Role of antioxidants in developing novel delivery systems as longevity
therapy
Manmohan
S. Jangdey,
Anshita Gupta, Abhishek K. Sah and Sanjay J. Daharwal
University
Institute of Pharmacy, Pt. Ravishankar Shukla University, Raipur (C. G.)
492001, India
*Corresponding Author E-mail: manuiopresearch@gmail.com
ABSTRACT:
An antioxidant is a molecule capable of
inhibiting the oxidation of other molecules. Oxidation is a chemical reaction
that transfers electrons from a substance to an oxidizing agent. Oxidation
reactions can produce free radicals. Antioxidants terminate these chain
reactions by removing free radical intermediates, and in the body will
drastically determine how long one will live. We have reviewed here sources of
antioxidant, the network of antioxidant, supplements, causes of ageing, antiageing nutrition and
different lipids based delivery system in longevity therapy. In addition to
these uses of natural antioxidants in medicine, the compounds have many
industrial uses, such as preservatives in food and cosmetics and preventing the
degradation of rubber and gasoline. It is concluded that Novel lipid based
delivery systems reviewed here possess the potential to develop as the new
generation smarter carrier systems for topical delivery of antioxidants.
KEYWORDS: Antioxidant, Supplements, Longevity.
INTRODUCTION:
The phenomenon of
aging is a course of diminished functionality and reserve capacity in all body
organs, resulting in an increased likelihood of disease and death. Skin aging
is a degenerative process wherein the results due to chronological/intrinsic
aging are overlaid with effects produced by environmental factors (e.g., sun,
heat, pollution and smoking)[2]. Antioxidants are
powerful nutrients that strengthen the immune system, help flush out free
radicals that cause a host of problems in the body [4]. Antioxidants are
substances that may protect cells from the damage caused by unstable molecules
known as free radicals. Free radical damage may lead to cancer. Antioxidants
interact with and stabilize free radicals and may prevent some of the damage
free radicals might otherwise cause. Examples of antioxidants include
beta-carotene, lycopene, vitamins C, E, and A, and other substances.
The primary job of
this network is to continually replenish the other members when they are lost
through oxidative stress. When one member of the network neutralizes a free
radical, it becomes a free radical itself, although much weaker. It is then replenished
by one or more of the other network members [5]. The newly regenerated molecule
moves on to find and repair another free radical molecule. Research shows
Antioxidants promote longevity, slow down the aging process cause by free
radicals, prevent artery clogging and diseases.
Without Antioxidants we will not be able to survive.
An
antioxidant is a molecule capable of inhibiting the oxidation of other
molecules. Oxidation is a chemical reaction that transfers electrons from a
substance to an oxidizing agent. Oxidation reactions can produce free radicals.
Antioxidants terminate these chain reactions by removing free radical
intermediates, and inhibit other oxidation reactions [9].
Antioxidants are
miracle workers, they fight diseases and help the body heal and keep the brain
healthy as we age. It’s clear to see the more antioxidants in the body will
drastically determine how long one will live. That's why it’s imperative that
our bodies have sufficient antioxidants to prevent free radicals from destroying
our body. Antioxidants are widely used as ingredients in dietary supplements to
maintain health. Antioxidants prevent diseases such as cancer, Alzheimer, boost
energy lever, lower blood sugar, prevents arthritis, prevent cardiovascular
disease, varicose veins and promote longevity by slowing the aging process. In
addition to these uses of natural antioxidants in medicine, the compounds have
many industrial uses, such as preservatives in food and cosmetics and
preventing the degradation of rubber and gasoline [7,8].
The Network
Antioxidants and Their Partners
Vitamin C :- Bridges the gap between fat- and
water-soluble antioxidants.
Vitamin E :- The most important nutrient for a healthy
heart.
CoQ-10:- Heart and cardiovascular
protection and energy booster.
Glutathione :-Your body's most
abundant antioxidant.
N-Acetyl Cysteine :- The best supplement for boosting glutathione.
Alpha-Lipoic Acid :-Unique in that it
works in every part of your cells.
Selenium :-
Powerful support for the network antioxidants.
Coenzyme Q-10 :- For a healthy heart and cardiovascular
system.
Glutathione :- Your
body's primary water-soluble antioxidant.
Lipoic acid :- The "universal" antioxidant,
because it works everywhere.
These are by no
means the only antioxidants that play a significant role in your health.
Working with this network are certain plant phytochemicals:
the bioflavonoid and carotenoids, and the trace
mineral selenium. The primary job of this network is to continually replenish
the other members when they are lost through oxidative stress. When one member
of the network neutralizes a free radical, it becomes a free radical itself,
although much weaker. It is then replenished by one or more of the other
network members. The newly regenerated molecule moves on to find and repair
another free radical molecule. This cycle then repeats itself continuously,
maintaining a healthy balance in your body. This process of cell oxidation and
recovery happens more times than you could imagine—about 10,000 times every day
for each of the trillions of cells in your body.
The
Network Works as a Team.
Although these
members of the network all work together, each has its own distinct function.
Because each cell in your body has a fat-based membrane (outer shell)
and a water-based nucleus (center), it needs
different antioxidants in different areas.
