Hydrophilic-Lipophilic Balance
Hydrophilic-Lipophilic Balance
Hydrophilic-Lipophilic Balance
Dispersed phase
Continuous phase
THEORY OF EMULSIFICATION
∆E = OW X ∆A
Not water-resistant
Examples: Hair conditioners, Sunscreen, vanishing cream, Wrinkle
Creams, Mayonnaise, milk, cream and butter.
Water in Oil – W/O
Dispersed phase / Internal phase = WATER
Dispersion medium/ continuous phase /External phase=WATER
Advantages
Waterproofing possible
Most effective for dry skin
Better stability
Disadvantages
Oily, tacky feel
More expensive
Examples: COLD CREAMS
Multiple Emulsions
Multiple phases
Oil in Water in Oil (O/W/O)
Water in Oil in Water (W/O/W)
Advantages
More effective than Oil in Water
Less greasy than Water in oil
Time release, active delivery possible
Disadvantages
Difficult to manufacture
Not always stable
PHARMACEUTICAL APPLICATIONS OF EMULSION
Masking of unpleasant taste:
Most important application of emulsion is for masking the
disagreeable taste of oily liquids by formulating them as o/w
emulsions. For e.g. some vitamins.
Increase the absorption:
Emulsions of oils like liquid paraffin and olive oil enhance the
rate and extent of their absorption from the alimentary canal
due to fine state of subdivisions.
Topically applied:
Medicinal agents that are irritating to the skin are less
irritating if present in the internal phase of emulsion.
Cold cream and vanishing creams are a emulsion which
are used externally.
More acceptable than greasy products (ointments).
PHARMACEUTICAL APPLICATIONS OF EMULSION
Parenteral administrations
Emulsions have been used for the intravenous administrations
of lipid nutrients.
w/o emulsions have been employed to disperse water soluble
antigenic materials in mineral oil for intramuscular depot
injection.
Aerosol
Emulsification is used in aerosol to produce foams
Prolonged Action
These products can also be used for the prolonged release of
drugs that are incorporated into the internal aqueous phase.
Formulation aspects:
Elements of the Formula
Formula Components
Oil Phase
Hydrophobic materials: Oils, fats, lipids
Affects viscosity, spread,
Aqueous phase
Extracts, colorants
Humectants
Thickeners
Emulsifiers
Holds it all together
Types of Emulsifying
agents
Synthetic Natural
Eg. Betains,
Aminoacids,
Lecithin
Advantages
They have greater degree of compatibility than do anionic and
cationic emulgents.
Less sensitive to changes in pH & electrolytes.
They are very useful for parenteral and oral administration because
of their low toxicity and irritancy.
Non-ionic surfactants
Sorbitan esters of fatty acids (Spans)
Sorbitan is esterified with lauric, palmitic, stearic or oleic fatty acid.
Variations in the type of fatty acid produce different Spans:
Span 20 with lauric acid (sorbitan monolaurate)
Span 40 with Palmitic acid (sorbitan monopalmitate)
Span 60 with stearic acid (sorbitan monostearate)
Span 80 with oleic acid (sorbitan monooleate)
Polysorbates (Tweens)
Polyethylene glycol derivatives of the sorbitan esters (Polyoxtethylene
sorbitan ester of fatty acids).
Variations in the type of fatty acid produce different tweens chain with
different oil and water solubility, (Tween 20, 40, 60 and 80).
Advantages of tweens:
o Compatible with other types of surfactants.
o Stable to heat, pH change and electrolytes.
o Low toxicity, for oral and parenteral preparations.
Disadvantages:
o Unpleasant taste.
o Inactivate some preservatives as parabenze by complexation
NATURAL EMULSIFIERS
Only acacia is regarded as primary emulsifier. The rest are used mainly as
emulsion stabilizer. They produce o/w emulsions.
A- Acacia: Its mucilage allow the oil to be sheared into finely divided globules.
However acacia is not viscous enough to prevent rapid rise of globules
(creaming) thus sometimes thickening agents e.g. agar or tragacanth are
added.
B- Tragacanth & Sodium alginate: The emulsifying ability is due to the high
viscosity of its mucilage.
More Polar
(High HLB)
Specific oils need emulsifier with specific HLB (polar/non-polar
character) to be effectively emulsified.
Emulsifiers should have similar HLB values to that of the respective
oils in order to achieve maximum stabilization.
Humectants
• Propylene glycol, glycerol and sorbitol (5%).
• Reduce the evaporation of water from opened package or from the
skin.
• At high concentration they cause dehydration and remove moisture
from the skin.
Antioxidants
Oxidation of vegetable oils cause its rancidity with unpleasant odor
and appearance
They are classified into:
True Antioxidants (oil soluble)
E.g. Butylated hydroxy anisole, Butylated hydroxy toluene,
L-tocopherol (Vitamin E).
they capable of involvement in free radical process, protecting the
oil from involvement.
Reducing agents:
E.g. Sodium metabisulfate, Cystein HCl , Ascorbic acid (Vitamin C).
EDTA as chelating agent retard the oxidation reaction as it
chelate metal ions that catalyze oxidation process.
Methods of Emulsion Preparation:
Conductivity measurements
Systems with aqueous continuous phases will readily conduct
electricity, whereas systems with oily continuous phases will not
since most oils are poor conductors
Staining tests
If a water-soluble dyes is added in an o/w emulsion the emulsion
takes up the color uniformity, phase is continuous phase.
Conversely if the emulsion is w/o type and dye being soluble in
water, the emulsion takes up the color only in the dispersed phase
and the emulsion is not uniformly colored.
2 r2 ( - o) g
V=
9
g = gravity constant
r = radius of the dispersed globules
= viscosity of the external phase
= density of the internal phase
o= density of the external phase
v = velocity of sedimentation of the dispersed spherical particles
From this this law it is clear that velocity is directly proportional to
density difference between the both phase, and radius of the globules.
Inversely proportional to viscosity of the external phase.
B- Coalescence (Breaking, Cracking)
Process of thinning and disruption of the liquid
film between the droplets, with the result that
fusion of two or more droplets occurs to form
larger droplets.
Cracking or coalescence of an emulsion leads
to the separation of dispersed phase as a layer.
Cracking is a irreversible process (permanent loss) .
Preventing Coalescence (Breaking, Cracking)
The coalescence of oil globules in an o/w emulsion is
resisted by the presence, of a mechanically strong
adsorbed layer of emulsifier around each globule.
2) Oxidation
GOOD LUCK ..