P15: Ocular Drug Delivery Flashcards

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1
Q

what are ocular dosage forms used to treat

A

belpharis, conjunctivitis, keratitis, trachoma, dry eye

intraocular disorders like glaucoma

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2
Q

what is the anatomy of the eye

A

cornea, pupil, iris, sclera, conjunctiva, aqueous humour, lens, vitreous homour, choroid, retina

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3
Q

what are the advantages of ocular dosage forms

A

drug delivery directly to the site of action, drug available at higher concentration than via oral administration, local application minimises side effects, self-administrations is easy

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4
Q

what are the disadvantages of ocular dosage forms

A

drug retention on eye surface is poor, rapid clearance, low tear volume so loss of dose, frequent dosing required, inconvenience resulting in poor patient compliance, sterile manufacture of dosage forms is essential, local side-effects, ointments can cause blurring of vision

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5
Q

where is the conjunctiva

A

located at the side of the eye and joins on to cornea and eyelids

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6
Q

what is the conjunctiva made from

A

non-keratinised, stratified squamous epithelium with goblet cells and also stratified columnar epithelium
highly vascularised with many microvessels

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7
Q

what does the conjunctiva do

A

produces and maintains tear film

greater permeability than cornea

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8
Q

what three layers is the cornea composed of

A

multi-layered lipid rich epithelium
central aqueous matrix called stroma
endothelium, single-celled and lipid rich

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9
Q

what does the cornea do

A

controls drug diffusion to inner eye
efficient permeation through lipoidal epithelium/endothelium and through aqueous stroma required drugs with oil and water solubility
cornea is avascular and negatively charged

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10
Q

what is lacrimal fluid

A

secreted from lacrimal glands into surface of eye

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11
Q

what is the pH of lacrimal fluid

A

7.4
good buffering capacity that neutralises unbuffered solutions effectively
beffering from carbonic acid, other weak acids and protein

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12
Q

what is corneal absorption

A

major route for ocular drug absorption, transcellular lipophilic and paracellular hydrophilic pathways, little evidence of active transport mechanisms, lipophilic-hydrophilic-lipophilic structure of cornea means that drug should have a degree of water and lipid solubility

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13
Q

what is conjunctival absorption

A

drug passes through conjunctiva and sclera, sclera is fibrous membrane mainly connective tissue to allow permeation of large hydrophilic compounds with poor corneal absorption, most drug is lost into local capillary bed and enters systemic circulation, transporters are present

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14
Q

when are suspensions preferred

A

when drug has chemical stability problems, used when potency of lipophilic drug is greater than that of its salts

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15
Q

how are drug salts chosen

A

solubility to ensure high concentration/driving force for absorption

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16
Q

what are the physical properties of aqueous ocular dosage forms

A

low molecular weight, water and oil solubility, balanced log P

17
Q

how does drug absorption occur across the cornea

A

essential in treatment of glaucoma, weakly acidic and basic drugs in use, lipid-aqueous-lipid nature of cornea structure

18
Q

what vehicle is used in aqueous ocular dosage forms

A

purified water USP

19
Q

how are viscosity modifying agents used in ocular dosage forms

A

hydrophilic polymers control flow rate of drops from dispenser to increase residence times of formulation
they must be filtered during manufacture, easily sterilised by filtration and compatible with other excipients

20
Q

what is polyacrylic acid used for

A

cross-linked form in aqueous gels to treat dry eye syndrome

21
Q

what are some examples of preservatives used in ocular formulations

A

benzalkonium chloride, parabens, organic alcohols, antioxidants

22
Q

what is intraocular drug delivery

A

intravitreal drug injection has become a popular method of treatment of many retinal diseases, including age-related macular degeneration, diabetic retinopathy and retinal vein occlusions
significant increase in frequent of intravitreal injections since introduction of anti-VEGF medications