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COSMETIC EXCIPIENTS Dr. R. R. Thenge Professor and Head, Department of Pharmaceutics, Dr. Rajendra Gode College of Pharmacy, Malkapur
Excipients Definition: An excipient is a pharmacologically inactive substance formulated alongside the active pharmaceutical ingredient of a medication. Cosmetic ingredients can generally be derived from a variety of sources, ranging from natural to synthetic substances. Purposes served by excipients : Provide bulk to the formulation. Facilitate drug absorption or solubility and other pharmacokinetic considerations. Aid in handling of “API” during manufacturing . Provide physical, chemical and microbial stability to the formulations. Surfactant, Heumectant , Emollient, antioxidants, Preservatives, Rheology modifiers.
Benefits of Excipients in cosmetics Cosmetic ingredients bring many benefits to consumers. Surfactants are essential for cleansing and foam building in shampoos and body washes. Humectants are frequently used in cosmetics as a way of increasing and maintaining moisture in the skin and hair. In the cosmetic formulating world emollients are ingredients incorporated into products to improve the feel of skin and hair. Rheology Modifiers are ingredients that alter the flow of a product. Additionally, they also alter the feel, offering increased slip and silkiness, and behavior. Antioxidants are ingredients used in cosmetic formulations to increase shelf life of cosmetic products and protect human cells against damages. Preservatives prevent contamination and ensure the longevity of cosmetics and personal care products.
Ideal Properties of Excipients
SURFACTANT Surfactants, are the compound that stabilized the mixture oil and water by reducing the surface tension at the interface between the oil and water molecules.
SURFACTANT Surfactants, or surface-active agents, are an amphiphilic group of molecules, having both a hydrophilic and a hydrophobic (or lipophilic ) part. Amphiphilic = double affinity as a polar- apolar duality Hydrophilic = Lipophobe Polar, high affinity Hydrophobe = lipophile Non Polar, alkyl chain PHOBE Greek roots phobos (fear) PHIL Greek roots philos (Love) Tail or hydrophobic group which has little affinity for water – this group is usually hydrocarbon (alkyl) chain. Head or hydrophilic group which has strong affinity for water & can be neutral or charged.
SURFACTANT
They can perform diverse functions including: cleaning, wetting, emulsification, solubilization , dispersion, foaming and sometimes even penetration enhancement and antimicrobial activity. Due to such an outstanding functional diversity, surfactants may be applied in production and processing of foods, agrochemicals, pharmaceuticals, personal care and laundry products, petroleum, mineral oils, lubricants, paints and many other . The nature of the hydrophilic moiety is commonly used to classify surfactants in four basic categories: anionic, cationic, amphoteric and non-ionic. FUNCTIONS OF SURFACTANT
PROPERTIES OF SURFACTANT In cosmetic products surfactants may serve as detergents (cleansing agents), emulsifiers, wetting or foaming agents, opacifiers, thickening agents, foam depressors, hair conditioners antistatic agents. Hence, the selection of a surfactant for a specific cosmetic product is a delicate task which depends on numerous factors, starting from the intended purpose of the product.
