Industrial pharmacy portion 3rd year pharmacy

Emulsions
Emulsions are liquid disperse systems consisting of at least two immiscible liquids (or two
liquids that are saturated with each other), one of which is dispersed as small globules (internal
or dispersed phase) within the other liquid phase (external or continuous phase), generally
stabilized by a third substance called emulsifying agent. The process of formation of an emulsion
is termed emulsification.

There are two basic types of emulsions

1. Oil-in-water (O/W) emulsion

2. Water-in-oil (W/O) emulsion

However, depending upon the need, more complex systems (referred to as “double emulsions” or
“multiple emulsions”) in which the oil-in-water or water-in-oil emulsions are dispersed in
another liquid medium can be formulated.

By considering particle size, pharmaceutical emulsions can be

1. Macro emulsions (droplets size usually exceeds 10 mm)

2. Mini emulsions (droplets size usually 0.1–10 µm)
3. Microemulsions (droplets size usually 100-600 nm)
4. Nano Emulsions (droplets size usually below 100 nm)

Emulsions can also be classified based on mode of administration into

1. Oral emulsions e.g., castor oil, liquid paraffin

2. External emulsions e.g., creams
3. Parenteral emulsions e.g., vitamins
4. Rectal emulsions e.g., enema.

This article will focus on oil-in-water (o/w) emulsions, water-in-oil emulsions, multiple
emulsions, and microemulsions.

Oil-in-water emulsion
Oil-in-water (o/w) emulsions contain oil droplets dispersed as globules throughout an aqueous
continuous phase. An oil-in-water emulsion is generally formed if the aqueous phase constitutes
more than 45% of the total weight and a water-loving emulsifier, such as sodium lauryl sulfate,
triethanolamine stearate, sodium oleate, and glyceryl monostearate is used. The emulsifier is
present in the external, continuous phase and helps stabilize the interface with the dispersed
phase globules.

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 Industrial pharmacy portion 3rd year pharmacy

Fats or oils for oral administration, either as medicaments in their own right or as vehicles for
oil-soluble drugs, are always formulated as o/w emulsions. Oil-in-water emulsions are non-
greasy and are easily removable from the skin surface. They are used externally to provide
cooling effect and internally to also mask the bitter taste of oil.

Water-soluble drugs are more quickly released from o/w emulsion. O/W emulsions give a
positive conductivity test as water, the external phase is a good conductor of electricity.

Water-in-oil emulsion
In a water-in-oil (w/o) emulsion, the aqueous phase is dispersed as globules in the oil continuous
phase. A lipophilic emulsifier is used for preparing w/o emulsions. The w/o emulsions are used
mainly for external applications and may contain one or several of the following emulsifiers:
calcium palmitate, sorbitan esters (Spans), cholesterol, and wool fats. Thus, the use of a
lipophilic emulsifier enables the formation of w/o emulsions with the oil phase as the external,
continuous phase.

An emulsion is a dispersed system containing at least two immiscible (or partially miscible)
liquid phases. The two phases of emulsions are stabilized by the presence of an emulsifier. The
droplet diameter of the dispersed phase extends from about 0.1 to 10 μM, although particle
diameters as small as 0.01 μM and as large as 100 μM are not uncommon.

This article focuses on the advantages and disadvantages of emulsions.

Advantages of emulsions
The advantages of emulsions as pharmaceutical products include the following:

1. Pharmaceutical emulsions may be used to deliver drugs that are poorly soluble in water but
readily soluble in oils. E.g., in oil-in-water emulsions the drug substance is dissolved in the
discontinuous or internal oil phase. Following oral administration the oil droplets (and hence the
drug) may then be absorbed using the normal absorption mechanism for oils. Some drugs are
more readily absorbed when administered as an emulsion than as other oral comparator
formulations.

2. Pharmaceutical emulsions may be used to mask the bitter taste and odor of drugs, in which the
drug is dissolved in the internal phase of an o/w emulsion. The external phase may then be
formulated to contain the appropriate sweetening and flavoring agents.

3. Drugs that are more stable in an oily phase compared to an aqueous medium can show
improved stability in an emulsion dosage form.

4. Intravenous emulsions of contrast media have been developed to assist in diagnosis.

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5. Emulsion can be used to prolong the release of the drug (especially semisolid emulsions)
thereby providing sustained release action. The oily phase can serve as a reservoir of the drug,
which slowly partitions into the aqueous phase for absorption.

6. Essential nutrients like carbohydrates, fats, and vitamins can all be emulsified and can be
administered to bedridden patients as sterile intravenous emulsions.

7. Pharmaceutical emulsions may be employed to administer drugs to patients who have

difficulty swallowing solid dosage forms.

8. Emulsions provide protection to drugs which are susceptible to oxidation or hydrolysis.

9. Emulsions are used widely to formulate externally used products like lotions, creams,
liniments etc.

Disadvantages of emulsions.

1. Pharmaceutical emulsions are thermodynamically unstable and therefore must be formulated

to stabilize the emulsion from separation of the two phases. This is by no means straightforward.

