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829 dosage 2 > exam 3 lecture 9 mucosal > Flashcards

exam 3 lecture 9 mucosal Flashcards

1
Q

mucosal drug delivery

A

via accessible body cavities covered with mucosa –> more permeable
oral (buccal, sublingual, gingival)
nasal
vaginal
intrauterine
rectal
ocular
pulmonary

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2
Q

advantages of mucosal drug delivery

A

avoid first pass
noninvasive
relative ease and convenience

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3
Q

disadvantages mucosal drug delivery

A

small area of absorption
taste
delivery limited MW of drug
local irriation

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4
Q

mucus

A

secreted by globlet cells/ salivary glands
functions: coats entry points, protects underlying tissue, keeps membranes moist
thickness varies: <1 um in oral cavity, 450 um in stomach

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5
Q

mucus components

A

mostly water
mucins (glycoproteins)
lipids
inorganic salts

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6
Q

mucin

A

glycoproteins: 20% proteins + 80% glycosylated carbs
extra large molecules membrane bound or secreted
gel-like structure of mucus
negative charge due to high sialic acid

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7
Q

mucin structure

A

sialic acid (-): carboxylic + hydroxyl groups
galactose
n-acetyleglucosamine
core sugars
protein
- contains cysteine rich domains for disulfide bonds

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8
Q

mucoadhesion

A

hydrogen bonding
state where polymers and mucus are held together by interfacial bonds
prolongs residence time of dosage form on the mucosal surface

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9
Q

puprposes of mucoadhesion

A

controlled released system
enhancement of poorly absorbed drug molecules
immobilization of dosage form at site of action

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10
Q

mechanisms of mucoadhesion

A

electrostatic interaction: positive charge of polymer and negative charge of sialic acid
H-bond
covalent bonding: disulfide bonds between thiolated polymer and cysteine-rich portion of mucin
physical interpenetration

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11
Q

oral mucosal

A

systemic or local
sublingual: more permeable and faster
buccal: less permeable

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12
Q

advantages of oral mucosa

A

avoid first pass
rapid absorption/onset of drug
easy to remove if therapy needs to be discontinued

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13
Q

disadvantage oral mucosa

A

small surface area
limited by taste

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14
Q

sublingual

A

relatively permeable
rapid onset
suitable for frequent dosing
nitroglycerin sublingual tab

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15
Q

buccal

A

relatively less permeable
slower absorption and onset of action
less influenced by saliva
suitable for sustained delivery

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16
Q

drug absorption oral mucosa

A

mechanisms:
-transcellular (intracellular)
-paracellular (intercellular)
absorbed into reticulated and jugular veins
drained into systemic circulation (first pass

17
Q

oral drug characteristics

A

predominantly lipophillic
mostly small MW drugs
maybe hydrophillic macromolecular weight

18
Q

buccal tablets

A

bioadhesive polymer layer (polyacrylic acids, cellulose)
matrix containing API and excipients
ex: oravig (miconazole) + fentora ( cephalon)
applying oravig: flat side on fingertip and push into upper gum

19
Q

atiq

A

cephalon
good bioavailability
lozenge on a stick
dosage form is rotating and dissolving against mucosal tissue
self-administer drugs to oral cavity is either transmucosal or GI absorption

20
Q

buccal patch

A

thinner and more flexible than buccal tabs
less obtrusive and more acceptable to patients

21
Q

advantage of nasal

A

avoids first pass elimination and destruction in GI
rapid absorption of drug molecules
relatively easy and convientn

22
Q

disadvantage nasal

A

possible tissue irritation
rapid removal of drug at site absorption
pathological conditions like cold/allergies may alter nasal bioavail
limited area of drug absorption

23
Q

nasal examples

A

zicam - zinc for cold symptoms
miacalcin - calcitonin for post-menopausal osteoporosis

24
Q

nasal cavity

A

respiratory region: main site for systemic drug delivery
- epithelium covered with mucus for humidification and warming of inhaled air
olfactory region: provides connection from CNS to atmosphere, contains small glands that produce secretions acting as a solvent for odorous

25
Q

nasal vaccines

A

nasal mucosa: first site of contact with inhaled antigens (influenza)
lymphoid tissue underneath nasal epithelium
vaccination against respiratory infections

26
Q

advantage of vaginal mucosa

A

rich blood supply
high permeability to certain drugs
avoidance of first pass

27
Q

disadvantage vaginal mucosa

A

hormone-dependent changes (pH)

28
Q

vaginal delivery systems

A

gels + creams: most widely used, drawback is leakage/mess/applicator
films
vaginal rings: pliable drug delivery device inserted into vagina

29
Q

IUD

A

small plastic device placed into uterine cavity for sustained UID drug release of contraception
local progestogenic effects in UID cavity
zero order release up to 5 years

30
Q

rectal mucosa

A

oral drugs can be admin by lower enteral route through anal portion / rectum
local: IBD
systemic: when oral admin not feasible
suppositories: solid dosage form for rectal insertion
rectal emenas: liquids introduced into rectum and colon via anus
PED and geriatrics

31
Q

ocular

A

local: great need for ocular drug delivery
requirements for ocular drug delivery:
-need to be clear
- good corneal penetration
- prolonged contact time with corneal epithelium
- simplicity of use
- non- irritating, comfortable

32
Q

challenges in ocular delivery

A

loss due to dilution bc of tear film
short residence time
not much flexibility in formulation adjustments

33
Q

ocular dosage forms

A

eye drops - reduce drainage
ointments
ocusert
contact lenses
erodable/ non-erodable implants

34
Q

intraocular implants

A

ciliart neurotrophic factor: proteons neural cells including photoreceptors –> slows retinal degradation
blood-retina barrier: restricts drug access from blood to retina tissue
oscular implant: loaded with human retinal pigment epithelium cells with CNTF gene to produce CNTF in situ

35
Q

encapsulated cell technology

A

semi-permeable membrane
allows oxygen and nutrients to cross and come in
allows drug to come out
does not allow immune cells to come in

829 dosage 2 (17 decks)

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