Aural And Nadal Flashcards
Advantages of the nasal route
• Easy to administer.
• Non-invasive, painless.
• Avoids first-pass effect
• Low enzymatic activity
• Direct route to brain is possible
• Potential to elicit a rapid onset of action.
• Newer formulations potentially allow for peptide delivery.
• Could achieve better systemic bioavailability than the oral
route:
Describe the nasal anatomy
- Split in to 2 halves by nasal septum
- Covered with mucous membrane containing
goblet cells secreting mucus.
• Absorption occurs across turbinates and septum
How are lipophilic and polar drugs transported across the nasal epithelium?
- Lipophilic Drugs: Transported transcellularly via:
• Passive diffusion (concentration-dependent)
• Receptor/carrier-mediated transport
• Vesicular transport mechanisms - Polar Drugs: Pass through epithelial tight junctions (paracellular pathway)
• Limited by molecular size (<1000 Da for effective transport)
What are the key functions of the nose in air filtration and drug delivery ?
• Functions of the Nose = passageway for air to the respiratory tract , Humidifies and warms incoming air
• Large particles trapped in nasal filter undergo rapid clearance
• Particles deposited on mucus are moved by ciliated epithelial cells toward the pharynx
• Site of particle deposition and clearance rate are crucial for local and systemic drug delivery
What is the function of the clearance system ?
• The function of this clearance system is to remove foreign substances from the nasal cavity, and this includes drugs.
What is local drug delivery ?
- Deliver directly at site of action
- rapid relief at lower dose compared to oral
- reduce systemic side effects
- eg. Nasal corticosteroids (reduces nasal mucosa
inflammation)
Why is intranasal delivery useful for systemic drug delivery, and what are some examples?
• Provides rapid onset of action, useful in emergencies.
• Bypasses first-pass metabolism, leading to faster drug absorption.
- eg. Fentanyl: Provides quick pain relief.
• Nasal delivery is effective but has low bioavailability.
How does solubility affect systemic absorption ?
- drug must be in solution to be absorbed