Anti-acne Preparations, anti-wrinkle and anti-oxidants.

1. - ANTI-ACNE PREPARATIONS
- ANTI- WRINKLES & ANTI-OXIDANTS
PPC – E01 COSMETICS
FALL 2022-2023
Prepared by: Dr. Nancy Abou Youssef, PhD
Lecturer of Pharmaceutics-
Pharos University in Alexandria 1
12/20/2022
Dr. Nancy Abou-Youssef
Presented by: Dr. Noha Ismail, PhD
Lecturer of Pharmaceutics-
Pharos University in Alexandria

2. LECTURE ILOs
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Part I:
 Etiology & development of Acne
 Stages of Acne & manifestations of each stage in acne
 Acne lines of treatment
Part II:
 Steps included in wrinkles formation
 Prevention or Camouflaging of wrinkles
 Anti wrinkle topical cosmeceuticals
• Topical estrogens
• Tretinion (prescription retinoids)
• Alpha hydroxy acids
• Topical Vitamins
 Other advanced techniques for dealing with wrinkles
12/20/2022
Dr. Nancy Abou-Youssef

3. 12/20/2022
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ANTI- ACNE PREPARATIONS

4. DEVELOPMENT OF ACNE :
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Formation of
micro-comedons
Non-inflammatory
Acne
Inflammatory
Acne
Papule
Pustule
Nodular
Acne
Closed Comedons
(white heads)
Open Comedons
(Black heads)

5. WHAT COUNTS FOR THE DEVELOPMENT OF ACNE ??? :
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•Hyperkeratosis
•Overproduction of sebum
•High count of Propionibacterium acnes

6. 1st STAGE IN ACNE: MICRO-COMEDO FORMATION
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 Accumulation of dead cells which form a
plug
 The plug prevents Sebum from being
released
 At this stage the blockage is invisible to the
eye and may take as long as eight to ten
weeks to develop into a visible blemish.

7. 2nd STAGE IN ACNE (Non- inflammatory)
CLOSED- COMEDO (white head)
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 As the plug becomes larger and more fully
blocks the pore opening it changes from a
microcomedo to a comedone.
 Since the comedone forms beneath the
surface of the skin and is closed to the
outside air, it does not discolor but stays
white, turning to a visible blemish.

8. PROGRESSED 2nd STAGE IN ACNE (Non- inflammatory)
OPEN- COMEDO (Black head)
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 Since it protrudes to skin surface, then the
comedone is open to the air, oxidizes and
becomes dark in color forming a
blackhead.

9. 3rd STAGE IN ACNE (Inflammatory)
PAPULE FORMATION
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 Propioni bacterium acnes bacteria, normally
found on the skin, combines with sebum and
result in inflammation and redness.
 At this point the inflammation is under the
surface of the skin and the result is a raised,
red, solid lesion.

10. 3rd STAGE IN ACNE (Inflammatory)
PUSTULE FORMATION
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 Additional inflammation and pus may form
causing a red, raised lesion that is often
painful to the touch.
 Pus is a mixture of white blood cells, dead
skin cells and bacteria.

11. 3rd STAGE IN ACNE (Inflammatory)
NODULE FORMATION (nodular acne)
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 Most severe inflammatory acne
 Large, hard inflamed bumps under the skin
surface which leave a scar after healing

12. TIPS ON ACNE TREATMENT:
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 Many people with acne first try to self-treat themselves before seeking the
assistance of a healthcare professional.
 But only non-inflammatory acne can be self-treated with OTC products.
 Wash skin twice daily with a cleanser of pH of 5.5–7 (less irritating and
damaging to the stratum corneum).
 Early treatment minimizes acne severity.
 Acne treatment is long-term and must be continuous and consistent.
 Acne may worsen at the beginning of treatment.
 There are additional cleansers that are marketed specifically for acne use
that contain an active anti-acne ingredient (e.g. benzoyl peroxide or salicylic
acid).
 Picking and squeezing of acne lesions must be avoided.

