
• Enzyme only work when in solution. They need
  water to function.

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The Target of the Enzymes is the Desmosome

• Enzymes attack the corneocyte at the junction of
  the desmosome.
• Enzymes work by time and concentration.
• Three major enzyme used in skin care
• Papain, Bromelain and Trypsin.

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Enzymes are Multifunctional

• Use an enzyme when ever you want to clean up an
  area with dead tissue,or biological debris.
• You can use an enzyme to remove several layers of
  dead skin to assist in penetration of an active.
• When used before an acid treatment it will allow
  more acid to penetrate the corneum.

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Proliferating Agents

• Proliferating agents are substances that cause
  the epidermis to grow faster.
• This action produces more cells and provides a
  thicker epidermis.
• Proliferators also cause an increase in collagen
  and elastin.

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Some Proliferating Agents

• Vitamin A is one of the best proliferating
  agents. It is a major treatment agent in aging
  skin.
• Vitamin is available in three forms Retinol is
  the alcohol form. Retinal is the aldehyde form
  and retinoic acid is the acid form. (Retinoic
  acid is a drug and cannot be use without an Rx)

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Some Bodily Proliferating Agent

• The body produces many substances generally known
  as growth factors such as, for example,
  platelet-derived growth factor (PDGF),
  platelet-derived angiogenesis factor (PDAF),
  vascular endothelial growth factor (VEGF),
  platelet-derived epidermal growth factor (PDEGF),
  transforming growth factor beta (TGF-B),
  transforming growth factor alpha (TGF-A),
  insulin-like growth factors 1 and 2 (IGF-1 and
  IGF-2), fibronectin, angiogenin, keratinocyte
  growth factor (KGF), epidermal growth factor
  (EGF), fibroblast growth factor (FGF), and many
  more.

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Plant Derived Growth Factors

• The five major types of plant hormones Auxins,
  Gibberellins, Cytokinins, Ethylene and Abscisic
  acid. Three plant hormones curenntly used in
  cosmetics are gibberellic acid, kinetin (a
  Cytokinin), and zeatin (a Cytokinin).

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More Exotic Plant Growth Agents

• More exotic plant growth factors include
• Brassinosteroids act with auxins to encourage
  leaf elongation and protect plants from some
  insects..
• Salicylates stimulate flowering and cause disease
  resistance in some plants.
• Systemin is a peptide involved in plant healing.
• Polyamines major role in cell proliferation and
  DNA replication in plants.
• Jasmonates-is involved in the plant wound
  response and defense mechanism, regulate growth,
  germination, stimulate proteins that protect the
  plant against environmental stresses, such as
  temperature changes, or droughts.

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Cosmetically Acceptable Growth Agents

• Live Yeast Cell Extract (LYCE) or (SRF) very
  effective, yeasty odor hard to mask.
• Ethoxylated Lipids, widely used.
• Non-ionic Surfactant effective, but can be
  irritating in high dosages.
• Alpha and Beta Hydroxy Acids

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Collagen and Elastin Builders

• Collagen and elastin are structural proteins
  produced by the fibroblasts in most tissues,
  chondrocytes in cartilage, osteoblasts in bone,
  pericytes in blood vessels. Half-life is in days.
• There are many biological agents that control
  both the formation of collagen and the
  destruction of collagen such as growth factors,
  hormones and cytokines. For example, TGFb and
  PDGF are two.

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Ingredients that Stimulate Collagen

• Fibroblast growth factor.
• Ascorbic acid
• Proline
• Asiatic acid
• Cu ions and copper peptide
• Sunscreens
• Bioflavanoids

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Elastin

• Elastic fibres are common in tissues which
  require the ability to deform repetitively and
  reversibly. Made in muscle cell and fibroblast.
• Elastin turnover is extremely slow with a
  half-life approaching the age of the organism.
  Elastin is mainly synthesised during development
  and any damaged elastin is either not replaced
  or replaced with non-functional fibers. Half-life
  is 60-70 years

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Ingredients that Stimulate Elastin

• Ethocyn- by Rx only. Very effective.
• TFGb1, IGF
• Ellagic acid-prevents elastase action
• Polyphenols- inhibits elastase
• Bioflavanoids-multifunctional

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Enzyme Inhibitors

• The esthetician is only recently aware of the
  importance of enzymes in skin care.
• Some enzymes are bad actors and work against
  maintaining healthy skin.
• Chief among these are the ubiquitous matrix
  metalloproteases.
• Enzyme inhibition will soon be a major new active
  category in skin care.

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The Matrix Metalloproteases

• There about 28 of these enzymes but you need to
  know only about 5 or 6 of them.
• MMPs for short. MMP Type I is the most
  important enzyme for skin care as it breaks down
  collagen Type I
• MMP 1, 2, 9 and 7,8, 13 in the menstrual cycle.
  (Major cause of cellulite)
• MMPs are enzymes able to degrade most components
  of the extracellular matrix such as collagens,
  elastins, laminins, fibronectins and the protein
  core of proteoglycans.

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Stylized Structure of Skin Showing Collagen and
MMPs
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Stylized Structure of Skin Showing Collagen and
MMPs
Epidermis
MMP
All of this is collagen
MMP
Fat Layer
Muscle Layer
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Stylized Structure of Skin Showing Collagen and
MMPs.
Epidermis
MMP
Skin Collapse
All of this is collagen
MMP
Fat Layer
Muscle Layer
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MMP Blocking Agents

• Oligomeric Proanthocyanidins (OPC)
• Polyphenols (green tea a good source)
• Endogenous tissue inhibitors TIMPs 1,2,3,4
• Chelating groups include hydroxamates,
  carboxylates, thiols, and phosphinyls.
• Chlorhexidine is a germicide as well.
• Tetracycline (doxycillin) very low dose.

