Vitamin A

• Environmental Defense
  • Free Radical Quenching (Oxygen, Ozone, Smoke, UV)
  • UVB & UVA Protection
• Anti-Aging
  • Prevention of Photodamage
  • Reversal of Photoaging
  • Slowdown of Chronic Aging
• Skin Elasticity
• Skin Firmness
• Moisturization

The Reasons For Interest in Anti-Aging Products

• The ‘Baby Boomers Generation'
  • Every eight minutes a member of this generation in the United States turns 50!!!
  • The primary drivers of trends in the Anti-aging market.
• Major Advances in formulation of prescription products which can reverse photaging (Retin-A ® , Renova ® ).
• Availability of cosmetic products with therapeutic activity which can either slowdown the aging process , or reverse photodamage and even intrinsic aging .

The Body Areas Most Prone to Aging

• The skin around the eyes is very fine and thin (0.05 mm).
• The face is continuously exposed to the elements and ages faster than
  other parts of the body.
• Hands are known to age five times faster than the rest of the body.

Solutions to Aging: Past & Present

• Stone-Age to 1970's - High Faith Products (“Hope-in-a-Jar”)
• The 1980's - High Faith/High Tech
• The 1990's - Bio-Active/High Performance Products

The Antioxidant & Vitamin Revolution of the 90's

Why Topical Vitamins in Skin Care?

• Highly Functional
• Work from within
• Protect
• Correct
• Beautify
• Safe - Free of side effects when used at the proper levels.

Vitamin A - Nutritional Functions

• Essential for vision
• Necessary for the proper functioning of the immune system
• Essential for tissue differentiation
• Helps maintain cell membrane structure
• Needed for the maintenance, growth, and health of teeth, nails, bones, hair, and skin
  Safe
  

Vitamin A - The Key Topical Benefits are:

• Anti-Keratinizing
• Increase of Skin Elasticity
• Thickening of the Epidermis and Dermis
• Normalization of Dry Skin
  Revearsal of Photodamage
• Reduction of Scaliness and Normalization of the Scalp, when used in hair care products.
  

The Vitamin A Family Consists of:

• Over 2,000 Retinoids
• The best known are:
  • Retinoic Acid
  • Retinol
  • Retinyl Palmitate
  • Retinyl Acetate
  • Retinyl Propionate
  
  The Studies

  Absorption of Vitamin A Palmitate through Human Skin

  The first study was reported in 1944 when young people were deprived of dietary vitamin A and their night vision was impaired and then restored after creams containing vitamin A were applied on their skin.

  Percutaneous Absorption and Bioconversion of Retinyl Palmitate to Retinol

  In a study conducted by James Bohnlein in 1994, It was demonstrated that topically applied vitamin A palmitate was absorbed by hairless guinea pig skin and human skin.

  
  
  
  Vitamin A Increase of Skin Elasticity

  

  
  

  Thickening of the Epidermis & Dermis

  
  Effect of Topical Vitamin A on Skin

  • Activation of the Fibroblasts which impact on the collagen production.

  Result: Thickening of the Epidermis and Dermis Decrease in Wrinkles and Fine Lines

  

  Vitamin A Effect of UV Light on Skin

  • UV Light reduces the levels of Vitamin A in the skin.
  • UV Light activates the collagenase which hydrolyzes the collagen in the connective tissues.
    

  Result: Sagging and Wrinkled Skin
  Revearsal of Skin Photodamage

  
  
  

  Vitamin A Derivatives Effects on Photodamaged Human Skin
  Dr. Albert Klingman, MD - July 1997

  Vitamin A Derivatives Effect on Human Skin

  • Objectives
    • Determine the activity of Vitamin A Palmitate, Vitamin A Acetate, and Retinoic Acid
      on Photodamaged Human Skin.
  • Subjects
    • 5 middle-aged women with moderately to severe photodamage of the dorsal forearms.
    • Each woman showed age spots, dryness with modests caling,uneven texture and mottling.