These are gentler than anionic surfactants and have inferior foaming properties than anionic surfactants. These are generally combined with other anionic surfactants to create milder shampoo. The largest group of surfactants consists of non- ionics , which do not dissociate in an aqueous solution. Their major characteristic is good skin and eye compatibility, and depending on the type they are weak to moderate foaming agents. Non-ionic surfactants may serve as cleansing agents (mainly in the combination with anionic surfactants), but are generally used as emulsifiers, dominantly in cosmetic products intended for sensitive skin, baby skin, as well as for everyday skin care. NON-IONIC SURFACTANTS Example Decyl glucoside Laureth (10, 23, 4) PEG-10 Sorbitan Laurate Polysorbate (20, 21, 40, 60, 61, 65, 80, 81) Steareth - (2, 10, 15, 20) Cocamidopropylamine oxide
ANIONIC SURFACTANTS Most of the available shampoos contain one of the anionic surfactants given below, as their primary surfactant. Following sulfates are the harshest anionic surfactant(s) that should be avoided These molecules contain a polar head group which carries a negative charge in slightly acidic, neutral or alkaline aqueous solutions. The most important functional groups are carboxyl ate, sulfate, sulfonate or phosphate Harshest anionic surfactant(s): Sodium Lauryl Sulphate (SLS) Sodium Lauryl Ether Sulphate (SLES) Milder and Gentle Anionic Surfactants: Sodium Cocyl Isethionate Sodium Lauryl Sulphoacetate
CATIONIC SURFACTANTS Due to the positive charge they carry, cationic surfactants are substantive to the keratin of hair which has determined their application in cosmetic industry as hair conditioners agents. On the other hand, some of the cationic surfactants are used as bactericidal agents or emulsifiers. Our hair is negatively charged. The more the hair is damaged, the more negative charge it carries. So, these positive charged cationic surfactants bond to the negatively charged hair and get adsorbed (not absorbed) on the hair shaft, and provide the conditioning effect. Ex. Cetrimonium chloride Cetrimonium bromide Behentrimonium methosulphate Behentrimonium chloride Quaternium-15
AMPHIPHILIC SURFACTANT They are generally used as foam stabilizers and thickening agents, but in the presence of acidic substances they tend to lose those properties. Two groups of these surfactants that may find use in cosmetics are alkylamido alkyl amines and alkyl substituted amino acids. These surfactants provide mild cleansing and are added with other anionic surfactants to reduce the irritation caused by them. They help to boost foam formation when combined with other surfactants. These surfactants cannot be used alone in the products as these do not provide good cleansing properties, so are always to be used as secondary surfactants. Ex. Cocamidopropyl betaine Coco betaine Sodium Cocoamphoacetate Disodium cocoamphodiacetate Disodium cocoamphodipropionate
Mechanism of Action of Surfactant in Shampoo
Mechanism of Action of Surfactant in Shampoo
SURFACTANT USED IN COSMETICS Group Subgroup Structure/Example Characteristics and Application Carboxylates Carboxylated salts/ Soaps CH 3 (CH 2 ) n COO–M+ M= Na, K, NH 4 Cleansing agents used as soap bars for fabric hand wash, skin cleansers (soap bars or liquids), shaving products, deodorant sticks, w/o emulsifiers Ester carboxylates Good foaming properties and substantivity on the hair used in shampoos Ether carboxylates RO(CH 2 CH 2 O) n C H 2 COONa Alkyl polyglycol ether carboxylate , sodium salt Emulsion stabilizers , good wetting and foam stability, stable in the presence of alkali or acid
Group Subgroup Structure/Example Characteristics and Application Sulfates Alkyl sulfates RCH 2 SO 4 –Na+ Sodium alkyl sulfate Properties depend on the chain length and the degree of branching of the hydrocarbon chain, good foaming prop- erties . Categorized as potential irritants but most useful cleansing agents for cosmetics, shampoos, skin cleansers Alkyl ether sulfates RCH 2 O(CH 2 CH 2 O) n SO 3 –Na Sodium alkyl ether sulfate Viscosity of surfactant solution is very sensitive to electro- lytes ; cleansing and foaming agents used in liquid soaps, shower gels, foam baths,shampoos Amide ether sulfates [RCONH(CH 2 CH 2 O) 3 SO 3 ] 2 Mg Magnesium PEG-3 cocamide Magnesium salts show excellent skin compatibility , good foaming agents; mild personal care cleaners Alkyl glyceride sulfates Sulfate RCOOCH 2 CH(OH)CH 2 OSO 4 Na Sodium alkyl monoglyceride sulfate Good foaming properties, foaming booster
