Cosmetics- Excipients

Excipients
1.Surfactants
Surfactants are compounds that lower the surface tension (or interfacial tension) between two liquids,
between a gas and a liquid, or between a liquid and a solid.
The surface-active molecule must be partly hydrophilic (water-soluble) and partly lipophilic (soluble
in lipids, or oils). It concentrates at the interfaces between bodies or droplets of water and those of oil, or
lipids, to act as an emulsifying agent, or foaming agent.

Amphiphilic molecules- hydrophobic tail and hydrophilic head

Hydrophobic part- hydrocarbon chain or ring
Hydrophilic part- polar group such as carboxylic, sulphate or sulphonate group

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 Excipients
• Surfactants are perhaps the most important of all cosmetic ingredients. Surfactants have so many useful
applications that the cosmetic industry probably wouldn't exist without them.
• In cosmetics, surfactants are used for cleansing, foaming, thickening, emulsifying, solubilizing, penetration
enhancement, antimicrobial effects, and other special effects
• When put in a water solution, they naturally create structures with lipophilic portions aligning with lipids and
hydrophilic portions aligning with water.

Function:

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.
• Solid particulates are just naturally picked up from the environment. They remain on hair and skin via Van der
Waals forces.
• 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.

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Excipients
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.
• Wetting also makes the product easier to spread and prevents it from balling up on the surface. This is useful in
cosmetic creams and lotions

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 in wards and the polar heads orient outwards
toward the water. Micelles are important for the creation of emulsions and for thickening

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

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CLASSIFICATION
1. Anionic surfactants
2. Cationic surfactants
3. Non- ionic surfactants
4. Ampholytic surfactants

1.Anionic surfactants
• Surfactants which have negative charge
• These type of surfactants are for cleansing systems such as shampoos, body washes, and facial washes
• Create high foam
• they are relatively inexpensive
• Disadvantages: skin irritation

1. SURFACTANTS HAVING ANIONIC GROUPS CONNECTED DIRECTLY TO HYDROPHOBIC UNIT

Eg:
a. fatty acid soaps
b. Alkyl sulphates
c. Alkyl sulphonates
d. Alkyl aryl sulphonates

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2. SURFACTANTS HAVING ANIONIC GROUPS CONNECTED THROUGH ESTER LINK
Eg:
a. Monoglyceride sulphates
b. Dialkyl sulphosuccinates
c. Polyethylene glycol ester

3.SURFACTANTS HAVING ANIONIC GROUPS CONNECTED THROUGH ETHER LINKS

Eg:
a. Alkyl ether sulphates
b. Phenol ether sulphates
c. Alkyl ether carboxylates

4. SURFACTANTS HAVING ANIONIC GROUPS CONNECTED THROUGH AMIDE LINKS

Eg
a.Alkanolamide sulphates
b. Sucrosinates
c. Taurines

5.SURFACTANTS HAVING ANIONIC GROUPS CONNECTED THROUGH AMIDINE LINKS

Eg: Imidazole sulphates

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❑ Nowadays there is a tendency for companies to get away from using ingredients with the name “sulfate” in them, so
other options are used. Other anionic surfactants include sulfosuccinates, alkyl benzene sulfanate, acyl methyl
taurates, acyl sarcocinates, the isethionates, propyl peptide condensates, monoglyceride sulfates and fatty glycerol,
ether sulfanates. These are all anionic surfactants that have been used in shampoos or body washes.

2.Cationic surfactants
• These are positively charged surfactant molecules. They are not used for cleansing formulas because they don’t clean,
rinse, or foam as well, and they are more irritating—so they have a lot of drawbacks.
• cationics are great for conditioning. They are substantive during use and are the primary ingredients for rinse-off hair
conditioners
• These are further divided into
a. Nitrogenous cationic surfactants
b.Non-nitrogenous cationic surfactant