Fat-soluble vitamin
E and coenzyme Q-10 protect the fatty cell membrane and the mitochondria, while
water-based vitamin C and glutathione protect the cell interior. Lipoic acid
has the unique ability to go anywhere. One member of the network rescues
another one when they become oxidized by free radicals. This clearly
demonstrates the principle that you need all of these antioxidants in
sufficient amounts.
Antioxidants-
Natural Defence System
1. A primary reason that humans
have a much longer life expectancy than other animals is that we have extremely
efficient antioxidant defense systems. The strength
of your antioxidant defense system depends on several
key factors:
2. Diet. You
need to get a good supply of protective antioxidants from your diet, so it's
important that you choose your foods with that in mind. In addition,
antioxidant superfoods and supplements are an
excellent way to complement the antioxidant foods you eat.
3. Antioxidant Enzymes. Our
bodies produce several enzymes (including superoxide dismutase and glutathione)
that provide antioxidant protection. In order to produce these enzymes, you
need nutritional building blocks such as manganese, zinc, iron, copper and
selenium from your food.
4. Two other important
antioxidants are manufactured in your body: coenzyme Q-10 and lipoic acid. Typically, your body's
production of these antioxidants begins to diminish as you get older, and
mature adults tend to have very low levels. It's nearly impossible to get much
of these from your diet as well.
5. Your Genes. Some of
your ability to produce these antioxidant enzymes in your body is determined by
the genes you inherited. Everyone has a unique set of genes that partially
determine your longevity, susceptibility to disease, and your rate of aging.
However, improving your diet can overcome most genetic handicaps you might have
it certainly makes sense to do all you can.
The antioxidant
network could be compared to a football team. A football team
has many players, and each player has their own specific role in executing a
play. You need all the members to do their specialized jobs, in sequence. If
you're missing the left guard or wide receiver, for example, the play won't
work as well as it could. Every individual is
important.
Antioxidant Facts:
Antioxidants work best as a team. You get better results with
moderate amounts of many different antioxidants than you'd get using very large
amounts of just one. That would be like fielding a football team using eleven
quarterbacks — you wouldn't expect things to work as well. That's why you want
to get many different members of the antioxidant family working together for
you.
Antioxidant Facts:
Combinations of antioxidants work better. All fruits and
vegetables contain many different phytonutrients all
on their own. These nutrients are designed by nature to work together in your
body, and research studies have backed this up, showing that antioxidants are
much more powerful when they are consumed in combinations.
Supplements: - Best
Sources of Antioxidants
Fruits and
vegetables are the most common source of antioxidants for most people.
There are literally
thousands of nutrients in fruits and vegetables categorized as phytochemicals, or phytonutrients, that contain powerful antioxidant properties.
A single fruit or
vegetable contains many different phytonutrients
Some of them, like onions, have dozens of
different antioxidant compounds, many of which have never been identified or isolated.
This makes it important to eat as wide a variety of antioxidant-rich foods as
possible, every day.
Herbs
and Spices.
An even more potent
source of antioxidants are herbs and spices such as
turmeric, ginger, garlic, cloves, cinnamon and many others. There's a reason
why herbs and spices have been used medicinally for thousands of years. It's
been noted that cultures where people consume a lot of spices tend to have very
low rates of degenerative diseases.
Fresh Juices and Smoothes.
A great way to pack a lot of antioxidants into one meal is by making fresh
juices, or fruit and vegetable smoothes. There's an entire section of this
website devoted to the art of making a smooth. My page on how to make a
smoothes the healthy way will help you get started.
Super foods are
specialized food products with an extremely high concentration of vitamins,
minerals and phytonutrients. Adding very small
portions of these foods to your diet can increase your intake of antioxidants,
even without altering the rest of your diet significantly .Super food products
are so easy to add to your daily diet because the serving sizes are very small
(usually about a tablespoon or two). At the same time, they contain the full
spectrum of phytonutrients that are in the fresh
source. There are many great reasons why you should use super food products.
It may be possible
for you to get all the nutrients you need for good health, including
antioxidants, from a well-diversified diet of whole foods. That's the goal,
anyway. Unfortunately, it can be a difficult thing to do and that's why you
might want to consider the benefits of antioxidant supplements.
There's so many
environmental stress factors working against your health that antioxidants have
become more important than ever.
The Benefits of
Antioxidant Supplements
One of the things
that has been discovered through antiageing
research is that to achieve optimal health and live longer, we need high levels
of antioxidants in our bodies.
Unless you were blessed
with superior genes, you won't have these higher levels without an
antioxidant-rich diet and antioxidant supplements. These are the key components
for a longer and healthier life.
