Topical vitamines and skin

02/16/17
Are topical
vitamins useful?

Yes, but
how and
why?
Reactive oxygen species
generated by ultraviolet light
result in photocarcinogenic and
photoaging changes in the skin.
Antioxidants protect skin from

these insults
 Virtually all plants and animals
protect themselves from the
sun using vitamins C and E
 Skin naturally uses antioxidants (AOs) to
protect itself from photodamage
physiologic and plant AOs: vitamin C,

vitamin E, selenium, zinc, silymarin, soy

isoflavones, and tea polyphenols. Their
topical use may favorably supplement
sunscreen protection and provide
additional anticarcinogenic protection. (J
Am Acad Dermatol 2003;48:1-19 )
 Vitamin C
Ascorbic acid (vitamin C) is a
cofactor required for the function of
several hydroxylases and
monooxygenases. It is not
synthesized in humans and some
other animal species and has to be
provided by diet or pharmacologic
means.
 Topical vitamin C was first studied as a
photoprotectant by using a porcine skin
model. In this study, histological
examination revealed that animals
treated with topical ascorbic acid
exhibited fewer sunburn cells than did
those animals treated with vehicle alone
when exposed to both UVA and UVB
irradiation.
 There are multiple studies that
demonstrate that mice treated
with topical vitamin C have less
erythema, fewer sunburn cells,
and decreased tumor formation
seen in treated skin after UV
exposure.
 Vitamin C, a strong antioxidant itself,
also reduces (and therefore recycles)
oxidized vitamin E back into its active
form so the antioxidant capabilities of
vitamin E are amplified in this way.
 Although the increase of types I
and III collagen production in
cells cultured in the presence of
ascorbic acid is well known, the
effects of ascorbate on other
extracellular matrix molecules
are still poorly understood.
 In fact, studies suggest that concentrations of
ascorbic acid that maximally stimulate collagen
biosynthesis act as an antagonist of elastin
accumulation. In a series of studies, Franzblau et al
elaborated on these observations by showing that
elastin accumulation was sharply diminished in cell
cultures treated with vitamin c. In other words,
we know that addition of ascorbic acid to
fibroblast cultures increases production of
collagen but may decrease production of
elastin by an unknown mechanism.
 Clinically the relevance of these effects on
collagen and elastin is unknown. There is
only one study in the literature that
examines the effects of topically applied
vitamin C on wrinkles. In this study, Cellex-
C decreased wrinkles when applied topically
for a period of three months. The patients
were evaluated using photography
assessments and optical profilometry.
 Unfortunately, the study cannot be
considered as a blinded study
because a large proportion of the
patients experienced stinging on the
side treated with vitamin C. However,
there was a significant difference in
the wrinkles on the treated side
versus the untreated side.
 vitamin c in melasma.
Although hydroquinone showed a
better response, ascorbic acid may
play a role in the therapy of
melasma as it is almost devoid of
side-effects; it could be used alone
or in combination therapy.
sunscreen and ascorbic acid would
be
very helpful in preventing the
aggravation of Darier's disease
caused by sun exposure.
J Dermatol. 2002 Jul;29(7):455-8.
Higher Concentrations
of Vitamin C in Breast
Milk are Linked to
Lower Rate of Infant
Atopy
Percutaneous absorption of
ascorbic acid is limited by its
impermeability and instability.
We can improve the
percutaneous absorption of
ascorbic acid by use of
iontophoresis after topical
application of ascorbic acid.
J Invest Dermatol. 2003 Nov;121(5):1118-25.

Allresurfacing techniques tested

produce significant increases in
the topical delivery of vitamin C .
The Er:YAG laser showed the

greatest enhancement of skin

permeation of vitamin C among
the modalities tested.
 The CO2 laser at a lower fluence promoted
vitamin C permeation with no ablation of the
stratum corneum or epidermal layers.
Further enhancement was observed with the
CO2 laser at higher fluences, which was
accompanied by a prominent ablation effect.
Microdermabrasion :The flux and skin
deposition of vitamin C across
microdermabrasion-treated skin was
approximately 20-fold higher than that
across intact skin.
 Delivery of topical L-ascorbic
acid into the skin is critically
dependent on formulation
characteristics.
 a stable aqueous solution of 15% L-
ascorbic acid (vitamin C) and 1% alpha-
tocopherol (vitamin E).
Appreciable photoprotection can be
obtained from the combination of
topical vitamins C and E. We suggest
that these natural products may protect
against skin cancer and photoaging.
UV photoprotection by combination topical antioxidants
vitamin C and vitamin E.

Lin JY, Selim MA, Shea CR, Grichnik JM, Omar MM, Monteiro-
Riviere NA, Pinnell
 Palm oil is a rich source of vitamin E,
carotenoids, tocotrienols and
tocopherols which are natural
antioxidants and act as scavengers
of oxygen free radicals.
In this study we therefore assessed
the anti-tumor promoting potential of
palm oilCancer Lett. 2003 Mar 31;192(2):151-60
 local treatment with E-mousse
for 3 weeks in diabetic
microangiopathy improves skin
microcirculation and the
metabolic condition.
Evaluation of the local effects of vitamin E (E-Mousse) on free radicals in diabetic microangiopathy:
a randomized, controlled trial.

