1_Drug_targeting

Question 1

Who first proposed the concept of targeted drugs?

Answer 1

Paul Ehrlich in 1906.

Question 2

What is drug targeting?

Answer 2

A technique aimed at directing a drug specifically to the intended site of action, increasing efficacy and reducing off-target effects.

Question 3

Why is drug targeting especially important?

Answer 3

In the treatment of diseases where selective action is necessary, such as cancer or infections.

Question 4

List the ideal characteristics for a targeted drug delivery system.

Answer 4

• Should be non-immunogenic.
• Should be physically and chemically stable in vivo and in vitro.
• Should limit drug distribution to specific organs, tissues, or cell targets.
• Drug release rate should be predictable and controllable.
• Carriers must be biodegradable or eliminated without issues.
• Preparation should be easy, reproducible, and cost-effective.

Question 5

What is a narrow therapeutic index?

Answer 5

A small therapeutic window requiring careful administration to avoid toxicity.

Question 6

What are the two primary types of drug targeting?

Answer 6

• Passive Targeting
• Active Targeting
• Physical Targeting

Question 7

What does passive targeting utilize?

Answer 7

Natural distribution patterns of drugs in the body, such as the EPR effect in cancerous tissues.

Question 8

What is the Enhanced Permeability and Retention (EPR) effect?

Answer 8

A phenomenon where nanoparticles accumulate in tumor tissues due to increased permeability of vasculature under pathological conditions.

Question 9

What is the ideal size range for drugs or nanoparticles to utilize the EPR effect?

Answer 9

10 - 500 nm.

Question 10

What is pegylation?

Answer 10

The chemical coupling of polyethylene glycol (PEG) to macromolecules to protect from immune system phagocytosis.

Question 11

What is Doxil?

Answer 11

Doxorubicin encapsulated in PEG-liposomes for passive tumor targeting.

Question 12

What is a common side effect of chemotherapeutics?

Answer 12

Toxicity leading to nausea, fatigue, hair loss, and other adverse reactions.

Question 13

What are the common components of standard breast cancer treatment?

Answer 13

• Anthracyclines
• Cyclophosphamide
• Taxanes

Question 14

What is trastuzumab?

Answer 14

A monoclonal antibody against HER2 that inhibits dimerization and promotes apoptosis of cancer cells.

Question 15

List advantages of targeted drug delivery systems.

Answer 15

• Reduced toxicity
• Decreased harmful effects
• Smaller dose
• Avoidance of first-pass metabolism
• Increased absorption of large molecules
• No peak in plasma concentration
• Selective targeting to infected cells
• Decreased toxicity to non-target cells

Question 16

List disadvantages of targeted drug delivery systems.

Answer 16

• Requires sophisticated technology
• Requires skilled staff for manufacturing
• Drug deposition may cause toxic symptoms
• Stability of dosage form is difficult to maintain
• Low drug loading in formulations
• High cost of storage and formulation