Some of the
immediate, specific benefits of antioxidants supplements that people have
reported include:
Weight
loss
Increased
energy
Younger-looking
skin
Lower
cholesterol
Stronger immune system
Relief
from inflammation
Back and joint pain relief
Relief
from arthritis
Better
sex life
Improved
sleep
Improved
memory and concentration
In addition,
antioxidant supplements have been shown to be effective against a wide variety
of health problems including:
Heart
disease
Cancer
Alzheimer’s
Arthritis
Cataracts
Diabetes
Glaucoma
Macular
degeneration
Gum
disease
Diseases
of the immune system
Strokes
3. Causes of ageing
a. Free
radicals & Oxidative Stress
Antioxidants
protect your cells from excessive attacks by destructive elements called free
radicals. Free radicals play a significant part in the aging process and
the development of degenerative diseases. This process is known as oxidative
stress, or oxidation. You've seen this process many times before, as in rotting
fruit or rusted metal. Your body ages in much the same way,
except it happens from the inside out. Free radicals may cause some
diseases all on their own, but more often, they weaken your immune system and
make your body vulnerable to diseases caused by other factors.
The
Aging Process.
You've seen
oxidation at work before, when you’ve sliced an apple and let it sit out for
awhile, or when you've seen rusting metal. Your body ages in
much the same way, except it's from the inside out. The aging process
results in loss of muscle tone, stiffening of tissue, and dry, wrinkled skin.
Aging also reduces
the number of healthy cells in your body. As more cells are affected and die
off, your body loses its ability to respond to infections and free radical
attacks. Eventually, this manifests in some kind of disease
"Free radicals
appear to play a central role in virtually every disease you can name, either
directly or secondarily... which disease develops depends on the site of the
free radical attack."
b.
Environmental
Sources of
oxidative stress, and the free radical reaction that causes it, are all around
you. They fall into the following general categories:
Environmental
toxins and pollution
Pesticides
and herbicides
Emotional
stress
Strenuous exercise
Chronic illnesses
Processed
foods and food additives
Chronic inflammation
Smoking
Ultraviolet
radiation from the sun
Electromagnetic
radiation
We Don't Eat Enough
Fruits and Vegetables.
Statistics show
that very few people in western cultures eat six or more servings of fresh
fruit and vegetables every day, as recommended. These are the best sources of
antioxidants in your diet.
Overeating —
Another of the Major Causes of Aging.
Another factor in
increased free radical production is the fact that many of us eat more calories
than we need. Food requires oxygen to convert it into energy. The more you eat,
the more oxygen is used, and the more free radicals are produced.
Industrial
Agriculture
Industrial
Agriculture Leads to Less Nutritious Foods. Due to the growing use of chemical
fertilizers and pesticides, modern crops are being harvested earlier than ever
before. That means produce has less time to absorb nutrients from the soil, and
chemical fertilizers often interfere with a plant's ability to take up those
nutrients.
Selective breeding
to increase crop yield has led to declines in the nutritional value in typical
factory-farmed fruits and vegetables. It has been documented that the average
vegetable found in today's supermarket is anywhere from 5 to 40 percent lower
in minerals (including magnesium, iron, calcium and zinc) than those harvested
just 50 years ago.
Eating Organically
Helps.
According to the Journal
of Applied Nutrition, organically-grown fruits and vegetables have
significantly higher nutritional content than conventional produce:
"Organically grown apples, wheat, sweet corn, potatoes and pears were
examined over a 2 year period and were 63% higher in calcium, 73% higher in
iron, 118% higher in magnesium, 178% higher in molybdenum, 91% higher in
phosphorus, 125% higher in potassium and 60% in zinc than conventionally grown
produce."
Genes
Genes Only Play a
Small Part in Your Rate of Aging - Some of your ability to protect
yourself from oxidative stress is determined by the genes you inherited. Each
individual body has a different capacity to produce antioxidant enzymes than
will defend against free radical attacks. This is one explanation of why things
like certain diseases and lifespan sometimes "runs in the family."
However, only about
10-20 percent of your rate of aging is dependent on your genes. The rest has to
do with your diet and lifestyle choices. This means that you are in control of
most aging factors.
Antioxidants Can
Trump Genetics - Although you can't do anything about the genes you
were born with, getting sufficient antioxidants can actually help your body
overcome any handicaps you may have inherited. You see, antioxidants have to
ability to control gene behavior; they have the
ability to actually turn good genes on and bad ones off!
Antiageing
nutrition and disease prevention
Many antioxidants
have been used for centuries in ancient and modern cultures around the world
for various diseases.7 In addition to their antioxidant activity,
most of them possess numerous other biologic properties, e.g.,
they can be anticarcinogenic and anti-inflammatory.
This article will discuss antioxidants that are currently marketed in cosmetic
formulations and will focus on their antioxidant activities.
