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Dosage II > 22: Mucosal > Flashcards

22: Mucosal Flashcards

1
Q

mucosal drug delivery

A

-via accessible body cavities covered with mucosa
-oral, nasal etc
-systemic or local
-mucoadhesion

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2
Q

Advantages of mucosal drug delivery

A

-avoid first pass
-non-invasive
-ease/convenience

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3
Q

disadvantages of mucosal delivery

A

-small area of absorption
-taste
-limited by weight of drug
-local tissue irritation, sensitivity to pathologic conditions

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4
Q

Mucus

A

-secreted by goblet cells or salivary glands
-mostly water, mucins, lipids, salts
-diffusion barrier for drugs
-target for mucoadhesionm

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5
Q

mucus functions

A

-coats all entry points to human body not covered by skin
-protects underlying epithelial tissues
-keeps mucosal membrane moist = lubrication

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6
Q

Mucin

A

-highly glycosolated proteins
-large molecules either membrane bound or secreted
-provides gel-like structure of mucus
-carries negative charge attributed to high content of sugar

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7
Q

Mucin structure

A

-cystein rich subdomains
-disulfide bonds
-protein and sugars

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8
Q

Mucoadhesion

A

-state in which polymers and mucus are held together by interfacial forces
-prolongs residence time

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9
Q

Mucoadhesion purposes

A

-controlled release
-enhance poorly absorbed drugs
-immobilization of the dosage form at desired state of action

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10
Q

Mechs of mucoadhesion

A

-electrostatic interaction
-hydrogen bonding
-covalent bonding
-physical interpenetration

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11
Q

Electrostatic interaction

A

-positive charged polymer + negative charged sialic acid in mucin

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12
Q

Hydrogen bonding

A

-COOH
-OH
-NH2

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13
Q

Covalent bonding

A

-disulfide bond between thiolated polymer and cysteine-rich portion of mucin

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14
Q

Structures?

A

slides 13-15

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15
Q

Oral mucosal

A

-systemic or local
-sublingual and buccal mucosa

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16
Q

oral mucosal advantages

A

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

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17
Q

oral mucosal disadvantages

A

-small surface area not good for low potency drugs
-limited by taste

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18
Q

slide17

A

slide17

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19
Q

Sublingual oral mucosal

A

-relatively permeable
-rapid onset
-more saliva = more mucus
-suitable for freq dosing and short-term delivery

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20
Q

Buccal oral mucosal

A

-less permeable than sublingual
-slower absorption and onset
-less influenced by saliva
-suitable for sustained delivery applications
-buccal tablets, patches, semisolids

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21
Q

Drug absorption via oral mucosal

A

-epithelium is a barrier
-transcellular
-paracellular by lipids
-absorbed into reticulated and jugular veins = drained into systemic circulation = avoid first pass

22
Q

Drugs delivered via oral mucosa

A

-mostly lipophillic
-mostly small molecular weight drugs
-MAYBE hydrophillic macromolecular weight drugs such as peptides, oligonucleotides, polysaccharides but they likely need enhancers bc saliva enzymes

23
Q

Buccal tablets

A

-bioadhesive polymer layer
-matrix w active ingredient and excipients

24
Q

Buccal tablet examples

A

-Oravig for candidiasis
-Fentora for fentanyl (take buccal first then sublingual if u can handle it)

25
Q

when taking buccal tablet do NOT

A

-crush, split, suck, chew, swallow

26
Q

Actiq

A

-fentanyl citrate
-lozenge on a stick
-rotate and dissolve against oral tissue
-for transmucosal or GI absorption

27
Q

Buccal patches

A

-thinner and more flexible
-less obtrusive, pt like them more

28
Q

Nasal mucosal advantages

A

-avoid first pass
-rapid absorption
-easy

29
Q

nasal mucosal disadvantages

A

-possible tissue irritation
-rapid clearance from nose
-cold or allergies can mess this up
-limited surface area

30
Q

Nasal mucosal examples

A

-Zicam for cold
-Miacalcin for osteoporosis

31
Q

Nasal cavity regions

A

-respiratory
-olfactory

32
Q

nasal respiratory region

A

-main site for systemic drug delivery
-relatively large surface area
-epithelium w mucus that lubes and warms air and removed foreign particles

33
Q

nasal olfactory region

A

-small surface area
-provides direct connection between CNS and atmosphere
-small glands that produce solvent for odorous substances

34
Q

Nasal systemic mucosal delivery

A

-via respiratory region
-fast and extended drug absorption
-analgesics, CVD, hormones, anti-inflammatory and anti-viral

35
Q

Local nasal mucosal drug delivery

A

-treat topical nasal disorders
-antihistamines and corticosteroids for rhinosinusitits
-decongestants for colds

36
Q

Nasal vaccines

A

-lymph tissue under nasal epithelium rich w dendritic cells, t cells, b cells bc it first site of contact w antigens
-vax against respiratory infections

37
Q

potential route for nasal drug delivery to CNS

A

-via olfactory region

38
Q

Vaginal mucosal drug delivery

A

-permeation across epithelial membrane
-gel, creams, films, rings

39
Q

vaginal delivery advantages

A

-rich blood supply
-high permeability
-avoidance of hepatic first pass

40
Q

disadvantages of vaginal admin

A

-hormone-dependent changes
-pH

41
Q

vaginal gels and creams

A

-leaky, messy, need applicator
-estrogen, spermicide

42
Q

Intrauterine drug delivery

A

-IUD in uterine cavity
-progesterone and levonorgestrel
-local effects in uterine cavity
-5 years

43
Q

rectal drug delivery

A

-drugs normally admin by oral can be put here too ! :)
-local: IBD
-systemic: when u cant do oral
-less popular now
-kids and olds

44
Q

Rectal dosage forms

A

-suppositories (solid that melts/dissolves)
-rectal emenas (liquids)

45
Q

Ocular drug delivery

A

-local is greatly needed bc blood-retina barrier

46
Q

Requirements for ocular drug delivery

A

-need to be clear
-good corneal penetration
-prolonged contact time w corneal epithelium
-simplicity of use
-comfy

47
Q

Challenges in ocular delivery

A

-loss due to dilution in tears, spillage, drainage
-short residence time
-not much flexibility in terms of pH, osmolarity, solubility

48
Q

Ocular dosage forms

A

-eye drops
-ointments
-ocusert
-contacts
-implants

49
Q

How to improve eye drops

A

-viscosity enhancers to reduce drainage

50
Q

Port delivery system

A

-permanent refillable implant
-insicion in eye
-flange, sealing septum, body, porous release control element

Dosage II (20 decks)

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