Nitrogenous cationic surfactants

These are grouped on the basis of a placement of cationic group.
➢ Quaternary ammonium salts in which nitrogen is directly attached to the hydrophobic part
E.g.Alkyl trimethyl ammonium salts
Dialkyl dimethyl ammonium salts
➢ Surfactants in which cationic group separated from the hydrophobic group
E.g.Quaternized amides of ethylenediamene
Quaternized amides of polyethylenediamene
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➢ Surfactants in which cationic group is located in a hetero cyclic ring
E.g. Alkyl pyridinium salts
Alkyl morpholinium salt
Alkyl imidazolinium salts
➢ Dicationic surfactants
E.g.Quarternized diamine salt
Non-nitrogenous cationic surfactant
Eg:Sulphonium salts
Phosphonium salts
3.Non- ionic surfactants
• Do not dissociate into ions when placed in solution
• Depending on the molecular structure these surfactants are more or less polar without charge
• Solubilizes oils and fragrances
• Used in low foaming, gentle cleansing systems like baby shampoo

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a. Aklanolamides
Eg: fatty acid alkanolamide, fatty acid dialkamnlamide
b. Polyethylene glycol derivatives
Eg: Alkyl poly glycol ether, Thioethers
c. Polyethyleneimine derivatives
Eg:Alkyl polyethyleneimine, Polyethyleneimine amide
4.Ampholytic surfactants
• Amphoteric surfactants can have both a negative charge and a positive charge, depending on the pH.
• These materials are also referred to as zwitterionic materials, and they include ingredients such as cocamidopropyl
betaine, cocoamphopropionate, and sodium lauraminopropionate.
• These three ingredients are probably the most commonly used amphoteric surfactants in cleansing products, particularly
in shampoos.
• Amphoterics are used because they have good detergency and are less irritating than the anionics. They also can help
thicken a formula and have a positive effect on foam, as they make the bubbles smaller and feel creamier.
• The main drawback to using them is that they are significantly more expensive and, on their own, don’t really foam well
enough to produce a good shampoo.
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APPLICATION

1.EMULSIFYING AGENTS
➢ Anionic, cationic and nonionic surfactants are used as emulsifying agents.
Anionic
➢ Used extensively in the formulation of hand creams and lotions
E.g. sulfuric esters
They tend to produce O/W type emulsion
Cationic
➢ Only few of them have been used as emulsifying agents
Nonionic
➢ These are compatible with a large number of cosmetics ingredients
E.g. Sorbitan fatty acid ester, Polyol fatty acid ester
Natural surfactants
E.g. Lecithin, Cholesterol, Saponins
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2.FOAMING AND CLEANSING AGENTS
Surfactants for their foaming and cleansing properties are used in shampoos
➢ Anionic
Eg: alkyl sulphates
➢ Cationics
• inferior cleansing and foaming properties
• These have affinity for proteins which may result in redeposition of dirt on hair fiber
• Irritant to eye
• Used as additives in small quantities(below 5%)
E.g., cetyl pyridinium salts
➢ NonIonics
• Devoid of irritation to eye mucous
• These can be used as main surfactants foe shampoos
E.g. sorbitol esters
➢ Amphoterics
• Used in the preparation of mild shampoos
• Compatible with other detergents
• Also contribute to the conditioning effect on hair
E.g Betains, Imidazoline derivative

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3.WETTING AGENTS
➢ All surfactants have wetting properties, the degree of wetting may differ
E.g. Alkyl ether sulphates

4.SOLUBILIZATION
➢ All surfactants above the CMC have solubilizing properties

2. EMOLLIENTS
Definition
Emollients is a humectant, a lubricant and an occluder. Occlusion put a layer of oil on skin’s surface, slowing down
water loss. A humectant enhances the surface of the skin’s capacity to hold water. A lubricant reduce friction when
anything rubs against the skin. or

Emollients are moisturising treatment applied directly to the skin to sooth and hydrate it. They cover the skin with
protective film to trap the moisture.