Vitamin E
Vitamin E (tocopherol) is a lipid-soluble antioxidant that is present
in the skin and found in various foods, such as vegetables, seeds, and meat.8
There are 8 active isoforms
that are grouped into tocopherols and tocotrienols. Of the 4 tocopherols
(á-, â-, ã- and ä-), á-tocopherol (AT) has the
highest activity. In animals, a topical application of á-tocopherol
has been shown to exert photoprotective effects by
reducing the number of sunburn cells,9 reducing ultraviolet B
(UVB)-induced damage,10 and inhibiting photocarcinogenesis.11 In humans, tocopherol 5%-8% cream that was applied to the face
improved signs of photoaging when compared with
placebo.12 Furthermore, application of vitamin E (5%) to human skin
under light-tight occlusion 24 hours before UV treatment was shown to inhibit
human macrophage metalloelastase, a member of the
matrix metalloproteinase family involved in the degradation of elastin.13
Newer studies suggest that the combined application of various antioxidants can
increase their potency when compared with 1 antioxidant alone, and consequently
can provide superior photoprotection, as has been
shown for the combination of vitamins E and C.14 Topical application
of vitamin E has been linked with various cutaneous
side-effects, including contact dermatitis.15-17
Coenzyme Q10
(CoQ10), or ubiquinone, is a fat-soluble antioxidant
that is found in all human cells as a component of the respiratory chain, as
well as in food, e.g., fish and shellfish. Up to 95% of the body’s energy
requirements seem to be provided by CoQ10.18 In vitro studies showed that CoQ10
suppressed the expression of collagenase following
ultraviolet A (UVA) irradiation.19 In human skin, few studies
exist on the topical effect of CoQ10. Nevertheless, CoQ10 is a popular topical
antioxidant included in several over-the-counter (OTC) cosmetic products. No
side-effects with topical application of CoQ10 have been reported to date.
The synthetic
analog of coenzyme Q10 is called idebenone,
which has been demonstrated to be stronger than CoQ10 and other well known
antioxidants.20 In humans, a study with a topical skin care
formulation containing idebenone showed positive
effects on photodamaged skin (i.e., reduction in skin
roughness/dryness, reduction in fine lines/wrinkles).21 However, the
effects on wrinkles were most likely due to hydration or skin irritation. There
is 1 report of contact dermatitis attributed to idebenone
0.5% in a cream.22
However; the authors have seen many patients who developed contact dermatitis
from skin care products containing idebenone.
Lycopene, a
powerful antioxidant, is a carotenoid found in red
fruits and vegetables. It is, in fact, responsible for their red color.23
Its chemopreventive effects
against photo-induced tumors have been proven in
mouse models.24 Despite very little clinical data, lycopene
is included in various skin care products.
Vitamin C
In humans vitamin C
(ascorbic acid) can be obtained solely from food, such as citrus fruits.
Sunlight and environmental pollution can deplete vitamin C present in the
epidermis25 and because vitamin C is a potent antioxidant, enhancing its levels
in the skin seems reasonable. Vitamin C predominantly exists in its reduced
form, ascorbic acid. Its oxidized form, dehydro-L-ascorbic
acid can be found in trace quantities and can revert back to ascorbic acid.
However, if the lactone ring irreversibly opens, diketogulonic acid is formed, which is no longer active.
This happens when vitamin C preparations are oxidized,
rendering them ineffective and useless.26 Thus, vitamin C
preparations should be kept in airtight, light-resistant containers to avoid
exposure to UV rays or the air.
Topical vitamin C
as a photoprotectant has been studied in vitro and in
vivo, demonstrating its effects in preventing sun damage by reducing sunburn
cells and decreasing erythema when exposed to both
UVA and UVB irradiation.27 The addition of topical vitamin C to
either a UVA or UVB sunscreen was shown to improve sun protection when compared
with sunscreen alone.28 Furthermore, adding topical vitamin C to
“after–sun” products has been shown to scavenge UV-induced reactive oxygen
species.29
Ascorbate is
required for collagen synthesis30 and the addition of ascorbic acid
increases collagen production in human skin fibroblasts.31 At the
same time it may reduce production of elastin by an
unknown mechanism.32 Two studies in humans have shown an improvement
in the appearance of wrinkles upon topical application of vitamin C.33,34 However,
more clinical trials are necessary to unravel all the effects of vitamin C on
skin and aging. Thus, vitamin C preparations are useful in preventing or
lessening the detrimental effects of UV radiation. Some patients experience
minimal discomfort (stinging and mild irritation) from topical application.
Green tea is a very
popular beverage as well as an antioxidant, that is
extracted from the plant Camellia sinensis. There are
4 major polyphenolic catechins,
of which Epigallocatechin 3-gallate (EGCG) is the
most abundant and biologically active. The green tea polyphenols
(GTP) possess not only antioxidant activity, but they also act as
anti-inflammatory and anticarcinogenic agents. GTP can
be administered either orally or topically.35 With
various in vitro and in vivo studies, green tea is probably the most studied
antioxidant. In vivo topical application of GTPs has been shown to suppress
chemo- and photocarcinogenesis in mice,36 and prevent UV-induced oxidative damage and
induction of matrix metalloproteinases.37 In human skin, GTPs
reduced UV-induced erythema, the number of sunburn
cells, immunosuppression, and DNA-damage.38
In spite of the limited data in humans, there are numerous OTC products
containing green tea, and using them every morning for photoprotection
in combination with a sunscreen makes sense. As with most of the antioxidants,
no controlled clinical trials exist and the concentration of phenols in the
various products is not standardized.
Silymarin,
derived from the milk thistle plant, Silybum marianum, is a natural polyphenolic
flavonoid. Its main component silybin
(silibinin), is considered
to be the most biologically active with strong antioxidant properties.39
In vivo studies have shown photoprotective effects
with topically applied silybin prior to, or
immediately after, UV irradiation.40 Thus, there is reasonable
evidence to include the compound into sunscreens.