Group Subgroup Structure/Example Characteristics and Application Sulfonates Alky sulfonates RCOOCH 2 CH(OH)CH 2 OSO 4 Na Sodium alkyl monoglyceride sulfate Very water soluble, showing good foaming, wetting and emulsifying properties; household products (detergents); acidic skin and hair cleansing compositions Alkyl-aryl sulfonates CH 3 (CH 2 ) n CH 2 SO 3 Na Primary sodium alkyl sulfonate Detergent for household products, fabric care, institutional and industrial products.Low ompatibility with skin, used as hydrotropes and in some anti- seborrheic reparations Sulfosuccinates Sodium linear alkylbenzene sulfonate The monoesters and their derivatives are used in personal care products, especially in shampoos, often in combina - tion with anionic surfactants Fatty acid isethionates and taurides RCOOCH 2 CH(COOR)SO 3 Na Sodium dialkyl sulfosuccinate Good wetting, foaming, and emulsifying properties. Excel- lent compatibility with the skin. Shampoos, bubble baths and cleaning products
Group Subgroup Structure/Example Characteristics and Application Phosphates Esters Alkyl phosphates Alkyl ether phosphates ROPO 3 H 2 Alkyl phosphoric ester High electrolyte nd low pH tolerance, used in acidic household and industrial cleaning products Acyl -Amino Acids and Salts Acyl glutamates RCONHCH( COONa )CH 2 CH 2 COO Na Sodium acyl glutamate Mild for skin and eyes;poor foamers . Shampoos, mildly acidic skin cleansers Acyl peptides RCO(NHC(X)HCO) n NHC (X)HCO Ona Sodium acyl polypeptide (X = amino acid) Mild surfactants , substantivity for hair shampoos, mildly acidic skin cleansers Acyl sarcosides RCON(CH 3 )CH 2 COONa Sodium acyl sarcoside Mild to skin. Shampoos
Sub group Function/Application Fatty alcohols Co-emulsifiers, opacifiers, thickening agents, foam depressors Alkoxylated ( ethoxylated or propoxylated ) fatty alcohols Emulsifiers, wetting agents and solubilizers . Household, industrial and personal care products Ethylene oxide/propylene oxide-block polymers Automatic dishwashing and laundry detergents, rinse aids.Good thickening an gelling properties makes them in- teresting for cosmetic products, they are used as emulsifiers, solubilizing or fluidizing agents. Alkylphenol ethoxylates ( alkylphenol polyglycol ethers) Wetting and washing agents, emulsifiers and solubilizers . Due to ecotoxicological reasons their use is diminished Alkyl polygycosides (APGs) Emulsifiers, wetting and foaming agents. Detergents , personal care cleansers, skin care products. Chemically stable in neutral, alkaline and acidic (pH< 5 ) conditions Ethoxylated Oils and Fats (lanolin and castor oil derivatives ) Emulsifiers, mainly used in cosmetic industry Straight alkanolamides Foamers , foam boosters and foam stabilizers. Household detergent products, shampoos and cleaners
Sub group Function/Application Ethoxylated alkanolamides Thickening, foam stabilizing and dispersing agents. Personal care cleansers Ethoxylated fatty acids Excellent emulsifiers for cosmetic, household and industrial use. Mild cleansers and viscosity agents. Domestic and industrial detergents (degreasing composition) Glycol and glycerol esters and ethoxylated derivatives Food industry, emulsifiers and stabilizers. In pharmaceutical and cosmetic industry they are used as emulsifying agents, oily compounds, refatting agents, emollients and skin conditioners in creams, lotions, ointments, and gels Sorbitan and sorbitol esters and ethoxylated derivatives Emulsifiers, components of oil phase, solubilizers and wetting agents in pharmaceutical, cosmetic and food indus - try, similar to the previous group Alkyl carbohydrate esters (Sugar or Sucrose Esters) Food-grade ingredients used as food additives ( emulsifiers and stabilizers). Mild surfactants which can be used as emulsifiers and cleansing agents with emollient properties. Amine oxides Solubilizers and detergents, compatible with all other surfactants. Shampoos (viscosity agents, reduce eye irritancy, enhance foam properties). Suitable in slightly acidic or neutral formulas. Domestic cleaners (used in association with anionic surfactants). Industrial applications: liquid bleach products, textile industry, foam stabilizers and in anti- corrosion formulations
NONHYDROCARBON SPECIALTY SURFACTANTS Alkoxylated Polysiloxanes Surfactants, which can be classified in the chemical group of organosilicones , are structurallyderived from polydimethylsiloxanes in which some methyl are replaced by hydrophilicgroups that can be of anionic, cationic, or nonionic nature. They are also used in cosmetics and hair care: In cosmetic or personal-care products as emulsifiers in, e.g., protective creams, hydrating body milks, liquid soaps, and shave creams, and In hair care products (e.g., shampoos, conditioners, gels, lotions, foams) Fluorosurfactants Fluorosurfactants form a distinct group of surfactants besides the conventional surfactants based on hydrocarbon chains. Fluorosurfactants differ from hydrocarbon surfactants by the hydrophobic moiety of the molecule, which is made of perfluoroalkyls chains F-(CF2-CF2) n. E.g. use in barrier creams that require good spreading and stable o/w emulsions.