  Result: Sagging and Wrinkled Skin

  
  Test Products

  Chart 10
  
  Formula Number
  Retinoid % Concentration
  Description & Other Test Parameters
  
  26447-156
  Retinyl Palmitate
  8,000 IU/g (+20%)
  
  
  26447-157
  Retinyl Acetate
  8,000 IU/g (+20%)
  
  
  26447-159
  None
  Placebo Cream
  
  Retin-A 0.025%
  Tretinoin, Vitamin A Acid
  All-Trans-Retinoic Acid
  

  Procedure

  • Products were applied to the dorsal forearms in large Hill-Top Chambers for three (3) weeks.
  • Products were applied every other day.
  • 3mm punch biopsies were obtained one day after removing the chambers.
    Biopsy from the untreated skin was also taken to asses the degree of photodamage before treatment.
  • The tissue was fixed in formalin and stained with H & E.

  Results

  Reading of Results

  • All slides were read and evaluation was done based on the following criteria:
    1. Acanthosis - a thick epidermis signifies a proliferative effect and moderation of atrophy.
    2. Partial Correction of atypia. The latter term refers to keratinocytes which are abnormal in size, shape, and staining properties.
    3. Enhanced granular layer.
    4. Reduction in horny layer thickness.

  Summary

  • After three weeks of application of the various vitamin A derivatives on photoaged human skin, the subjects showed the typical retinoid effects:
    • Correction of Atrophy and Atypia
    • Increase in the granular layer with the prominent large granules
    • Normal orderly cell differentiation
    • Increased intercellular spaces of the epidermis

  Vitamin A Palmitate Scalp Normalization Study

  • Objective
    • Evaluation of 10,000 IU/g of Vitamin A Palmitate in a shampoo and a conditioner for its anti-scaling effects.
  • Evaluations
    • On days 0, 14, 21, and 24, the degree of scaling was graded.
  • Grading
    • 0 - 1 : Very little scaling
    • 2 - 3 : Mild scaling
    • 4 - 5 : Moderate scaling
    • 6 - 7 : Heavy scaling
    • 8 - 10 : Severe scaling

  Vitamin A Effect on Mucous Membranes

  • Essential for structure and function
  • In deficient state, mucous production is reduced.
  • Can be considered as cancer preventative ingredient due to the effect on squamous metaplasia.
  • Treatment senile vaginitis.

  
  Vitamin A Derivatives Formulating Techniques

  • Temperature: Vitamin A derivatives are heat sensitive and should be added to the emulsion at 40C (104 F)
  • Oxygen: Sensitive to oxygen and therefore, require addition of antioxidants, especially 0.1% Tocopherol and 0.1% Ascorbyl Palmitate.
  • Incompatible with BHT (yellowing) when exposed to light and elevated temperatures.
  • Heavy Metals: Sensitive Heavy Metals and the addition of chelating materials is necessary.
  • pH: Optimal pH is 6 with a range of 4.5 to 6.5
  • Package: Exposure to light and oxygen should be avoided and an opaque and tight package is a must.
  • Manufacturing Conditions: Preferred manufacturing conditions include reduced light exposure and moderate agitation (to eliminate aeration).
  • Comparative Stability of Vitamin A derivatives: The most stable form is vitamin A Palmitate and the least stable is vitamin A alcohol.
  • Base Types: oily systems, W/O emulsions, or O/W Microemulsions.
  • Use Levels: 5,000 IU to 8,000 UI/g (20% overage is recommended to compensate for stability losses.)
    

  Summary

  • The major skin care trends are:
    • Environmental Defense
    • Anti-Aging
    • Skin Elasticity
    • Skin Firmness
    • Skin Moisturization
  • Vitamins are popular in skin care because of:
    • Highly funtional
    • Work from within
    • Protect
    • Correct
    • Beautify
    • Safe
  • Vitamin A Derivatives are extremely useful because of the topical benefits:
    • Increase of skin elasticity
    • Thickening of the epidermis and dermis
    • Reversal of photodamge and effacement of wrinkles
    • Reduction of scaliness and normalization of the scalp

  Conclusion

  • Vitamin A Derivatives, due to their unique characteristics, are expected to play a very major role of the 21 st century cosmetics because of the interest in anti-aging in general and healthy skin in particular.