Routes of Administration (Topical) Flashcards

1
Q

What are the different ways a drug can be delivered topically?

A
  • Topical
  • Administered at tissue surface (site of therapeutic action) for local condition
  • Minimise systemic effects
  • Transdermal
  • Administered at tissue surface act at a remote site (systemic)
  • Percutaneous: Through skin
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2
Q

Name some formulations for topical use?

A
  • Ointment
  • Creams
  • Gel
  • Lotion
  • Foam
  • Spray
  • Patch
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3
Q

What is an ointment?

A
  • Drug dissolved in greasy base
  • Promotes hydration by minimising transepidermal water loss
  • Difficult to spread, patient acceptability low
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4
Q

What is a cream?

A
  • Semi solid emulsion (commonly oil and water)
  • Oily creams (W/O) w= continuous, O = oil added to water is less greasy than ointments
  • Excellent patient acceptability
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5
Q

What is a gel?

A
  • Semi solid or viscous liquid : often clear or transparent
  • Drug dissolved or dispersed in liquid component
  • May form a film on skin when dried
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6
Q

What is a lotion?

A
  • Typically water based and non-occlusive (doesn’t seal off skin)
  • Solution, suspension or emulsion
  • High spreadability (on hair skin)
  • Short residence time
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7
Q

What is a foam?

A
  • Dispersion of gas within a liquid phase
  • Available as pressurised cans, foam generated during use is stable momentarily
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8
Q

What is a spray?

A
  • Aerosol: dispersion of liquid droplets in gas
  • Fine mist generated. Administered without direct skin contact. Even coverage with large SA
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9
Q

What is a patch/

A
  • Similar to transdermal but for topical delivery
  • Drug on adhesive film
  • Provides dose retention and protection of formulation from environmental contamination
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10
Q

What are the advantages of topical delivery?

A
  • Avoids GI drug degradation and hepatic first pass metabolism
  • Non-invasive
  • Better drug targeting and minimal side effects
  • Easy dose withdrawal (side effects)
  • Convenient/ portable
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11
Q

What are the disadvantages of topical delivery?

A
  • Low skin permeability (skin tries to keep chemicals out) and uptake = slow
  • Skin irritation
  • Hard to determine dose accurately
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12
Q

What are the cellular layers of the skin?

A
  • Epidermis
  • Dermis
  • Hypodermis
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13
Q

What is the epidermis?

A
  • Stratum corneum : dead cells with a protein envelope
  • Permeability barrier.
  • Corneocytes (bricks) = hydrophilic
  • Extracellular lipid matrix (mortar) = lipophilic
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14
Q

What are the dermal drug transport mechanisms?

A
  • Partitioning: from 1 medium into another, solubility driven
  • Diffusion: within the same medium, down concentration gradient
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15
Q

What are transcellular and paracellular pathways for topical dosage forms?

A
  • Transcellular: Straight through cells. One end to another (hydrophilic drugs)
  • Paracellular: Around corneocytes (lipophilic drugs). Corneocytes have hydrophilic centres
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16
Q

What is the shunt pathway?

A
  • Through hair follicles and sebaceous glands
  • Traditionally regarded as negligible due to small skin area
17
Q

What are factors affecting dermal drug transport?

A
  • Drug properties: Lipophilicity, molecular weight
  • Anatomical site: Barrier thickness, hair follicle density
  • Age: thickness of skin, corneocytes enlarge with age
  • Disease: Broken skin, thickened skin
18
Q

What is tape stripping to access topical drug penetration?

A
  • Stratum corneum progressively removed by adhesive tape
  • Drug assayed relative to protein content on strip
19
Q

How do you use the diffusion cell to assess topical drug penetration?

A
  • Skin sandwiched between donor and receptor chambers
  • Statum corneum facing towards donor and administered
  • Receptor C = filled with receptor buffer
  • Only route = from donor to receptor through skin
  • Drug sampled from receptor C and assayed
20
Q

What are the in vivo skin models?

A
  • Human skin
  • Animal skin (pig skin)
21
Q

What are the in vitro skin models?

A
  • Artificial membranes: Bio engineered skin, cheap, ethical