APPLICATIONS Detergency: One of the most common applications of surfactants in cosmetics is for cleansing formulations. When skin and hair get dirty there are really two types of dirt: solid particulates and oily deposits. The oily deposits come from natural sebum which is produced in the hair follicles. Although rinsing the surface with water can remove some of the dirt, oily deposits will tend to adhere to the more lipophilic surfaces of hair and skin. Surfactants in detergent help get rid of these oily deposits.
APPLICATIONS Wetting: Surfactants are also wetting agents that reduce the contact angle between a solution put on a surface and the surface. This property allows surfactants to spread more easily on the surface and inject themselves between the oily deposit and the skin or hair surface. This lifts up the oil and allows it to be removed.
Foaming: Foam is an important characteristic of cleansing cosmetics. It is formed when air is dispersed in a continuous liquid medium. The air bubbles are surrounded by thin layers of liquid, and the surfactants help stabilize the bubbles that are formed and creating foam. APPLICATIONS
Thickening: In a water/surfactant solution in which water is the major ingredient, surfactants align themselves in structures called micelles. These are tiny spherical structures in which the lipophilic tails orient inwards and the polar heads orient outwards toward the water. Micelles are important for the creation of emulsions and for thickening. APPLICATIONS
Emulsification: Another major application of surfactants to cosmetics is in the creation of semi-stable mixtures of oil and water, or emulsions. Emulsions are the creams and lotions that deliver beneficial lipid materials to the surface of skin and hair. They can be simple oil-in-water or water-in-oil emulsions or more complex multiple emulsions. APPLICATIONS
HUMECTANT
A humectant is a substance that is used to keep things moist. Humectants are hygroscopic substances. It is often a molecule with several hydrophilic groups, most often hydroxyl groups, but amines, and carboxyl groups sometimes esterified can be encountered as well; the affinity to form hydrogen bonds with molecules of water is crucial. In embalming humectants are usually added to a solution in cases where the body is dehydrated or emaciated to help restore that tissue to a more natural and hydrated appearance. Structure of humectants The molecular structure of humectants vary widely, but they all have multiple hydroxyl group (-OH) or other hydrophilic sites that can interact through hydrogen bonding with water molecules. For the most part humectants are non-polar molecules compatible with water. HUMECTANT
The way humectants work is that they attract water from either the atmosphere or from the body and bind it to itself via hydrogen bonding. This property known as hygroscopicity can be measured for any kind of humectant. The amount of water that a material can bind at a specific humidity is called the equilibrium hygroscopicity . It is determined by placing a known quantity of a material in a fixed humidity chamber then measuring the change in mass of the material. When this test is done on a common humectant like Glycerin you find that it will absorb 25% of its weight in water when exposed to 50% humidity. Under the same conditions another common humectant, Propylene Glycol will absorb 20% its weight in water. In general, the more moisture a humectant will absorb, the better a humectant it makes for formulations. HUMECTANT
Mechanism of action: Mostly low molecular weight substances with water attracting properties into the stratum corneum . Used along with other components to retain the water content. Indication : Xerosis , ichthyosis Adverse effect: Irritation (urea, lactic acid) Example : Glycerol, propylene glycol, panthenol sorbitol , urea, alpha hydroxy acids, hyaluronic acid HUMECTANT
Ideal cosmetic humectants Although many materials have this humectant property, not all of them work well in cosmetics. There are a variety of characteristics we look for when choosing cosmetic humectants. These include… High moisturize absorption over a wide range of humidities . Consistent moisture content even with changing humidity Non-toxic and safe to use for cosmetics Low odor and low color Low viscosity to make compounding easier Generally non-reactive with other cosmetic ingredients Low cost and readily available HUMECTANT
Glycerin - The most common humectant in cosmetics is glycerin or glycerol. This is a molecule that has three -OH groups on it. It is an odorless, clear liquid that can be derived from natural sources. While it can be found in nature it is primarily manufactured as a bi-product of chemical reactions with fats and oils. It can also be synthesized from petroleum sources. Glycerin is perhaps the most versatile humectant in cosmetics and comes closest to being ideal. Its principle drawback is that at high levels is can feel sticky. When formulating with it you need to keep the levels low or find oth Sorbitol - This is a 6 Carbon sugar that has 6 -OH groups. It can be derived from glucose so can maintain a natural story. It is more hygroscopic than glycerin and doesn’t suffer from the stickiness problem. However, it is more expensive which is why it is not used as extensively as glycerin or propylene glycol. HUMECTANT