13. ACNE TREATMENT:
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 Many people with acne first try to self-treat themselves before seeking the
assistance of a healthcare professional.
 FDA states that any product labeled as an “acne drug product” is defined as:
“A drug product used to reduce the number of acne blemishes, acne pimples,
blackheads and whiteheads.”
 The FDA defines OTC products that fit this description to include:
• Salicylic acid,
• Sulphur
• Benzoyl peroxide

14. TOPICAL OTC DRUGS FOR ACNE TREATMENT:
1- BENZOYL PEROXIDE (BPO):
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 Benzoyl peroxide is clinically effective in acne, primarily because of its
bactericidal activity against Proprioni bacterium acnes and possibly
because of its mild comedolytic, keratolytic and anti-inflammatory
effects.
 Benzoyl peroxide has greater antimicrobial properties against P. acnes
than any of the topical antibiotics alone.
 The main site of pharmacological action is the pilosebaceous canal. BPO
penetrates through the follicular opening, probably by dissolving into
sebaceous lipids, and then exerts its antimicrobial activity.
 Benzoyl peroxide is available as OTC in 2.5–10% strengths and as either
washes or leave-on products (e.g. cream, lotion, gel).
 Skin irritation is a common side effect and a dose relation seems to exist
between efficacy and irritation. Thus, a controlled-release formulation
would clearly be advantageous.
 It is known to cause bleaching of hair and clothes

15. TOPICAL OTC DRUGS FOR ACNE TREATMENT:
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1- BENZOYL PEROXIDE (BPO):
 BPO use is frequently accompanied by redness, dryness in skin, that can
extend to a flaky skin ,…….So certain precautions should be taken !!
2- SALICYLIC ACID
 Unlike the alpha-hydroxy acids, it is aromatic hydroxy acids which is
lipid-soluble allowing it to penetrate not only the epidermis but also the
pilo sebaceous unit, rendering it as a very effective keratolytic.
 Salicylic acid also exerts anti-inflammatory effects by inhibiting
arachidonic acid.
 Salicylic acid more effective than benzoyl peroxide in treating
comedonal acne, BUT less effective than benzoyl peroxide in
treating inflammatory acne.
greater antimicrobial properties against P. acnes
than any of the topical antibiotics alone

16. TOPICAL OTC DRUGS FOR ACNE TREATMENT:
3- SULPHUR
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 Sulphur continues to be used today for a variety of conditions because of its
antifungal and bacteriostatic properties.
 It is believed by some to also have a keratolytic effect.
 Sulphur is available OTC in concentrations of 3–8%.
 Sulphur malodor and messiness of sulphur limits its use.

17. SCHEME FOR ACNE TREATMENT:
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Acne stage Treatment of choice
Micro-comedon stage Twice daily wash, with medicated soap
Non- inflammatory acne
(White & black heads)
Topical OTC drugs:
•Benzoyl peroxide
•Salicylic acid - - - - -> Which is better of the three???
•Sulphur
Inflammatory Acne
(Papule & Pustule)
Mild:
Topical OTC drugs- - - - -> Which is better of the three???
+
Topical Antibiotics:
Erythromycin or Clindamycin
Moderate:
Topical OTC drugs +
Oral Antibiotics: (Erythromycin – Tetracycline - Doxycycline)
Nodular Acne Isotretinoin +
Intra-lesional corticosteroid injections

18. ANTI-WRINKLE & ANTI-OXIDANT
PREPARATIONS
Dr. Nancy Abou Youssef, PhD
Lecturer of Pharmaceutics-
Pharos University in Alexandria
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12/20/2022
Dr. Nancy Abou-Youssef

