Anterior segment - ocular surface

Conjunctival Topical Delivery

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  • Topical administration into the inferior fornix is the most common route of ocular drug delivery

  • Typical drop of ocular medication is 50 microlitres
  • The conjunctival sac has a 15-30 microL capacity (dependent on blinking)
  • Most applicators deliver 50-100 microL per drop
    • A substantial amount is lost due to overspill and tear turnover
  • The conjunctival stroma is highly vascular so facilitates effective absorption
  • There is also absorption via the nasal and nasopharyngeal mucosa
  • Factors affecting absorption:
    • Tear film instability affects the time the drug stays in the conj
    • Altered tear film pH can affect drug ionization and its diffusion
      • Precorneal tear film buffers drugs and changes their pH and then their ionization. Purely ionized drugs tend not to penetrate an intact cornea

      • Depending on the status of the drug, it is delivered in a more acidic or alkaline drop solution to ensure more unionised, therefore more lipid soluble to increase corneal absorption

      • However: acidic and alkaline preparations can cause irritation and tearing so increase drug clearance

    • Environmental temperature and humidity
    • Blink rate: increases drug clearance
  • Increased viscosity helps increase time in conj
    • Polyvinyl alcohol
    • Hydroxypropylcellulose 

Hot Topic

The corneal epithelium is a greater barrier to hydrophilic than lipophilic drugs

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