Mucoadhesion

Definition
Bioadhesion is defined as an ability of material to
adhere to biological tissue for an extended period of
time.
In the case of polymer attached to the mucin layer,
the term mucoadhesion is used.
Mucoadhesive dosage forms may be designed to
prolong retention at the site of application, providing a
controlled rate of drug release for improved therapeutic
outcome.

Ideal characteristics of
mucoadhesive approach
Rapid adherence to the mucosal layer without any
change in the physical property of the delivery matrix
Minimum interference to the release of the active agent
Biodegradable without producing any toxic byproducts
Enhance the penetration of the active agent

Advantages of mucoadhesion
Increased residence time leading to enhanced
adsorption
Improved intimacy of contact with various biological
membranes
Improved bioavailability through the protection of
bioactive molecules from physical and chemical
degradation
Targeting and localization of a release device at a
specific site

Disadvantages of mucoadhesion
Medication that administered orally do not enter the
blood stream immediately after passage through buccal
mucosa
Certain drugs undergo drug destruction when
administered orally and affect liver metabolism
Oral ingestion results in more exposure of a drug to the
GIT and destruct normal microflora resulting in diarrhea
and overgrowing dangerous organisms
The absorption is adversely affected by the presence of
food

Factors influencing the strength of

the mucoadhesion
Molecular weight and
crosslinking of the
polymer
The spatial
configuration of the
polymer
Concentration

The adhesive strength increases by increasing the Mr and decreasing

crosslinking density so polymer does not lose its flexibility and
elasticity.
In the case of a linear polymer, bioadhesion is improved by increasing
the Mr. In the case of a nonlinear polymer, it needs a significant
increase of Mr.
Need optimum concentration, not necessarily the highest.

Chain flexibility

Increased to enable interpenetration of polymer chains through the

mucus layer.

Hydration capability

If the degree of hydration is high, the adhesive properties of a

polymer are lost due to the formation of slippery, non-adhesive
mucilage near the interface.
Polymers containing hydroxyl, carboxyl, and some amines and
sulfates are potentially good bioadhesives.

Functional groups

Main stages in mucoadhesion

Contact stage
The mucoadhesive polymers
must spread over the mucus
layer to initiate close
contact and to increase the
surface area of contact.
Consolidation stage
The adhesive joints must be
strengthened and
consolidated, leading to a
prolonged adhesion.

Source: www.scielo.br