Formulation Considerations of
Emulsions
DPH
Semester VIII
Feb , 2025
Asra Abid
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unioffaisalabad
Formulation Considerations
• The choice of oil, emulsifier and emulsion type depends upon its use and
route of administration.
• Emulsion characteristics like droplet size distribution and rheology controls
emulsion stability and therapeutic response can also cause potential
toxicity and chemical incompatibilities.
• So formulation of emulsion with exact pharmacokinetic characteristics and
tissue distribution is important.
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Formulation considerations:
• Basic ingredients are:
• 1. Pharmaceutical oils
• 2. Distilled Water
• 3. Pharmaceutical emulsifiers
• 4. Preservatives
• 5. Antioxidants
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Pharmaceutical Oils:
• Pharmaceutical oils may be simple esters, fixed and volatile oils, hydrocarbons
and turpenoids derivatives.
• Oil can be a medicament or a carrier of drug or a part of mixed emulsifier system.
• The oils with vegetable origin can undergo auto oxidation so an antioxidant is
added to avoid degradation.
• For parentral emulsions the choice is oil is very restricted because of toxicity.
Long chain triglycerides are used for this purpose.
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• Paraffin Oil: It is a transparent, colorless, viscous oil obtained from
petroleum by the process of distillation.
• It is also known as mineral oil or liquid paraffin.
• It is an emollient, lubricant and oleaginous vehicle so it is used as
excipient in many topical preparations.
• It is used in different concentrations.
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Pharmaceutical Emulsifiers:
• Emulsifiers have both hydrophilic and lipophilic portions but only one
dominates.
• They can be classified on the basis of their hydrophilic lipophilic
balance commonly known as HLB value.
• Every emulsifying agent is given a HLB value which indicates its
polarity.
• The HLB values ranges from 40 (sodium lauryl sulfate) to 1 oleic acid.
• The commonly used emulsifiers ranges from [Link] more polar is
the emulsifier, the more is the HLB value.
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Classification Of Emulsifying Agents:
• Emulsifying agents can be classified according to: 1) chemical
structure:
Synthetic Emulsifying Agents
Natural Emulsifying Agents
2) Mechanism of action:
Monomolecular
Multi-molecular
Solid particle films.
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Synthetic Emulsifying Agents
1) Anionic: (pH > 8)
Sodium stearate
Potassium laurate
Sodium dodecyl sulfate
Sodium sulfosuccinate.
Sodium or potassium oleate
Triethanolamine stearate
sodium lauryl sulfate.
2) Cationic: (pH 3-7)
Benzalkonium chloride,
Benzethonium chloride
Quaternary ammonium salts.
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3) Non Ionic (pH 3-10)
Polyglycol,
Fatty acid esters,
Lecithin.
Sorbitan esters (Spans).
Polyoxyethylene derivatives of sorbitan esters (Tweens),
Glyceryl esters.
* * * Cationic and Anionic surfactants are generally limited to use in
topical, o/w emulsions * * *
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Natural Emulsifying Agents
Derived from Plants and Animals:
Vegetable derivatives:
Acacia
Tragacanth
Agar
Pectin
Lecithin
Animal derivatives:
Gelatin
Lanolin
Cholesterol
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Finely Divided or Finely
Dispersed Solid Particle Emulsifiers
These agents form a particulate layer around dispersed
particles. Most will swell in the dispersion medium to
increase viscosity. Most commonly they support the
formation of o/w emulsions, but some may support
w/o emulsions. For Instance,,
Bentonite
Veegum,
Magnesium Hydroxide,
Aluminum Hydroxide
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Auxiliary Emulsifying Agents
• A variety of fatty acids (e.g., stearic acid), fatty alcohols (e.g.,
stearyl or cetyl alcohol), and fatty esters (e.g., glyceryl
monostearate) serve to stabilize emulsions through their ability
to thicken the emulsion..
•.
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• Low HLB Indicates ?
Low number of hydrophilic groups on the Molecule thus imparting
Lipophilic character:
Spans have low HLB numbers, Because of their oil soluble character,
Spans will cause the oil phase to predominate and form an w/o emulsion.
• High HLB indicates ?
• Emulsifier has a large number of hydrophilic groups on the molecule thus
imparting hydrophilic Character.
• Tweens have higher HLB numbers, Because of their water soluble
character, Tweens will cause the water phase to predominate and form an
o/w emulsion.
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HLB value & Application
1~3 Anti-foaming agent.
3~6 W/o emulsifying agents.
7~9 Wetting agents.
8 ~ 18 O/w emulsifying agents.
13 ~15 Detergents.
15 ~18 Solubilizing Agents.
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How to Calculate HLB ????
• Combinations of emulsifiers can produce more
stable emulsions than using a single emulsifier
with the same HLB number. The HLB value of a
combination of emulsifiers can be calculated as
follows:
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Numerical 1:
• What is the HLB value of a surfactant system
composed of 20 g Span 20 (HLB = 8.6) and 5 g
Tween 21 (HLB = 13.3)?
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Characteristics of emulsifier:
• It should be able to reduce the interfacial tension between the two immiscible
liquids.
• It should be physically and chemically stable, inert and
compatible with the other ingredients of the formulation.
• It should be non irritant and non toxic.
• It should be organoleptically inert i.e. should not impart any color, odour or taste
to the preparation.
• It should be able to produce and maintain the required viscosity of the
preparation.
• It should be able to form a coherent film around the globules of e dispersed
phase and should prevent the coalescence.
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Preservatives:
• Preservatives are added to avoid the health hazards because of the
degradation in color, odour or pH due to microbial attack.
• Contamination may be due to the natural raw material water,
processing equipments or patients themselves.
• W/O emulsions are stable than O/W emulsions. Preservatives are not
used in sterilized parentral preparations.
• The examples of preservatives used in oral and topical emulsions are
benzoic acid, parabenzoates, phenoxyethanol and chlorocresol.
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Antioxidants and humectants
• Antioxidants are used to avoid oxidative degradation.
• The examples are butylated hydroxyanisol, butylated hydroxytoluene
and alkyl gallates.
• Humectants are used in topical preparations to lessen the
evaporation of water.
• The examples are propylene glycol, glycerol and sorbitol (5%).
• At high concentrations their effect can be reversed and they can
dehydrate the skin