19. WRINKLES FORMATION
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12/20/2022
Dr. Nancy Abou-Youssef

20. WRINKLES FORMATION
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12/20/2022
Dr. Nancy Abou-Youssef
• The interconnected, elastic fiber network in the dermis degrades and
is replaced (especially in the case of sun-exposed skin) by large
deposits of poorly organized elastin deep in the dermis. This leads
directly to loss of resiliency—the ability of the skin to quickly return to its
original shape after distortion.
• Collagen fibers become less well organized and the collagen itself
undergoes chemical changes that reduce its mechanical flexibility.
Repeated imperfect collagen repair can lead to ‗‗scar like‘‘ patches of
stiff, aligned collagen.
• The epidermis thins with age and
the properties of the stratum
corneum change with reduced
barrier repair properties and
decreased elasticity. These
changes are particularly important
in causing ‗‗fine lines‘‘.
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‫ف‬

21. WRINKLES FORMATION
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12/20/2022
Dr. Nancy Abou-Youssef
 Specially, In sun-exposed skin with chronic (years) of photo damage
there is a marked increase in certain types of sulfated glycos-
aminoglycans (A change in glycos-aminoglycans composition). Glycos-
aminoglycans can hold as much as 1000 times their own weight water
in an elastic gel, these changes hugely impact the water content of the
dermis.
 The subcutaneous fat layer (especially in women) decreases
dramatically in thickness, which leads to increased pressure from the
surrounding skin (pushing the wrinkle closed).

22. PREVENTION/ CAMOUFLAGE
OF WRINKLES:
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Dr. Nancy Abou-Youssef
 Moisturizers
 Sun Screens
 Avoid using harsh conditions; like hot water for wash
 Put away powdered base and
Lighten Up foundations
 Use Cosmetics cautiously:
- Of a simple, occlusive nature may essentially ‗‗fill in‘‘ the wrinkle valleys.
- Others are of a color or substance that changes reflected light from the wrinkle
sufficiently to minimize its appearance.

23. TREATMENT OF WRINKLES:
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12/20/2022
Dr. Nancy Abou-Youssef
1- Topical estrogens:
One of the most popular anti-aging preparations in the 1930s was the facial
moisturizers containing estrogen.
 Topical estrogen: has been shown to increase the production of the
overall collagen fiber count after six months of application. It also increased
the acid mucopolysaccharide and hyaluronic acid levels in the skin, which
are important for maintaining skin hydration and barrier function.
BUT……topical estrogen creams and estrogen replacement therapy are so
controversial !!!!
- There have been some concerns that estrogens predispose women to
malignant melanoma in the literature, although the reports are contradictory.
- Topical estrogens are even more controversial, since they are theoretically
linked to breast cancer and cancer of other female organs.

24. TREATMENT OF WRINKLES:
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12/20/2022
Dr. Nancy Abou-Youssef
Other Cosmeceuticals ( Functioning cosmetics):
 Since the removal of the first cosmeceutical, topical estrogen, from the
market, many other cosmeceutical formulations have been introduced.
 The Cosmeceuticals; formulation ingredients‘ come from a list of raw
materials that are generally recognized as safe…..Mostly Herbal origin.
 Plants are rich in endogenous antioxidants, and several vitamins.
Such as, Aloe, German chamomile, Green tea, Milk thistle, Oats,
Pomegranate, Pumpkin and many others, both orally & for topical use.

25. TREATMENT OF WRINKLES:
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12/20/2022
Dr. Nancy Abou-Youssef
Other Cosmeceuticals ( Functioning cosmetics):
 Retinoids:
represent one of the most important categories of cosmeceuticals both in
prescription and OTC.
 Retinoids define a class of substances comprising vitamin A (retinol)
and its naturally and synthetic derivatives.
Tretinion (Prescription retinoid), as anti-wrinkle:
 Reverse photo-induced skin changes:
 Transform an atrophic epidermis into a hyperplastic, thicker epidermis
and compact SC, resulting in the improvement of skin wrinkling and
exfoliation of retained stratum corneum.
 Tretinoin also induces papillary dermal collagen synthesis, new blood
vessel formation, increased glycosaminoglycan deposition.

