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.

 

Antioxidant for Super foods

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

 

c. Antioxidant Deficiencies

Antioxidant Deficiencies Are One of the Major Causes of Aging. The growing rate of degenerative diseases in our culture today points to an epidemic of antioxidant deficiencies. How did this happen? Well, first, the human body evolved while eating a lot more food, especially fruits and vegetables, combined with a strenuous lifestyle. Today, we live a relatively sedate lifestyle, combined with less nutritious food. At the same time, our rate of exposure to oxidative stress has been climbing dramatically, especially in the last hundred years. The human body has not had enough evolutionary time to adapt to these new stress factors. Biologists say that the we are essentially the same as humans were 40,000 years ago.

 

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

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.

 

Idebenone

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

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

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

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

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.

 

Resveratrol

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

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

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

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

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

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

 

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Received on 19.05.2014          Modified on 30.05.2014

Accepted on 13.06.2014      ©A&V Publications All right reserved

Research J.  Science and Tech. 6(3): July- Sept., 2014; Page 119-127