Coffee Berry (VDF
Future Ceuticals) is the proprietary name for an
antioxidant extracted from the fruit of the coffee plant Coffea
arabica. It has been shown to be a stronger
antioxidant than green tea, pomegranate extract, vitamins C and E.41 It contains polyphenols, which are
well known for their antioxidant properties.42 In 2007, a product containing
Coffee Berry polyphenols 1% (Revalé
skin, Stiefel Laboratories) was launched. The company
claims that its use over a 6-week period can result in significant improvement
of hyper pigmentation, fine lines, wrinkles, and overall appearance.
Furthermore, there have been no reports of irritation by patients with
sensitive skin. However, further prospective, randomized and controlled human
studies assessing the antioxidant effects of topical preparations containing
Coffee Berry extract are needed.
The antioxidant resveratrol is a polyphenolic phytoalexin compound that is found in grapes, nuts, fruits,
and red wine, among others.43 In vitro and in vivo studies have shown that,
when topically applied, resveratrol protects against
UVB-mediated cutaneous damage and inhibits
UVB-mediated oxidative stress.44-46 The
effect of resveratrol on human skin and photoaging remains to be examined. It is included in a few
products that claim to have antiaging benefits.
Grape seed is
extracted from Vitis vinifera
and is rich in proanthocyanidins, which belong to the
flavonoid family. Proanthocyanidins
are potent antioxidants with strong free radical scavenging activities.47
Grape seed extract has been shown to be an even stronger scavenger of free
radicals than vitamins C and E.48 A possible antioxidant mechanism
of photoprotection by grape seed proanthocyanidins
(GSP) was suggested by Mittal, et al.49
GSP was shown to inhibit the depletion of antioxidant defense
components induced by UVB,50 and topical application of grape seed
extract seems to enhance the sun protection factor in humans.43 It
is included in topical cosmetic formulations for antiageing
purposes.
Pomegranate extracts
can be obtained from various parts of the fruit Punica
granatum, such as the juice, seed, and peel. In
particular, the phenolic components have potent
antioxidant activity.51 Topical application of the peel extract was
shown to restore catalase, peroxidase,
and superoxide dismutase enzyme activities in vivo.52 The fruit extract has
been shown to ameliorate UVA-mediated damages,53 and protect against
the adverse effects of UVB radiation in vitro.54 Pomegranate extract
is available in various skin care products.
Genistein is an isoflavone derived from soybeans with the capacity to
inhibit UV-induced oxidative DNA damage.55 Genistein,
either topically applied or orally supplemented, was shown to effectively
protect human skin against UVB-induced skin photodamage.56, It is
included in various products such as facial moisturizers, sunscreens, and other
skin care formulations that claim to provide anti-aging effects.
Pycnogenol can be
extracted from the French maritime pine (Pinus pinaster). It contains flavonoids and phenolic
compounds, which act as potent free-radical scavengers. Immunosuppression
and a reduction of the inflammatory sunburn reaction were observed in mice
after topical application of pycnogenol 0.05%–0.2%.58
The potential of pycnogenol
to provide photoprotection for humans has been
investigated for oral supplementation, showing that a significantly elevated UV
radiation level was necessary in order to reach 1 minimal erythema
dose.56
Niacinamide, or nicotinamide, is the biologically active amide of vitamin
B3. Besides its antioxidant activity, it has also been shown to exhibit
anti-inflammatory, depigmenting, and immunomodulant properties. The use of niacinamide
has been shown to improve the texture and tone of the skin, and reduce fine
lines, wrinkles, and hyperpigmentation.57 Topical niacinamide is well tolerated and can be found in various
skin care products.
Lipid based novel delivery systems in antiageing
Emulsions: Following
are the different emulsion delivery systems used in cosmetics.
a. Microemulsions: They are stable, transparent
dispersions of oil and water stabilized by an interfacial film of surfactant
molecules and having diameter <100 nm (7).Since microemulsions
were discovered approximately six decades ago, their applications in cosmetics
have increased because of their good appearance, thermodynamic stability, high solubilization power, an ideas of preparation. Penetration
of vitamin E and quercetin was enhanced when employed
in a micro emulsion . Quercetin
en capsulated in micro emulsion did not cause skin irritation and was effective
against UVB induced damage. Microemulsioncontaining ascorbyl palmitate effectively
prevents UVA induced lipid peroxidation 8-10 .
b. Liquid
crystals: Liquid crystalline phase is the intermediary state between solid
and
liquid,
representing a state of incomplete melting. Emulsions containing liquid
crystals have been observed to release active at much slower rate than those
without this stabilizing component. For example, timed release of vitamin A palmitate containing liquid crystals dispersed in
water-based gel 8, 12.
c. Multiple
emulsions: Multiple emulsions are a type of polydisperse
systems, in which the dispersion phase contains another dispersion phase. They
are of two types: w/o/w type and o/w/o type. These are excellent and exciting
potential systems for slow or controlled release of actives. O/W/O multiple
emulsions have potential applications because of more occlusivity
on skin and acceptability. Moreover higher amounts of active substances can be
retained in epidermis and dermis using these systems.
