Lecture 13: Transdermal drug delivery in CV Flashcards

1
Q

What are the three layers of the skin?

A
  1. Epidermis
  2. Dermis
  3. Subcutaneous tissue
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2
Q

What cells are found in the epidermis?

A
  • Keratinocytes
  • Melanocytes
  • Langerhans cells
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3
Q

What is found in the dermis layer? (5)

A
  • Sweat duct
  • Sebaceous gland
  • Sweat gland
  • Arrector pili
  • Hair follicle
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4
Q

What is found in the subcateneous tissue?

A
  • Blood vessels
  • Fat lobules
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5
Q

What is the principle barrier of the skin?

A

Stratum corneum

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6
Q

What is the largest organ of the body?

A

Skin

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7
Q

What is the size of the skin?

A

1.8m2

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8
Q

What is the pH of the skin surface

A

pH 5

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9
Q

What are the routes transdermal drugs use?

A
  1. Shunt route
  2. Trancellular route
  3. Intracellular route
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10
Q

What are the physiochemical properties affecting transdermal drug delivery?

A
  • Ability to cross lipid bilayer, especially corneocytes
  • Diffusion through aqueous environment, epidermis
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11
Q

What are the general properties required for transdermal drug delivery?

A
  • Molecular weight < 500
  • LogP in the range of 1 to 4
  • Maximum daily dose of 10mg/ day
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12
Q

Give examples of drugs delivered transdermally (3)

A
  • Estradiol
  • Fentanyl
  • Nicotine
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13
Q

What is ficks law of diffusion?

A

Flux of drug molecules from high to low concentration

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14
Q

What are the five principles of skin permeation?

A
  1. Selection of suitable drug molecule
  2. Release of drug from formulation
  3. Use thermodynamics
  4. Alcohol can help - partitions into skin, sets up a transient reservoir for drug to partition into, drives maximum thermodynamic activity
  5. Occlusion increases delivery of most drugs - Hydrates skin by blocking transdermal water loss, EMLA cream applied under occlusive dressing
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15
Q

How is skin permeation measured?

A

Using franz diffusion cell

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16
Q

What are the advantages of transdermal patches?

A
  • Avoids the harsh environment of the GI tract
  • Drug reaches systemic circulation whilst avoiding 1st pass metabolism
  • Patches can be easily and quickly removed
  • High potent compliance
17
Q

What are the advantages of transdermal patches?

A
  • Avoids the harsh environment of the GI tract
  • Drug reaches systemic circulation whilst avoiding 1st pass metabolism
  • Patches can be easily and quickly removed
  • High potent compliance
18
Q

What are the limitations of transdermal patches?

A
  • Low dose of drug
  • Drug needs to meet specific physiochemical criteria for delivery
19
Q

Name the approved transdermal patches? (9)

A
  • Scopolamine
  • Nicotine
  • Estradiol
  • Fentanyl
  • Buprenorphine
  • Testosterone
  • Glyceryl nitrate
  • Methylphenidate
  • Selegiline MOI
20
Q

What is scopolamine for?

A

Motion sickness

21
Q

What is nicotine for?

A

Smoking cessation

22
Q

What is estradiol used for?

A

HRT

23
Q

What is fentanyl used for?

A

Chronic pain

24
Q

What is buprenorphine used for?

A

Chronic pain

25
Q

What is glyceryl nitrate used for?

A

Angina

26
Q

What is methylphenidate used for?

A

ADHD

27
Q

What is selegiline MOI used for?

A

Parkinsons disease

28
Q

What are the three different types of patches?

A
  1. Simple drug in adhesive patch
  2. Drug in matrix patch
  3. Rate limiting membrane type patch