Definition of a cream
o A cream is viscous, semi-solid emulsion (either o/w or w/o
depending on the emulsifying agent used)
o Pharmaceutical / medicated cream is a semi-solid dosage form
that contain one or more active pharmaceutical ingredients
dispersed or dissolved in a cream base
Function: Used topically for therapeutic or cosmetic purposes
Topical drug delivery
o Definition: The application of a drug formulation directly to
the skin or mucous membranes to exert a local or systemic
effect
o Why use this route?
Localised effect
Local anaesthetics – numbing of the skin
Anti-inflammatories – treat inflammation on the
skin
Oral route is unavailable
Patients with nausea / vomiting, difficulties
swallowing (paediatrics + geriatrics)
Oral drug delivery is unsuitable
Extremely lipophilic drug – very poor oral
absorption and better absorption through the skin
Bypass hepatic metabolism
o Routes of absoprtion
Transcellular – Through the cells of the stratum
corneum
Intercellular – Between the cells of the stratum
corneum
Appendageal – Via hair follicles, sweat glands, or
sebaceous glands (minor route)
o Factors affecting drug absorption
Factor Simple Explanation
The drug must separate from the cream or ointment base before it can
Release from base
enter the skin.
Concentration A higher drug concentration on the skin surface drives the drug into
gradient the skin faster.
Drugs that are somewhat lipophilic (fat-loving) can pass through the
Lipophilicity
oily skin layers better.
Smaller drug molecules move through the skin more easily than
Molecular size
larger ones.
Diffusion through The drug must pass through the layers of skin, especially the outer
layers barrier (stratum corneum).
o
Types of creams
o o/w creams
- composition: usually contain an equal amount of oil and
water or a lower amount / conc. of oil
small droplets of oil dispersed in an aqueous
continous phase
- emulsifying agents:
synthetic waxes (macrogols, cetomacrogols) – water
soluble bases
self-emulsifying waxes (emulsifying wax)
fatty alcohols (cetostearyl alcohol)
surfactants:
Non-ionic – polysorbates (Tweens – tween 20,
tween 80)
Anionic (-ve charge hydrophilic head group) –
sodium lauryl sulfate (SLS), sodium sulfate
Natural emulsifiers: acacia, gelatin
- Properties / characteristics: white, lightweight (low
viscosity), non-greasy, smooth, spreads easily, rapidly
absorbed, easily water washable
- Uses:
Topical drug delivery of APIs for acute conditions (e.g.
anti-inflammatories, antifungals, local anaesthetics
etc.)
Sooth irritated / inflamed skin – acute eczema
flare-ups, allergic dermatitis, and insect bites
Cosmetic applications (e.g. moisturising creams,
sunscreens etc.)
- Advantages: usually quicker drug release rate (water
facilitates the diffusion), rapid drug absorption, and better
patient acceptability
- Disadvantages: Susceptible to microbial growth – affects
stability (higher water content and often requires a
preservative), short residence time on the skin (can be
easily removed)
o w/o creams
- composition: usually contain a higher amount of oil than
water
small droplets of water dispersed in an oily continous
phase
- emulsifying agents:
Natural emulsifiers: wool fat (lanolin), bees wax, wool
alcohols (absorption bases)
fatty alcohols (cetyl alcohol, stearyl alcohol)
surfactants:
Non-ionic – sorbitan esters (Spans – span 60,
span 80), glyceryl monostearate
- Properties / characteristics: creamy white, heavy feel
on skin (high viscosity), greasy, occlusive (forms a barrier),
difficult to spread (feels sticky), not easily water washable
- Advantages: usually slower drug release rate (suitable for
chronic conditions), long-term stability compared to o/w
creams (less susceptible to microial growth), fewer
preservatives required, emollient (long-term moisturising
and hydrating effect) and provides a protective barrier,
longer residence time on the skin
- Disadvantages: poor patient acceptibility due to sticky,
heavier feel on the skin
- Uses:
Topical drug delivery of APIs for chronic conditions
(e.g. chronic dry skin conditions – psoriasis, eczema)
Emollient therapy and barrier protection (e.g. hand
creams, nappy creams etc.)
Cosmetic application – night creams etc.
o Preparation methods of creams
- Fusion Method
Used for: Emulsifying waxes, oils, and emulsifiers
(aren’t sensitive to heat - thermolabile)
Steps:
Heat the oil phase (oils, waxes, emulsifiers) in a
separate container.
Heat the aqueous phase (water, water-soluble
ingredients) in another container.
Slowly combine the two phases while stirring
continuously.
Allow the mixture to cool, stirring occasionally
until it thickens into a cream.
- Levigation (wet grinding)
Used for: Incorporating solid ingredients into the
cream base.
Steps:
Triturate the solid drug or active ingredient with
a small amount of the cream base or a
levigating agent.
Once smooth, gradually add more base, continuing to
mix thoroughly.
Ensure the mixture is free of grit and uniformly
blended.
-Geometric Dilution
Used for: Mixing small amounts of active ingredients
with a larger base.
Steps:
Take a small amount of the active ingredient
and mix it with an equal portion of the base.
Add an equal amount of base to the mixture
and blend.
Continue adding base in equal portions, mixing
well each time until the entire base is
incorporated.
o Doubling up technique
- involves gradually mixing equal amounts of two substances
in successive steps, doubling the quantity with each step,
until a uniform mixture is achieved
- Used when:
When mixing a small amount of an active ingredient
or colourant into a larger quantity of base
Ensure even distribution and prevents clumping or
uneven dispersion
- If you have 1 g of drug and 15 g of cream base:
Step 1: Mix 1 g drug + 1 g base
Step 2: Add 2 g base (total 4 g), mix
Step 3: Add 4 g base (total 8 g), mix
Step 4: Add remaining 7 g base, mix
Differences between Emulsions and Creams
Properties Cream Emulsion
A liquid or semi-solid
A semi-solid dosage form
Definition system of two immiscible
containing an emulsion base
liquids (oil and water)
Semi-solid (thicker, Usually liquid (but can be
Appearance
spreadable) semi-solid, e.g. in creams)
Broader use – in oral,
Function and Used topically for therapeutic
topical, or parenteral
Application or cosmetic purposes
formulations
Typically contains an O/W or Composed of two
Composition W/O emulsion along with immiscible liquids, one
other excipients dispersed in the other
Hydrocortisone cream (O/W), Milk (natural emulsion),
Example
cold cream (W/O) emulsified oral syrups