26. TREATMENT OF WRINKLES:
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Dr. Nancy Abou-Youssef
Other Cosmeceuticals ( Functioning cosmetics):
Tretinion (Prescription retinoid):
 Side Effects:
• Patients who initiate treatment may experience varying degrees of
erythema and dermatitis for the first two to six weeks of therapy.
, Then the skin ―hardens‖ ……….
 Topical tretinoin is the most commonly used
cutaneous prescription Cosmeceutical

27. TREATMENT OF WRINKLES:
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Dr. Nancy Abou-Youssef
Other Cosmeceuticals ( Functioning cosmetics):
 Alpha Hydroxy Acids (AHAs):
Hydroxy acids represent the oldest facial Anti wrinkle cosmeceuticals.
 Alpha hydroxy acids include glycolic, lactic, citric, malic, mandelic,
and tartaric acid.
 Glycolic acid is the most popular of the alpha hydroxy acids for antiaging
purposes available in OTC and prescription products.
 Acidic pH……..!!!!
Mechanism of action of Glycolic acid:
 Epidermal effects: are manifested by decreased keratinocyte cohesion
(Keratolysis), which may be due to alterations in ionic bonding.
 Dermal effects: include increases synthesis of glycosaminoglycans and
increases fibroblast proliferation and production of collagen and elastin.
 Visibly this translates into less cutaneous wrinkling.

28. TREATMENT OF WRINKLES:
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Dr. Nancy Abou-Youssef
Topical Vitamins Topical effects Formulation Challenges
Vitamin A
(Retinoids)
- Improvement of skin fine lines,
wrinkles, roughness, and
hyperpigmentation (Previously
discussed).
- Associated irritation tends
to define an upper
concentration limit in their
use.
- Instability, especially to
oxygen and light.
Vitamin B3
(Niacinamide)
- Significant improvement
in skin barrier measured by a
lowered TEWL.
- Improves skin elastic properties.
- Hydrolysis to nicotinic acid,
which can induce intense skin
reddening (flushing) response.
Vitamin B5
(Pantothenic acid)
-Pro vitamin B5
(Panthenol)
- Skin hydration and the associated
improvement in roughness, scaling,
and epidermal elasticity;
improved skin barrier function;
protection against skin irritation;
skin soothing; anti-inflammatory
and anti-pruritic effects.
- Panthenol at high
concentrations can yield
sticky/greasy feeling. Thus,
Conc. >1% require special
formulation adjustment

29. TREATMENT OF WRINKLES:
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Dr. Nancy Abou-Youssef
Topical
Vitamins
Topical effects Formulation Challenges
Vitamin C
(Ascorbic acid)
- Antioxidant and it increases the production of
collagen, thus participate in wrinkles
reduction.
- Skin lightener and Anti-inflammatory
- Instability (Oxygen
sensitivity)….accompani
loss of activity & rapid p
yellowing.
Vitamin E
(Tochopherol)
- Prevent oxidative damage to skin, such as
preventing acute
and chronic ultraviolet (UV) radiation damage.
- Stable with no adverse e
to skin
Pro-vitamin D
(Dehydrochole
sterol)
- Converted into active vitamin D upon
exposure to UV
- Epidermal growth and differentiation, in
addition to skin barrier activities
- Vit.D products are often
potent, requiring caution
selecting topical doses.

30. OTHER TECHNIQUES FOR DEALING WITH
WRINKLES:
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 Injectable anti-aging Techniques
 Botulinum Toxins Injections
 Hyaluronic acid fillers Injections
 Calcium Hydroxyl apatite Injections
 Poly lactic acid fillers Injections
 Resurfacing Techniques
 Superficial & Medium depth chemical peeling
 Laser resurfacing
 Non ablative Laser
 Dermabrasion.
12/20/2022
Dr. Nancy Abou-Youssef