d. Nanoemulsions: These systems are fine oil-in-water
dispersions, having droplet diameter smaller than 100nm with aesthetic
properties i.e. low viscosity and transparency, making these systems suitable
for their application in cosmetics. But, in comparison with microemulsions,
they are in a metastable state and are very fragile
systems by nature14. The nanoemulsion
ofCoQ10 and vitamin E acetate was proven to be a promising cosmetic ingredient
to prevent premature skin aging by protecting the mitochondrial DNA against
UV-induced mutations (15). A study on antioxidant synergy formulation nanoemulsion (ASF) containing different tocopherol
isomers indicated that preparations containing gamma, alpha, and delta tocopherol enhanced anti-inflammatory properties and
increased bioavailability compared to their suspensions16.
2. Vesicular
systems: In several studies, the diffusion of a drug was facilitated or
achieved certain selectivity into human and nonhuman skin by vesicle
encapsulation (85) percent of the papers). Only a few papers claimed that the
vesicles have no effect on the skin (5 percent) 17.
a. Liposomes: Liposomes
are the most widely known vesicular cosmetic delivery systems. These vesicles
contain from one to several concentric lipid bilayers
with intercalated aqueous sections. Topically liposomes
of fer wide ar ray of advantags inuclidei n g
biodegradability, nontoxicity, moisturizing and
restoring action, sustained dermal release and similarity to biological
membranes enabling penetration into epidermal barrier compared to other
delivery systems5. Several drugs and cosmetics in this form are
already commercially available and successfully used, with lesser incidence of
side effects.
b. Phytosomes: Some studies have reported that
phospholipids exhibit a marked affinity for some classes of flavonoids,
a new series of compounds denominated as “phytosome”
has been developed by complexation with polar botanical
derivatives such as catechin, quercetin,
eoscin and glycyrrhetinic
acid. Phytosomes are complexes between a pure phospholipid and pure active principles from the chemical
perspective. The soothing activity of silymarin has
shown to be increased by six fold in silymarin phytosomes compared to free active principles, which is
proposed to be due to higher affinity of complexes for skin phospholipids. The
green tea (polyphenol), grape seed, silybum marianum,
hawthorn extracts and olive polyphenols were successfully
commercialized as phytosomes for antioxidant, free
radical scavenger, uv protectant actions14.
c. T ransferosomes: In the 1990s, transfersomes,
i.e., lipid vesicles containing large fractions of fatty acids, were
introduced. Transfersomes are vesicles composed of
phospholipids as their main ingredient with 10-25 percent surfactant and 3-10
percent ethanol. In consequence, their bilayers are
much more elastic than those of liposomes. Higher
membrane hydrophilicity and flexibility both help transfersomes to avoid aggregation and fusion, which are
observed with liposomes. When applied nonocclusively, they significantly improve skin depose it
ion of a - tocopherol and its photo stability 5,
10.
CONCLUSION:
Incorporation of
antioxidants or radical scavengers in suitable delivery systems is important in
order to transport them as cosmetic ingredients against skin ageing, especially
as curative therapeutic in addition to their prophylactic action. Novel lipid
based delivery systems reviewed here possess the potential to develop as the
new generation smarter carrier systems for topical delivery of antioxidants
REFERENCES:
1. D.L. Madey,
S.R. Pinnell, Operative Techniques in Oculoplastic,Orbital and
Reconstructive Surgery, 4(2),
pp. 62-64 (2001).
2. P.K. Farris, Dermatol Surg., 31, pp. 814-818 (2005). 3. European Congress On
Anti-Aging & Aesthetic Medicine (ECAAAM) 2009.
4. M. Majeed,
L. Prakash, Sabinsa
Corporation, USA, www.sabinsa.com.
5. I.P. Kaur,
M. Kapila et al., Ageing Res. Rev., 6, pp. 271-288 (2007).
6. H. Lautenschlager,
Kosmetik International, 11, pp. 46-48 (2004).
7. E.B. Souto,
R.H. Muller, Nanoparticulate Drug Delivery
Systems. Informa Healthcare USA, Inc, 166, pp. 213-234 (2007).
8. V.B. Patravale,
S.D. Mandawgade, Int. J. of Cosmet.
Sci., 30,pp.19-33
(2008)
9. P. Boonme,
J. Cosmet. Dermatol., 6(4), pp.
223-228 (2007).
10. F.T. Vicentini,
M.J. Fonseca et al., Eur. J. Pharm. Biopharm., 69(3),pp.994897 (2008).
11. C. Lin, M. Lee, Food
Chemistry, 116, pp. 923-928
(2009).
12. R.C. Massaro,
M.S. Zabagli et al., Boll Chim
Farm., 142(7), pp.264-270
(2003).
13. T. Yanaki,
Studies in Surface Science and Catalysis, 132, pp.1009-1014 (2001).
14. O. Sonneville-Aubrun,
J.T. Simonnet, et al., Advances in Colloid and
Interface Science, 108-109,
pp. 145-149 (2004).