Propylene Glycol - This is another common humectant in cosmetics. It is non-toxic, low odor, low viscosity and compatible with many ingredients. It doesn’t absorb quite as much water as glycerin however, it still is excellent for this application. It also doesn’t have the stickiness problem of glycerin and is less expensive. Propylene glycol is similar to glycerin in chemical structure having three Carbon atoms. The main difference is that it only contain two -OH groups. The primary drawback to propylene glycol is that it is synthetically produced from petroleum processing. It also has a bad reputation suffering from misinformation about it on the Internet. But from a formulation standpoint, it is excellent. Butylene glycol - This is a clear, low viscosity liquid that works well as a humectant. It is a 4 Carbon molecule that contains two -OH groups. It is similar in humectancy to propylene glycol and makes a good substitute if you are trying to move away from that material. It is also a more effective solubilizer than both Glycerin and Propylene Glycol. HUMECTANT
PEG - There is a whole range of polymeric humectants based on the polymerization Ethylene Glycol. PEGs with an average molecular weight of 200 - 2000 are the ones that exhibit useful humectancy . When formulating, the higher the PEG molecular weight the less water soluble it will be. Sodium PCA - This humectant is found naturally in human skin so it is often included as part of the Natural Moisturizing Factor. It makes for a good story. It is a highly effective humectant and can bind water 1.5 times better than glycerin. As humectants go, it is one of the best performing ingredients. However, its relatively higher cost has limited its application. Urea - Urea is used as a 10% cream for the treatment of ichthyosis and hyperkeratotic skin disorders, and in lower concentrations for the treatment of dry skin. In the treatmentof onychomycosis , urea is added to a medicinal formulation at 40% as a keratoplastic agent to increase the bioavailability of the drug. HUMECTANT
EMOLLIENT
Emollients are cosmetic preparations used for protecting, moisturizing, and lubricating the skin. These functions are normally performed by sebum produced by healthy skin. The word "emollient" is derived from the Latin verb mollire , to soften. They are mainly lipids and oils, which hydrate and improve the skin softness, flexibility, and smoothness. The skin slip or lubricity contributes to consumer satisfaction. Emollients are available as lotions , creams , ointments , bath oils , or soap substitutes . Petrolatum ( White Soft Paraffin ) is probably the most effective emollient. Other popular emollients are castor oil , cetyl alcohol , cetearyl alcohol , cocoa butter , isopropyl myristate , isopropyl almitate , lanolin , liquidparaffin , polyethylene glycols , shea butter , silicone oils , stearic acid , and stearyl alcohol . EMOLLIENT
Emollients are topical treatments (treatments that are applied directly to the skin). They reduce water loss from the outer layer of skin (epidermis) by covering it with a protective film. Emollients are also sometimes known as moisturizers. Emollients come in several different forms, including: soap substitutes bath oils moisturizing creams and ointments EMOLLIENT
Mechanism of action: Saturated and unsaturated variabel length hydrocarbon which helps in skin barrier function, membrane fuidity and cell signaling leading to overall improvement in skin texture and appearance. Often used in combination with emulsifier. Indication : Skin dryness, roughness, populosquamous disorder and routine skin care Adverse effect: rarely contact irritant Example : Choleaterol , squalene , fatty acid, fatty alcoho , pseudoceramide EMOLLIENT
Emollients may be medicated or non-medicated. Non-medicated topical emollients or moisturizers contain occlusive agents(fat soluble emollients), and humectants( water soluble emollient). Emollients offer an occlusive barrier and they smooth flaky skin cells, to make the skin look smoother. Some spread more easily than others. Esters and oils can be used. Emollients has three basic actions: Occlusion - Occlusive agents coat the skin, forming a physical barrier that prevents the loss of water. EX- Petrolatum, waxes, oils, and silicones. They can be uncomfortable on the skin, so they may be combined with an emollient Humectants - They attract water from the atmosphere and from the lower layers of skin to moisturize the surface of the skin. They can feel sticky, so they will be combined with other elements like emollients. Ex. glycerin, urea and pyrrolidine carboxylic acid. lubrication – reduce the friction when anything rubbed against the skin.. CLASSIFICATION OF EMOLLIENT