2. Pharmaceutical emulsions may be difficult to manufacture.

3. Storage conditions may affect stability.

4. Bulky, difficult to transport, and prone to container breakages.

5. Liable to microbial contamination which can lead to cracking.

6. Uniform and accurate dose my not be achieved.

Pharmaceutical suspension is a liquid dosage form containing finely divided, undissolved drug
particles dispersed throughout a liquid vehicle in which the drug exhibits a minimum degree of
solubility. This dosage form is used for providing a liquid dosage form for insoluble drugs.

In an ideal suspension, particles are uniformly dispersed and remain so even after prolonged
periods of time. Even if sedimentation occurs, particles should readily redisperse upon mild
agitation of the container.

Suspensions have a number of therapeutic applications across different routes of administration.

Most suspensions are available in ready-to-use form from the manufacturer. In cases of physical
or chemical incompatibility, they are marketed as reconstitutable medications in unit-dose sachet
or multidose bottles.

Read Also: How to Reconstitute Oral Suspension

This article focuses on the advantages and disadvantages of pharmaceutical suspensions

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Advantages of suspensions dosage form

The following advantages can be obtained by formulating API as a suspension dosage form.

1. Suspensions are a useful drug delivery system for therapeutic agents that have a low solubility.
Although low-solubility therapeutic agents may be solubilised and therefore administered as a
solution, the volume of the solvent required to perform this may be large. In addition,
formulations in which the drug has been solubilised using a co-solvent may exhibit precipitation
issues upon storage.

2. Pharmaceutical suspensions may be formulated to mask the unpleasant/ bitter taste of drug.
E.g. Chloramphenicol.

3. Pharmaceutical suspensions may serve as an alternative means used to administer drugs to

children including paediatric and geriatric patients and older patients who have difficulty
swallowing solid dosage forms.

4. Drug in suspension exhibits higher rate of bioavailability than other dosage forms.
Bioavailability is in following order, Solution > Suspension > Capsule > Compressed Tablet >
Coated tablet.

5. Pharmaceutical suspensions may be formulated to provide controlled drug delivery, e.g. as

intramuscular injections.

6. Chemical stability of certain drugs e.g., Procaine penicillin G can be improved when
formulated as suspensions.

7. Pharmaceutical suspension offers resistance to degradation of drugs due to hydrolysis,

oxidation or microbial activity.

8. Duration and onset of action can be controlled e.g., Protamine Zinc-Insulin suspension.

9. When compared to solution dosage forms, relatively higher concentration of drugs can be
incorporated into suspension products.

Disadvantages of suspensions dosage form

The disadvantages of suspensions as pharmaceutical products include the following:

1. Pharmaceutical suspensions are fundamentally unstable and for this reason, it requires
formulation skill to ensure that the physical stability of the formulation is retained over the
period of the shelf-life.

2. Aesthetic pharmaceutical suspension is difficult to formulate that is they lack elegance.

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3. Accuracy of dosage is less reliable than with solution unless suspension is packed in unit
dosage form.

4. Suspension formulations may be bulky and therefore difficult for a patient to carry.

5. Preparation must be shaken prior to measuring a dose.

6. Pourability and syringeability issues (e.g., injectable suspensions)

7. Crystal formation (Ostwald ripening) and breaking of suspension.

Multiple emulsions

Multiple emulsions are emulsions whose dispersed phase contains droplets of another emulsion.
They can be considered as emulsions of emulsions.

Multiple emulsions can be either

1. Water-in-oil-in-water (w1/o/w2) emulsion

2. Oil-in-water-in-oil (o1/w/o2) emulsion.

Emulsifying a w/o emulsion using water-soluble surfactants (which stabilize an oily dispersed
phase) can produce w/o/w emulsions with an external aqueous phase, which generally has a
lower viscosity than the primary w/o emulsion. Oil-in-water-in-oil (o/w/o) type multiple
emulsions on the other hand consist of very small droplets of oil dispersed in the water globules
of a water-in-oil emulsion.

Both water-in-oil-in-water (w/o/w) and oil-in-water-in-oil (o/w/o) multiple emulsions are of

interest as delayed- and/or sustained-action drug delivery systems. They also have applications in
cosmetics. Multiple emulsions can also be used for the encapsulation of peptides/proteins and
hydrophilic drugs.

Microemulsions
Microemulsions are visually homogeneous, transparent/isotropic systems of low viscosity. In
their simplest form, microemulsions are small droplets (diameter 5–140 nm) of one liquid
dispersed throughout another by virtue of the presence of a fairly large amount of surfactant(s)
and cosolvent(s). Microemulsions have a very finely subdivided dispersed phase, and often
contain a high concentration of the emulsifier(s) and a cosolvent (such as ethanol).

Microemulsions are thermodynamically stable for prolonged periods of time. They can be
dispersions of o/w or w/o. The type of microemulsion (w/o or o/w) formed is determined largely
by the nature of the surfactants. Microemulsions can be used to increase the bioavailability of
poorly water-soluble drugs by incorporating them into the oily phase. Incorporation of etoposide
and methotrexate diester derivative into w/o microemulsion has been suggested as a potential
carrier for cancer therapy.

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References sources
 Dash, A., Singh, S. and Tolman, J. (2014). Pharmaceutics: Basic Principles and Application to
Pharmacy Practice.USA: Elsevier Inc.
 Mahato, R. and Narang, A. (2018). Pharmaceutical Dosage Forms and Drug Delivery (3rd ).New
York: Taylor & Francis Group, LLC.

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