• Used for protecting, moisturizing and lubricating the skin

• Cosmetic ingredients which help to maintain the soft , smooth and pliable appearance of the skin; They function
by their ability to remain on the skin surface or in stratum corneum to act as lubricant, to reduce flaking, and to
improve the skin’s appearance.
• They reduce water loss from outer layer of skin (epidermis ) by covering it with a protective film
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• Emollients are available as lotions, creams, ointments, bath oils or soap substitutes
• Petrolatum( white soft paraffin) most effective emollients
Emollients may be medicated or non medicated.
• Non medicated Topical emollients or moisturizers contain occlusive agents ( fat soluble emollients) and
humectants( water soluble emollients)
• Emollients offers 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

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Medicated emollients
• Some emollients contain medicated formulas that can be used to treat some skin conditions such as

➢ Eczema: A long term(chronic) skin condition that causes the skin to become reddened ,dry, itchy and cracked.
➢ Psoriasis: Chronic non infectious skin condition that causes red, flaky patches of skin

CLASSIFICATION OF EMOLLIENT MATERIALS

➢ Hydrocarbon oils and waxes: mineral oil, petrolatum,paraffin, ceresin, ozokerite.
➢ Silicone oils: dimethyl polysiloxane, methyl phenylpolysiloxanes
➢ Triglyceride esters: vegetable and animal fats and oil
➢ Acetoglyceride esters: acetylated monoglycerides
➢ Ethoxylated glyceride: ethoxylated glyceryl monostearate
➢ Alkyl esters : hexyl laurate, isohexyl laurate, isohexyl palmitate,decyl oleate
➢ Alkenyl esters : oleyl myristate, oleyl stearate, oleyl oleate
➢ Fatty acids : stearic, myristic, palmitic acids
➢ Fatty alcohols : lauryl, myristyl, cetyl, stearyl alcohol
➢ Fatty alcohol ethers : ethoxylated lauryl, cetyl, stearyl,isostearyl and lanolin alcohols
➢ Ether-esters : fatty acid esters of ethoxylated fatty alcohol
➢ Lanolin and derivatives: lanolin, lanolin oil, lanolin wax, lanolin alcohols, lanolin fatty acids
➢ Polyhydric alcohols and polyether derivatives: propylene glycol,dipropylene glycol, polypropylene glycol 2000, 4000,
sorbitol

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➢ Polyhydric alcohol esters: Ethylene glycol mono and di fatty acid esters, diethylene glycol mono and di fatty acid
esters etc
➢ Wax esters: lanolin(de-oiled wax fraction), beeswax, spermaceti , myristyl myristate, stearyl stearate
➢ Beeswax derivatives: polyoxyethylene sorbitol beeswax
➢ Vegetable waxes: carnauba, candelilla
➢ Phospholipids: lecithin and derivatives
➢ Sterols: cholesterols, cholesterol fatty acid esters
➢ Amides: fatty acid amides, ethoxylated fatty acid amides, solid fatty acid alkanolamine

Lipophilic Emollients
• They produce heavy and greasy feeling on the skin
• Hydrophobic fatty acid esters are an almost unlimited sourse of synthetic emollients and refatteners: they
provide lighter and more pleasant skin feel than oils and waxes
• The feel they impart and their impact on foam is related to the fatty acid chain length: short chain (isopropyl
myristate, octayl octanoate) deliver dryer feel and have less impact on foam than longer ones (Stearates and
isostearates), which are greasier and detrimental to foam quantity and stability
• They are also used as conditioners ( Petrolatum or ceresin, coca butter, mineral oil )
• They reduce the defatting of skin possibly caused by surfactant based cleanser