CLASSIFICATION OF EMOLLIENT
MEDICATED EMOLLIENTS Some emollients contain specially medicated formulas that can be used to treat skin conditions such as: eczema: a long-term (chronic) skin condition that causes the skin to become reddened, dry, itchy and cracked. psoriasis: a chronic non-infectious skin condition that causes red, flaky patches of skin. CLASSIFICATION OF EMOLLIENT
Emollients can be applied as often as recommended by the manufacturer to keep the skin well moisturized and in good condition. In particular, it is a good idea to regularly apply an emollient to your hands because they are exposed to the elements more than any other part of your body. You may also want to use emollients after: washing your hands having a bath taking a shower Emollients are best applied when the skin is moist and should ideally be applied to the skin at least three or four times a day. WHEN TO APPLY EMOLLIENTS
1) Soap substitutes Certain skincare products can remove your skin's surface layer of natural oils. These include: Soaps, shampoos, ordinary bubble baths, shower gels This can make your skin dry and can further aggravate long-term (chronic) skin conditions such as eczema. Soap substitutes, such as aqueous cream or emulsifying ointment, can be used instead of soap for hand washing and bathing. Aqueous cream can also be used as a substitute for shaving foam. OTHER TYPES OF EMOLLIENT
2) Emollient bath additives Emollient bath additives can be added to a lukewarm bath to help prevent the loss of moisture from your skin. Bath additives can make surfaces slippery, so always use a non-slip mat and be careful when getting yourself or your child out of the bath. Some bath oils include an antiseptic which can help prevent infection. However, these products should only be used occasionally unless the infection is recurrent or widespread. Never use more than the recommended amount of bath additive, If the concentration is too high, it may cause skin irritation, particularly when used with antiseptic bath oils. OTHER TYPES OF EMOLLIENT
Creams Creams contain a mixture of fat and water and feel light and cool to the skin. For this reason many people with eczema prefer creams for day time use. All creams contain preservatives and people can become sensitive to them, although this is not common. AproDerm ® Emollient Cream contains: Active Ingredients: White Soft Paraffin 15%, Liquid Paraffin 6%. Other Ingredients: Ceteareth-20, Macrogol Cetostearyl Ether, Cetostearyl Alcohol, Sodium Hydrogen Phosphate, Phosphoric Acid / Sodium Hydroxide, Euxyl PE 9010, Purified Water. • Storage: • Store below 25°C. Do not refrigerate or freeze. OTHER TYPES OF EMOLLIENT
Lotion • Lotions contain more water and less fat than creams, but are not very effective at moisturising the skin. However, they are useful for hairy areas of the body. Contains the most water and least oil, so are the least effective in moisturising the skin. They usually contain preservatives (ingredients that help to protect the product from bacteria/germs and increase its shelf life) which may cause skin irritation. Lotions are useful for hairy areas such as scalps and areas of weepy skin. OTHER TYPES OF EMOLLIENT
Ointments Ointments do not contain preservatives. Ointments can be very greasy and some people find them cosmetically unacceptable. However, because they are very effective at holding water in the skin, they are useful for very dry and thickened skin. Ointments should not be used on weeping eczema – use a cream or lotion instead. Greasy in nature, they are usually made of white soft paraffin or liquid paraffin and are ideal for very dry or thickened skin. Normally applied at night, they do not usually contain preservatives and are therefore less likely to cause skin reactions. OTHER TYPES OF EMOLLIENT
For best results: Apply emollients and moisturizers after bathing, while the water is still trapped in the skin Use at least three times a day, or according to a doctor's instructions Apply gently, and follow the direction of hair growth Do not rub up and down as this can lead to itching, block hair follicles, and generate heat in the skin Continue to use the emollient after a flareup has cleared, to prevent it from returning Used daily, nonmedicated products can help to keep mild to moderate cases of eczema at bay, and they can reduce the need for corticosteroid creams. Nonmedicated moisturizers have not been found to be toxic, but most are safe during pregnancy and for pediatric use. HOW TO USE EMOLLIENTS