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Antioxidants

• An antioxidant is a molecule capable of slowing
  or preventing the oxidation of other molecules.
  Oxidation is a chemical reaction that transfers
  electrons from one substance to an other
  substance termed an oxidizing agent.
• Oxidation describes the loss of electrons by a
  molecule, atom or ion
• Reduction describes the gain of electrons by a
  molecule, atom or ion.

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Put another way

• Oxidation is the gain of oxygen, or loss of an
  electron
• Reduction is the gain of hydrogen, or an electron
• Free radicals form when a stable molecule is
  attacked and in some manner loses an electron and
  becomes unstable.
• Antioxidants either prevent this action, or stop
  it once it happens.

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Aging Skin and Energy

• Aging skin is characterized by decrease ATP, the
  energy source for the body.
• Mitochondria supply this energy but are
  decreased in aging skin. CoQ10 and oxygen are two
  ingredients that help increase skin energy by
  stimulating mitochondria.

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Some Excellent Antioxidants

• Vitamin E fat soluble essential for life. Stops
  cell membrane oxidation by free radicals.
• Vitamin C restores vitamin E, critical in
  stopping many free radical reactions.
• A lipoic acid- critical in many metabolic
  reaction as a cofactor in enzyme reaction.
• Regenerates vitamin C after reduction.

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Some Excellent Antioxidants

• CoQ10 or ubiquinone essential for metabolism of
  glucose and general antioxidant. Critical
  component of mitochondria.
• Polyphenol are powerful anti-cancer agents.
• Carnosine stabilizes cell membranes, act to
  quench free radicals.
• Carotenoids free radical scavenger
• Soya products- powerful antioxidant, immune
  stimulator, and cancer preventor.

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Anti-Glycation Ingredients

• Glycation is a relatively new term for use by
  estheticians, but it is a critical term. Much of
  the cardiovascular disease and skin aging can be
  attributed to the process of glycation.
• Glycation is the non-enzymatic joining of a sugar
  molecule to a protein that results in an abnormal
  or nonfunctioning compound.

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Effects of AGE Products
1. Forms a glue that makes blood vessels
inelastic and stenotic. 2. Promotes
inflammation. 3. Affects fats, DNA, and other
biological materials.
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Advanced Glycation End Products (AGE)
The end result of the process of glycation is the
formation of AGE products that crosslink with
other proteins and lipids and inactivate them, or
make them essentially nonfunctional.
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Simple Glycation Process
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Some Anti-Glycation Supplements

• Aminoguanidine
• Carnosine
• Taurine
• Herbs ginger, tumeric, rosemary, thyme,
  stinging nettles, and many others.
• Benfotiamine excellent glycation preventor
• Pyridoxamine powerful anti-glycation agent

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Skin Care Application

• Diet and oral supplements as noted above.
• Use a night cream that contains anti-glycation
  ingredients.
• Check level of pentosidine as index of efficacy.
  At least twice a year
• Make daily use of sunscreens if exposed to sun at
  extended times between 10AM-2 PM

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Some Notes on Inflammation

• Inflammation is a complex biological response to
  an actual, or potential threat to the body.
• Inflammation can be acute or chronic.
• Most inflammatory processes are not due to
  infection.
• Aging is considered by some biologist to be a
  response to one, or more inflammatory agents.

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Summary of Basic Inflammation

• The inflammatory reaction is very complex, but it
  can be broken down into two major phases or
  stages
• The Vascular Stage characterizes by redness and
  swelling.
• The Cellular Stage characterized by white blood
  cell migration and secretion of humoral agents of
  inflammation.

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The Arachidonic Acid Cascade

• Step One Arachidonic acid in the cell membrane is
  liberated by phospholipase A2.
• Arachidonic acid is broken down in to two
  pathways.
• Lipoxygenase pathway make leukotriens.
• Cyclooxygenase pathway makes endoperoxides.
• These agents together produce the final
  inflammatory response.
• Arachi- from Greek arakis meaning a groundnut

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Why is the AAC Important?

• Most anti-inflammatory agent action on the on the
  arachidonic acid cascade to stop it or to inhibit
  it.
• Cell Membrane
• Arachidonic acid a phospholipase A2
• Lipoxygenase
  Cyclooxygenase

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Cortisone
Inhibits
Here
Cell Membrane
Arachidonic acid a phospholipase A2

NSAIA Here Lipoxygenase
Cycloxygenase
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Anti-Inflammatory Agents

• Cortisone has 26 different forms. Most potent.
• Non-Steroid anti-inflammatory Agents
• Over 50 products which includes
• Aspirin
• Ibuprofen
• Salicylic acid
• Indomethocin

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Pant Derived Anti-Inflammatory Agents

• Over 300 substances from plants. A few are
• Allantoin , apigenin, ascorbic acid, bisabolol
• Boswellic acid, bromelain, caffeic acid
• Curcumin, ellagic acid, emodin, ferulic acid
• Genistein, hesperidin, lupeol
• Papain, tocopherol, thymol, ursolic acid

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Plant Materials

• Normally are highly colored, the less refined the
  more they are colored and the harder they are to
  formula.
• Natural sources may be contaminated with other
  plants, or extracting materials.
• Know your source and ask questions.

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Summary

• The esthetician has available many active
  ingredients with which to treat clients.
• Esthetician should be well informed about all
  active ingredients they use.
• Active ingredients require careful dosage to
  achieve maximum benefit. (Dose/response)