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Hydrophilic lipids
• They are preferred for foaming skin- cleansing preparations.
• Ethoxylation and propoxylation make lipids more compatible with water and more easily soluble in aqueous
surfactant solution
Lanolin
• Extracted from sheep wool grease, it is a complex mixture of esters of high molecular weight lanolin alcohols
and of lanolin acids
• Lanolin alcohols and lanolin oil are recommended as super fatting agent in soaps
• Ethoxylation of hydroxyl group of lanolin or its derivatives lead to hydrophilic , water-soluble lanolin
compounds, offering a broad range of useful emollients to the formulators
Lecithin
• Natural mixture of polar and neutral lipid
• Vegetable source of lecithin used in personal-care products are soyabean and maize,egg yolk is the only animal
source of lecithin used in cosmetics and toiletries
Silicone derivatives
• Used as Personal care products- polydimethyl silicoxane( dimethicone)
• They are not suitable in water or in surfactant solution: their incorporation into liquid require an emulsification
process
• Viscosity about 100 to several thousand centistokes.
• High to medium molecular weight dimethicone are occlusive, skin protective emollients- used in skin cleanser
• Low molecular weights are dryer emollients- used in skin cleanser
• Good film forming agent, lubricants, imparting a nongreasy, nontacky silky feel compared with heavy metals
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When to apply Emollients
• 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 good idea to regularly apply an emollient to your hands because they are exposed to elements
other than any part of your body.
• You may also want to apply emollients after
✓ Washing your hands
✓ Having a bath
✓ Taking a shower
• Best applied when the skin is moist and should ideally be applied to skin at least 3to 4 times a day
Side effects
• Irritant Reaction
• Folliculitis
• Facial Rashes

Applications
• Emollients are effective for soothing and healing dry skin due Eczema, psoriasis, atopic dermatitis,
hypothyroidism ,diabetes, kidney disease
• Emollients can treat these conditions as well as other skin irritations such as burns from radiation treatments
and diaper rash.

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 3.Rheological additives
• Rheological additives are mainly used to increase storage stability and impart non-Newtonian characteristics to
personal care formulations
• Rheological additives for aqueous and non aqueous formulations are proven tools for use to personal care,skin
care and decorative cosmetics

Classification

1.BASED ON CHEMICAL NATURE

Organic thickeners Inorganic thickeners
Castor oil derivatives Bentonite
Poly amides Hectorite
Poly urea Silicas
Cellulose derivatives Organoclays

2.BASED ON INTERACTION OF THICKENERS

Non associative thickeners
• cellulose derivatives
• gum and starch derivatives
Associative thickeners
• hydrophobically modified poly ether polyurethane
• hydrophobically modified acrylic thickeners
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Aqueous-Phase Additives
•RHEOLUXE Associate Thickeners
•HECTORITE
•BENTONE hydrophilic Clays

Non-Aqueous-Phase Additives
•BENTONE organophilic Clays
•BENTONE GEL
•THIXCIN R Rheological Additive

Aqueous-Phase Additives
➢ Rheoluxe associate thickener
• These are nonionic polymeric thickeners designed specifically for the personal care market
• It consists of urethane and Poly ether Polyol based associative thickeners with superior performance in
difficult systems (high salt levels or with extremes in pH).
• Due to its structure, Rheoluxe is soluble in water, but associates with lipophilic materials to build viscosity
• MOA: Associative thickeners increase the viscosity of aqueous systems through a system of molecular
associations and interactions.

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➢ Hectorite
• It is a unique swelling clay offering several advantages.
• hectorite’s special properties compared with bentonite, are:
•lower iron content
•lighter colour
•higher swelling capacity
•greater gel strength
•no crystalline silica
• Due to its small size, platelet shape and large surface area, hectorite is able to form strong, stable viscous gels.
➢ Bentone hydrophilic clays
• Bentone MA, EW, and LT rheological additives provide thixotropy and suspension control to the aqueous phase.
• Bentone MA and EW form gels by producing an open, 3-dimensional network of the individual clay platelet.
• These are stable across the range ph 6-11 and offer good tolerance to electrolytes
• Bentone LT forms a similar network, but it is strengthened by the presence of a special cellulose, greatly
enhancing stability and thickening characteristics.
• Bentone LT is stable across a broader range, pH 3-11, and is also the least electrolyte-sensitive product.
• Bentone rheological additives are non-abrasive
• The skin feels pleasant and silky quite different to that associated with the majority of cellulose,
polymer and polysaccharide-based thickeners.
• The Bentone products impart a thermostable viscosity comtrol