Emollients can be applied as often as you like to keep the skin well moisturized and in good condition. Ideally, this should be done at least three or four times a day. It's especially important to regularly apply an emollient to your hands and face, as they're exposed to the elements more than any other part of your body. Certain activities, such as swimming or gardening, can irritate the skin. It may help to apply an emollient before doing these. It's a good idea to protect babies' hands and cheeks with an emollient before meal times to stop them getting sore from food and drink. Emollients are best applied after washing your hands, taking a bath or showering because this is when the skin most needs moisture. The emollient should be applied as soon as you have patted your skin dry to ensure it is properly absorbed. WHEN TO APPLY:
Possible reactions to emollients can include: Irritant reactions: These include an overheating, 'burning' sensation or stinging. It is usually caused by a reaction to a certain ingredient contained in the cream or lotion. If the stinging is painful and continues, try a different emollient. Folliculitis : Some emollients that work by sealing wounds or cracks in the skin with a protective barrier (occlusive) can occasionally cause hair follicles to become blocked and inflamed ( folliculitis ) and cause boils (painful, red bumps on the skin) Facial rashes: Some facial emollients can cause rashes on the face and can aggravate acne (a skin condition that occurs on the face and commonly affects people during their teenage years). REACTIONS OF EMOLLIENTS
For eczema and psoriasis Moisturizers and emollients are recommended for people with eczema and psoriasis, at any age. People with eczema or psoriasis can finds soap too drying to the skin , Many bar soaps, liquid soaps, and cleansers and perfume products can irritate the skin. Emollient soaps substitutes do not foam but they clean the hands and skin. For children who are at risk of developing infected eczema, bath oils with an antiseptic may offer protection, but these should be used occasionally. The label will state the recommended amount that should be used. A high concentration may cause skin irritation. Emollient creams and ointments are less greasy than ointments, but they might sting after the first application, especially if the skin is very dry. Symptoms normally settle down within a few days. APPLICATIONS
The type of emollient to use will depend on how dry the skin is, and where the emollient will be applied. Aqueous creams or emulsifying ointments are good alternatives for hand and bath soaps, because they do not strip the skin of its surface layer, as most soaps do. Aqueous creams can be used instead of shaving foam. Bubble baths can dry and irritate the skin, but bathing helps to remove skin and dirt that could contribute to infection. Emollient bath additives or bath oils added to bathwater can help prevent the loss of moisture from the skin. Emollients can come in bottles, large pump dispensers, tubes, tubs, and jars. They are mainly sold over-the-counter, without a prescription, but some products need a prescription. ▪ Patients with psoriasis or eczema have extremely dry skin, so they will need to apply emollients more frequently. They may benefit more from medicated emollients which help prevent flare-ups, inflammation, and infection. ▪ APPLICATIONS
These products may be more effective if applied after washing or bathing, when the skin most needs moisturizing. Medicated emollients for psoriasis and eczema may contain corticosteroids, salicylic acid, vitamin D analogs, coal tar, tazarotene , anthralin , tacrolimus , and pimecrolimus . These should be used with a doctor's recommendation, as some of them they may cause itching or irritation, and extensive steroid use can have serious side effects. APPLICATIONS Before After Eczema Condition Before After Psoriasis Condition
PRESERVATIVES Preservatives are substances added to various pharmaceutical dosage forms and cosmetic preparations to prevent or inhibit microbial growth. An ideal preservative would be effective at low concentrations against all possible micro-organism, be nontoxic and compatible with other constituent of the preparation and be stable for the shelf-life of the preparation. Preservatives are Used to prevent spoilage of formulations Reasons of spoilage: Oxidation Microbial growth Absence of preservative causes deterioration Water: responsible for microbe growth Anhydrous preparations: microbes attack Preparation contains oils & fats: both
PRESERVATIVES Ideal Properties of Preservatives It should not be irritant. It should not be toxic. It should be physically and chemically stable. Preservative should be compatible with other ingredients used in formulation. It should act as good antimicrobial agent and should exert wide spectrum of activity. It should act as preservative in small concentration i.e. it must be potent. It should maintain activity throughout product manufacturing, shelf life and usage.