Ruffini I, Belcaro G, Cesarone MR, Geroulakos G, Di Renzo A, Milani M, Coen L, Ricci A, Brandolini R, Dugall M,
Pomante P, Cornelli U, Acerbi G, Corsi M, Griffin M, Ippolito E, Bavera P.
 Vitamin A (retinol )
vitamin A (retinol),is an essential
nutrient which plays a role in cell
growth and differentiation. The
retinoids, which interact with nuclear
receptors and affect gene transcription,
have enormous therapeutic potential,
particularly if they are receptor- and
function-selective.
 Retinol
Is classified as a cosmetic
Early forms were very unstable
Although binds to RARs, does not
cause clinical erythema.
In a 12 week trial: improvement in skin
texture, clarity, sallowness, mottled
pigmentation, pore size, and fine
wrinkling
 Retinol
A substantial margin of safety with
respect to the potential for systemic
absorption.
Not all products are equal, poor
formulation and packaging may lead to
oxidation and loss of potency.
Roc Retinol Actif-pur (now replaced by
Retin-Ox correction) and Neutrogena
Healthy skin are proper ones.
Retinoid-induced epidermal hyperplasia in human skin organ
culture: inhibition with soy extract and soy isoflavones.

: Exp Mol Pathol. 2004 Dec;77(3):176-83.

use of soy extract or its constituent

isoflavones in conjunction with 14-all
trans RA may provide a way to mitigate
unwanted epidermal effects of topical
retinoid therapy without compromising
beneficial retinoid effects in the dermis.
Genistein,is the major isoflavone in
extracts of soy,responsible for this effect.
 Retinoids in D.M

This article suggests that prophylactic

use of retinoid-containing
preparations might be useful in
preventing the development of
nonhealing skin ulcers resultant
from minor traumas in at-risk skin.
Diabetes. 2005 Mar;54(3):
Topical pretreatment of diabetic rats with all-trans retinoic acid
improves healing of subsequently induced abrasion wounds.

Lateef H, Abatan OI, Aslam MN, Stevens MJ, Varani J.

 Procyanidins present in grape seeds
are known to exert anti-
inflammatory, anti-arthritic and anti-
allergic activities, prevent skin aging,
scavenge oxygen free radicals and
inhibit UV radiation-induced
peroxidation activity.

Anti-tumor-promoting activity of a polyphenolic fraction isolated from grape seeds in the

mouse skin two-stage initiation-promotion protocol and identification of procyanidin B5-3'-
gallate as the most effective antioxidant constituent.

Zhao J, Wang J, Chen Y, Agarwal R

 Lycopen
Ultraviolet (UV) rays cause depletion of
the antioxidant substances contained in
the epidermis. This is the rationale for
the use of topical antioxidant
substances. lycopene-based products
have a much greater protective ability
than the products containing the mixture
of vitamins E and C.
J Eur Acad Dermatol Venereol. 2004 Jan;18(1):52-5.
Zinc
Zinc protects against UV
radiation, enhances wound
healing, contributes to
immune and
neuropsychiatric functions,
and decreases the relative
risk of cancer and
cardiovascular disease.
 All body tissues contain
zinc; in skin, it is five to six
times more concentrated
in the epidermis than the
dermis.
 Zinc is required for the normal
growth, development and function of
mammals. It is an essential element
of more than 200 metalloenzymes,
including the antioxidant enzyme,
superoxide dismutase, and affects
their conformity, stability, and
activity.
 Abundant evidence
demonstrates the antioxidant
role of zinc. Topical zinc, in the
form of divalent zinc ions, has
been reported to provide
antioxidant photoprotection for
skin.
 Two antioxidant mechanisms have been
proposed for zinc:
zinc ions may replace redox active
molecules, such as iron and copper, at
critical sites in cell membranes and
proteins; alternatively, zinc ions may
induce the synthesis of metallothionein,
sulfhydryl-rich proteins that protect
against free radical
 In conclusion regular application of skin care
products containing antioxidants may be of
the utmost benefit in efficiently preparing
our skin against exogenous oxidative
stressors occurring during daily life.
Furthermore, sunscreening agents may also
benefit from combination with antioxidants
resulting in increased safety and efficacy of
such photoprotective products
 Kojic acid,
a fungal metabolic product, has been
used as a skin-depigmenting agent in
skin care products marketed in Japan.
Iron in the skin is known to be involved
in wrinkling as a result of chronic
photodamage. Kojic acid is expected to
have anti-wrinkling activity, since it
possesses iron-chelating activity.

Prevention of the photodamage in the hairless mouse dorsal skin by kojic acid as an iron chelator.

Mitani H, Koshiishi I, Sumita T, Eur J Pharmacol. 2001 Jan 5;411(1-2):169-174

 Mequinol
A new topical solution containing 4-
hydroxyanisole (mequinol) 2%/tretinoin
0.01% (Solage) was compared with its active
components, its vehicle, and hydroquinone
(HQ) 3% in the treatment of solar lentigines. In
conclusion, the mequinol 2%/tretinoin 0.01%
solution is a highly effective and well-tolerated
treatment for solar lentigines and related
hyperpigmented lesions, being superior to HQ
3% for lesions on the forearm and of similar
efficacy for lesions on the face.

: Cutis. 2004 Nov;74(5):319-22

 Since the skin not only fulfils a protective
function for the organism but is also an
active peripheral endocrine organ, which
even releases effective hormones in the
circulation, local hormone substitution
could become interesting in the future.