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Non-Aqueous-Phase Additives
➢ Bentone organophilic Clays
• Hectorite reacts with special vegetable Quaternary ammonium salts to produce organoclays able to thicken
and gel organic liquids
• The correct choice of Bentone additive is determined largely by the polarity of the system to be thickened
• Bentone additives need to be efficiently dispersed using high shear equipment and then to be activated
with the optimum level of a chemical activator, such as propylene carbonate

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➢ Bentone gel
• Bentone gel additives are optimally dispersed and activated pre dispersions.
• Benefits include:
▪ optimally dispersed
▪ high-shear dispersion not necessary
▪ no polar activation required
▪ easy to handle and use
▪ can be added at any appropriate and convenient stage in manufacture
• The use of a Bentone gel enables the formulator, to achieve the maximum efficiency without the need for
shearing and activation.
• On the production scale, time is saved and the highest degree of reproducibility attained, leading to potential
cost savings.
• Bentone gel additives can be added at any convenient suitable stage in the manufacturing cycle.
• Bentone gel additives are very high-viscosity, shear thinning products. The use of medium- to high-shear
• mixing equipment is recommended
➢ Thixcin R Rheological Additive
• For the highest degree of thixotropy in aliphatic liquids,Thixcin R additive is the product to use.
• It gives water repellency, stabilizes emulsions and acts as a stiffening agent in lipsticks and ointments.
• Thixcin R is a castor oil derivative.It requires temperature-controlled activation within the range 55-60°C (130-
140°F) and high-shear mixing to develop its full structure.
• Thixcin R is in compliance with Ecocert; The ecological and organic cosmetics standards

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Application

Lipsticks
• maintain homogeneity in molten and setting stages
• increase high-temperature integrity
• eliminate oil migration
• reduce “creasing” around lips
Mascara
• improve film-build
• increase water-resistance
• eliminate oil migration
Emulsions
• elevate drop-point temperature of water-in-oil creams
• improve emulsion stability
• enable cold-process emulsification
• create novel viscosity effects
UV Sunscreen
• eliminate ultra fine Ti02 skin-whitening problems
• enhance sun protection factor (SPF)
• optimize use of sunscreen actives
• reduce separation and settlement

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Antiperspirant Aerosols
• uniform distribution of active ingredients
• soft and dry skin feel
• significant less whitening
• reduced separation and settlement

4. Preservatives
Preservatives are the chemical substances used to improve or amplify shelf life of drugs by decreasing or lowering
the oxidation of active and excipients and by reducing microbial production.
Ideal requirements of preservative
• Should be free from toxic irritant or sensitizing effects at the concentrations used on the skin or mucous
membrane.
• It should be stable to heat and prolonged storage.
• Should be free from gross incompatibility with other ingredients in the formula and with packaging material.
• Should be active at low concentration and should retain its effectiveness over a wide range of pH values.
• Should be non –volatile.
• Should be readily soluble at its effective concentration.
• Be with odour and colour.
• Be able to retain its activity in the presence of metallic salts of aluminium,zinc and iron.
• Should be non –corrosive to collapsible metallic tubes as well as non injurious to rubber linings

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CLASSIFICATION OF PRESERVATIVES
MECHANISM OF ACTION :
• Antioxidants
• Antimicrobial Agents
• Chelating Agents
SOURCE:
• Naturally obtained
• Synthetically prepared

ANTI-OXIDANTS:
• Anti oxidants are used to reduced the oxidation of active compound and excipients due to formation of free
radicals by using their self reducing activity in finished product.
Eg.
BHA (Butylated hydroxyanisole)
BHT (Butylated hydroxytoulene)
Propyl gallate
ANTI-MICROBIAL PRESERVATIVES:
• It is added in product to minimize risk of spoilage and to kill low levels of contaminants introduced during
storage or repeated use of a multi-dose container.
• These agents mainly work by inhibiting the cell wall, cell membrane growth or other bacterial organelles which
may attack our product.
Eg .Benzoic acid,Methyl parabens,Sodium benzoate, Chlorobutanol, Phenyl mercuric nitrate.
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CHELATING AGENTS:
• Chelating agents act as preservatives and protect product by forming complex with it preventing its
deterioration.
Examples include: EDTA, Citric acid.
NATURAL PRESERVATIVES:-
• These drugs are obtained by natural sources that is plant, mineral sources, animal etc.
Eg. Neem Oil, Salt (sodium chloride), Lemon, Honey.
SYNTHETIC PRESERVTIVES
• These preservative are man made by chemical synthesis active against by various micro-organisms in small
concentration.
Eg. Benzoates, Sodium benzoate Sorbates, Propionates, Nitrites.