PRESERVATIVES FACTORS AFFECTING EFFECTIVENESS OF PRESERVATIVES pH Concentration Susceptibility of organism Interference by ingredients of cosmetics Influence of solid particles
PRESERVATIVES GUIDELINES FOR SELECTION OF PRESERVATIVES Identify the materials which promotes microbial growth e.g. glycerin, gums, proteins, carbohydrates, cellulose. pH i.e. some are active in acidic or basic Partition of preservatives (Shown activity in oil and water) Least toxic should be selected
PRESERVATIVES Contamination of formulations Separation of emulsions, Product discoloration, Formation of gases and odors in formulations Skin infection to the user.
PRESERVATIVES Some Adverse Affects of Preservatives Parabens : cracked or inflamed skins Quaternium-15: contact dermatitis, especially in those with sensitive skin, an infant's skin Formaldehyde: environment & health problem Sorbic acid: allergic reactions Euxyl K 400, Phenoxyethanol & Methyldibromo glutaronitrile : contact dermatitis
PRESERVATIVES
ANTIOXIDANTS Many drugs are subject to oxidative degradation. Such reaction are mediated by free radicals or by molecular oxygen or removal of hydrogen . Oxidative decomposition is catalyzed by metal, hydrogen and hydroxyl ions. Drugs possessing a favorable oxidation potential will be especially vulnerable to oxidation. Antioxidants : Antioxidants are the compounds which prevents the oxidation of ingredients from the pharmaceutical formulation. They protect the drug product by acting as reducing agent ( eg . ascorbic acid, sodium bisulphite , thiourea ) or preferentially oxidized or by blocking an oxidative chain reaction ( eg . Ascorbic acid esters, butylhydroxy anisole and tocopherols .) which are the true antioxidants. They are added to pharmaceutical formulations as redox systems possessing higher oxidative potential than the drug that they are designed to protect or as chain inhibitors of radical induced decomposition.
ANTIOXIDANTS Typically antioxidants are employed in low concentrations (0.2% w/w) and it is usual for the concentration of antioxidant in the finished product to be markedly less than the initial concentration, due to oxidative degradation during manufacture of the dosage form. Antioxidants may also be employed in conjunction with chelating agents, e.g. ethylenediamine tetraacetic acid, citric acid, that act to form complexes with heavy-metal ions, ions that are normally involved in oxidative degradation.
ANTIOXIDANTS Ideal characteristics of antioxidants It should be effective in low concentrations. It should dissolve readily in the substrate. It must be non-toxic, non-irritant and non-sensitizing. It should not impart any taste, odour or colour to the product. It should be neutral and should not react chemically with other ingredients present. It should be stable and effective over a wide range of pH range and should be of low volatility.
ANTIOXIDANTS MECHANISM OF ANTIOXIDANTS The effect of antioxidants is to break up the chains formed during the propagation process by providing a hydrogen atom or an electron to the free radical and receiving the excess energy possessed by the activated molecule.
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ANTIOXIDANTS Applications of Antioxidants cosmetic antioxidants are ingredients used in cosmetic formulations to increase shelf life of cosmetic products and protect human cells against damages.” The cosmetic antioxidants market study covers natural and chemically derived antioxidants used in various cosmetic products such as skincare, haircare , and makeup. These antioxidants are widely used in various anti-aging, anti-inflammatory, UV protection, moisturizing, and hair conditioning products. Vitamin A, vitamin E, butylated hydroxytoluene (BHT), and butylated hydroxyanisole (BHA) are some of the major antioxidants covered in this study. Aging is a natural phenomenon; however, the consumption of antioxidants can slow down the aging process. The aging population is one of the largest consumers of cosmetic products. With the growing aging population around the world, anti-aging skincare products are in high demand.