bioadhasives Flashcards
What is bioadhesion?
the attachment or association of a drug carrier system to a biological surface for extended periods of time
What is a drug carrier system?
any pharmaceutical dosage form containing a bioadhesive polymer or ligand
2 types of biological surfaces and their type of adhesion
- mucus layer lining the biological membrane - mucoadhesion
2. epithelial cells beneath the mucus - cytoadhesion
mucous membrane
epithelial cell layer covered by mucous layer
single cell layer or stratified multilayer
mucus
secreted by goblet cells or specialised glands
viscoelastic gel matrix or mucin glycoproteins
mucus thickness varies
- 50-450 microm in stomach
- <1 microm in mouth
mucous turnover
around 4-5hrs
affects resistance time of mucoadhesive formulation
nature of mucoadhesive bonds
- non-specific interactions between mucous and mucoadhesive polymer
- physical or mechanical interactions
- chemical bonds
- > ionic (mucous is -ve charged), H bonds, van der waals interactions
types of mucoadhesive polymers
- hydrogels
2. hydrophobic polymers
What are hydrogels?
hydrophilic polymer with swelling capacity
examples of hydrogels
carbopols
chitosan (+ve charge, can ionic bond)
sodium alginate
cellulose derivatives
type of delivery for hydrogels
buccal
nasal
most popular mucoadhesive polymer
hydrogels
What are hydrophobic polymers?
non-swellable
- only van der waals interactions
example of hydrophobic polymer
polylactic acid (PLA)
type of delivery for hydrophobic polymers
oral delivery
properties of mucoadhesive hydrogels
hydrophilic functional group
high Mr
cross linked network
hydrophilic functional group of hydrogels
form H bonds or ionic bonds with the mucus layer
water uptake results in polymer swelling and chain disentanglement
3 types of hydrophilic functional groups of hydrogels
- anionic polymers - H bonding interaction with mucin, eg carbomer
- cationic polymers - ionic and H bonding interaction with mucin, eg chitosan
- non-ionic - H bonding interaction with mucin
high Mr of hydrogels
- polymer chain length -> entanglement with mucin chains
- optimin Mw = 10,000-4.000.000 Da
- too high Mr - slow hydration and inadequate bond formation
- too low Mr - excessive hydration, gel formation and complete dissolution in ucus, loss of adhesive ability
cross linked networks
degree of cross linking affects swelling capacity and chain mobility
high degre of cross linking may prevent over hydration but may restrict chain mobility
-> need partial cross linking, retains liquid behaviour so it can continue to interact
drug release process from mucoadhesive hydrogels
- hydration of polymer and swelling of network
- chain relaxation and difusion of dissolved drug
What is cytoadhesion?
adhesion to cells
cell specific bioadhesion
- a recognition ligand is attached to the drug carrier
- useful for oral delivery
cell specific ligands
- lectins
- bacterial adhesins