15. D. Schmid,
F. Zulli, Cosmetics & Toiletries, 122(1), pp. 71-76(2007).
16. F. Kuo,
R.J. Nicolosi, Int. J. Pharm., 363, pp. 206-213 (2008).
17. J. Frelichowska,
M.A. Bolzinger et al., Int. J. Pharm., 371, pp.56-63 (2009).
18. McDaniel
DH, Neudecker BA, Dinardo
JC, et al. Idebenone: a new antioxidant-Part I. Relative assessment
of oxidativie stress protection capacity compared to
commonly know antioxidants. J Cosmet Dermatol 4(1):10–7 (2005 Jan).
19. assessment
in photodamaged skin of 0.5% and 1.0% idebenone. J Cosmet Dermatol 4(3):167-73 (2005 Sep).
20. Sasseville
D, Moreau L, Al-Sowaidi M. Allergic contact
dermatitis to idebenone used as an antioxidant in an
anti-wrinkle cream. Contact Dermatitis 56(2):117-8 (2007 Feb).
21. Britton G. Structure and
properties of carotenoids in relation to function.
FASEB J 9(15):1551-8 (1995 Dec).
22. Fazekas
Z, Gao D, Saladi RN, et al.
Protective effects of lycopene against ultraviolet
B–induced photodamage. Nutr
Cancer 47(2):181-7 (2003).
23. Thiele JJ, Traber MG, Tsange KG, et al. In
vivo exposure to ozone depletes vitamins C and
E and induces lipid peroxidation in epidermal layers
of murine skin. Free Radic Biol Med 23(3):385–91 (1997).
24. Mclauren
S. Nutrition and wound healing. Wound Care 1:45 (1992). Gilchrest B (Ed.). Photodamage.
London:Blackwell Science
(1995).
25. Darr
D, Dunston S, Faust H, et al. Effectiveness of
antioxidants (vitamin C and E) with and without sunscreens as topical photoprotectants. Acta Derm Venereol 76(4):264-8 (1996
Jul).
26. Cabelli
DE, Bielski BH. Kinetics and mechanism for the
oxidation of ascorbic acid/ascorbate by HO2/O2
radicals: a pulse radiolysis and stopped flow photolysis study. J Phys Chem 87:1805 (1983).
27. Kivirikko KI, Myllyla R. Post-translational
processing of procollagens. Ann NY Acad Sci 460:187-201 (1985).
28. Geesin
JC, Darr D, Kaufman R, et al. Ascorbic acid
specifically increases type I and type III procollagen
messenger RNA levels in human skin fibroblast. J Invest Dermatol
90(4):420-4 (1988 Apr).
29. Davidson JM, LuValle PA, Zoia O, et al. Ascorbate differentially regulates elastin
and collagen biosynthesis in vascular smooth muscle cells and skin fibroblasts
by pretranslational mechanisms. J Biol
Chem 272(1):345-52 (1997 Jan).
30. Traikovich
SS. Use of topical ascorbic acid and its effects on photodamaged
skin topography. Arch Otolaryngol Head Neck Surg 125(10):1091-8 (1999 Oct).
31. Humbert
PG, Haftek M, Creidi P, et
al. Topical ascorbic acid in photoaged skin. Clinical
topographical and ultrastructural evaluation:
double-blind study vs. placebo. Exp Dermatol
12(3):237-44 (2003 Jun).
32. Katiyar
SK, Ahmad N, Mukhtar H. Green tea and skin. Arch Dermatol 136(8):989-94 (2000 Aug).
33. Wang ZY, Agarwal
R, Bickers DR, et al. Protection against ultraviolet B radiation-induced photocarcinogenesis in hairless mice by green tea polyphenols. Carcinogenesis 12(8):1527-30 (1991 Aug).
34. Vayalil
PK, Mittal A, Hara Y, et al. Green tea polyphenols 37. prevent
ultraviolet light-induced oxidative damage and matrix metalloproteinases
expression in mouse skin. J Invest Dermatol
122(6):1480-7 (2004 Jun).
35. Elmets
CA, Singh D, Tubesing K, et al. Cutaneous
photoprotection from ultraviolet injury by green tea polyphenols. J Am Acad Dermatol 44(3):425-32 (2001 Mar).
36. Svobodová
A, Psotová J, Walterová D.
Natural phenolics in the prevention of UV-induced
skin damage. A review. Biomed Pap Med Fac Univ Palacky
Olomouc Czech Repub 147(2):137-45 (2003 Dec).
37. Dhanalakshmi
S, Mallikarjuna GU, Singh RP, et al. Silibinin prevents ultraviolet radiation-caused skin
damages in SKH-1 hairless mice via a decrease in thymine dimmer positive cells
and an up-regulation of p53-p21/Cip 1 in epidermis.
Carcinogenesis 25(8):1459-65 (2004 Aug).
38. Farris P. Idebenone,
green tea, and CoffeeBerry41. ® extract: new and
innovative antioxidants. Dermatol Ther
20(5):322-9 (2007 Sep-Oct).
39. Biological effects and
potential molecular targets. Histol Histopathol 23(4):487-96 (2008 Apr).