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.

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APPLICATIONS

• Ascorbic acid is used as an antioxidant in aqueous pharmaceutical formulations at a concentration of 0.01–0.1%

w/v.
• Ascorbic acid has been used to adjust the pH of solutions for injection, and as adjuvant for oral liquids.
• Ascorbic acid has also proven useful as a stabilizing agent in mixed micelles containing tetrazepam.
• Methyl paraben is widely used as an antimicrobial preservative in cosmetics, food products, and pharmaceutical
formulations.
• Methyl paraben used in ophthalmic preparations.
• Sodium benzoate is used primarily as an antimicrobial preservative in cosmetics, foods, and pharmaceuticals. It is
used in concentrations of 0.02–0.5% in oral medicines, 0.5% in parenteral products, and 0.1–0.5% in cosmetics.
• Sodium chloride is widely used in a variety of parenteral and non parenteral pharmaceutical formulations, where
the primary use is to produce isotonic solutions.
• Sodium chloride has been used as a lubricant and diluent in capsules and direct-compression tablet
formulations.
• Sodium chloride has also been used as a channeling agent and as an osmotic agent in the cores of controlled-
release tablets.
• It has been used as a porosity modifier in tablet coatings, and to control drug release from microcapsules.
• Sodium sulfite is used as an effective antimicrobial preservative, particularly against fungi at low pH (0.1% w/v)

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 5.Humectant
• Hygroscopic material used in cosmetic products used to reduce the loss of moisture content in material in
contact with the product.
• Used to keep cream soft: Vanishing cream
• Possess emollient action: Vanishing cream
• It form thin film on skin when applied, influences the texture & condition of skin, all moisturizing preparation
contains humectants

Ideal properties of humectant

• Must absorb moisture from atmosphere
• Should cause a little change only in water content with the change in RH within normal RH range.
• Compatible with other materials
• Colorless , Good odor & taste.
• Non-toxic, non-irritant
• Non- corrosive to packaging material
• Not solidify or crystallize at normal condition
• Not be too costly
• Viscosity & temperature curve should be relatively flat.

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Types of humectant
Three classes:
• Inorganic
• Metal-organic
• Organic
Inorganic humectants
Example: Calcium chloride
Disadvantages:
• Compatibility problem
• Corrosive nature
➢ Limited use in cosmetics
Metal-organic humectants
Example: Sodium lactate
Advantages:
• Greater hygroscopic power than glycerin
Disadvantages:
problem, Corrosive nature, Pronounced taste
➢ Generally used in skin cream as no risk of toxicity
➢ Admixture of Sodium lactate + lactic acid is used to overcome pH problems.
➢ Limited used in cosmetics

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Organic humectant
• Polyhydric alcohols, their esters & ethers
• Widely used in cosmetics
• Most commonly used are:
• Ethylene glycol, Propylene glycol, Polyethylene glycol ,Glycerol, Sorbitol
Polyethylene glycol
• Polyethylene oxide (PEO), Polyoxyethylene (POE)
• Available in varying molecular weight
• Based on concentration, effectiveness is depends
• PEG 400 = mol. wt. is 400 Daltons

Other humectants in cosmetics

Di-ethylene glycol ,Triethylene glycol , Di- propylene glycol , Polyoxyethylene glycerin , Xylitol ,Mannitol
Sorbiton ,Polyoxyethylene sorbitol , Glucose , Triethanolamine ,Triethanolamine lactate , Urea

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