40. Afaq
F, Adhami VM, Ahmad N. Prevention of short-term
ultraviolet B radiation-mediated damages by resveratrol
in SKH-1 hairless mice. Toxicol Appl
Pharmacol 186(1):28-37 (2003 Jan).
41. Aziz MH, Afaq F, Ahmad N. Prevention of ultraviolet-B radiation
damage by resveratrol in mouse skin is mediated via
modulation in survivin. Photochem
Photobiol 81(1):25-31 (2005 Jan-Feb).
42. Aziz MH, Reagan-Shaw S, Wu J,
et al. Chemoprevention of skin cancer by grape constituent
resveratrol: relevance to human disease? FASEB J
19(9):1193-5 (2005 Jul).
43. Adhami
VM, Afaq F, Ahmad N. Suppression of ultraviolet B
exposure-mediated activation of NF-kappaB in normal
human keratinocytes by resveratrol.
Neoplasia 5(1):74-82 (2003 ).
44. Vinson JA, Dabbagh YA, Serry MM, et al.
Plant flavonoids, especially tea flavonols,
are powerful antioxidants using an in vitro oxidation
model for heart disease. J Agric Food Chem 43:2800-2
(1995).
45. Bagchi
D, Bagchi M, Stohs SJ, et
al. Free radicals and grape seed proanthocyanidin
extract: importance in human health and disease prevention. Toxicology
148(2-3):187-97 (2000 Aug).
46. Mittal
A, Elmets CA, Katiyar SK.
Dietary feeding of proanthocyanidins from grape seeds
prevents photocarcinogenesis in SKH-1 hairless mice:
relationship to decreased fat and
lipid peroxidation. Carcinogenesis 24(8):1379-88
(2003 Aug).
47. Mantena
SK, Katiyar SK. Grape seed proanthocyanidins
inhibit UV-radiation-induced oxidative
stress and activation of MAPK and NF-kappaB signaling in human epidermal keratinocytes.
Free Radic Biol Med.
40(9):1603-14 (2006 May).
48. Gil MI, Tomás-Barberán
FA, Hess-Pierce B, et al. Antioxidant activity of pomegranate juice and its relationship with phenolic composition and processing. J Agric Food Chem 48(10):4581-9 (2000 Oct).
49. Chidambara Murthy KN, Jayaprakasha
GK, Singh RP. Studie s on antioxidant activity
of pomegranate
(Punica granatum) peel extract using in vivo models. J Agric Food Chem 50(17):4791-5 (2000 Oct).
50. Syed DN, Malik A, Hadi N, et al. Photochemopreventive
effect of pomegranate fruit extract on UVA-mediated activation of cellular
pathways in normal human epidermal keratinocytes. Photochem Photobiol 82(2):398-405 (2006 Mar-Apr).
51. Modulates
UV-B-mediated phosphorylation of mitogen-activated
protein kinases and activation of nuclear factor
kappa B in normal human epidermal keratinocytes
paragraph sign. Photochem Photobiol
81(1):38-45 (2005 Jan-Feb).
52. Wei H, Cai
Q, Rahn RO. Inhibition of UV light- and Fenton
reaction-induced oxidative DNA damage by
the soybean isoflavone genistein.
Carcinogenesis 17:73-7 (1996).
53. Wei H, Saladi R, Lu Y, et al. Isoflavone
genistein: photoprotection
and clinical implications in dermatology. J Nutr
133(11 Suppl 1):3811S-3819S (2003 Nov).
54. Maziere C, Dantin F, Dubois F, et
al. Biphasic effect of UVA radiation on STAT1 activity and tyrosine phosphorylation in cultured human keratinocytes.
Free Radic Biol Med
28(9):1430-7 (2000 May).
55. Sime
S, Reeve VE. Protection from inflammation, immunosuppression and carcinogenesis
induced by UV radiation in mice by topical Pycnogenol.
Photochem Photobiol
79(2):193-8 (2004 Feb).
56. Saliou
C, Rimbach G, Moini H, et
al. Solar ultraviolet-induced erythema in human skin
and nuclear factor-kappa-B-dependent gene expression in keratinocytes
are modulated by a French
maritime pine bark extract. Free Radic Biol Med 30(2):154-60 (2001 Jan).
57. Bissett
DL, Oblong JE, Berge CA. Niacinamide: a B vitamin
that improves aging facial skin appearance. Dermatol Surg 31(7 Pt 2):860-5 (2005 Jul).
58. Cho HS, Lee MH, Lee JW, et
al. Anti-wrinkling effects of the mixture of vitamin C, vitamin E, pycnogenol and evening
primrose oil, and molecular mechanisms on hairless mouse skin caused by chronic
ultraviolet B irradiation. Photodermatol Photoimmunol Photomed; 23(5):155-62 (2007 Oct).
59. Lin FH, Lin JY, Gupta RD, et
al. Ferulic acid stabilizes a solution of vitamins A
and E and doubles its photoprotection of skin. J
Invest Dermatol 125(4):826-32 (2005 Oct).
Received on 19.05.2014 Modified on 30.05.2014
Accepted on 13.06.2014
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