BUCCAL DRUG DELIVERY SYSTEM
M.P. Venkatesh
Asst. Professor
Dept. of Pharmaceutics
JSSCP, Mysore
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DEFINITION OF MUCO/BIOADHESION
Bioadhesion may be defined as the state in which
two materials, at least one of which is biological in
nature, are held together for extended periods of
time by interfacial forces.
In the pharmaceutical sciences, when the adhesive
attachment is to mucus or a mucous membrane, the
phenomenon is referred to as mucoadhesion.
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BUCCAL DRUG DELIVERY SYSTEMS
Buccal route of drug delivery is a good alternative,
amongst the various routes of drug delivery. Oral route
is perhaps the most preferred for the patients.
Within the oral mucosal cavity, the buccal region
offers an attractive route of administration for systemic
drug delivery.
Considering the low patient compliance of rectal
vaginal, sublingual and nasal drug delivery for
controlled release ,the buccal mucosa has rich blood
supply and it is relatively permeable.
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Drug delivery via the membranes of oral cavity can be sub
divided as follows:
1) SUBLINGUAL DELIVERY:
It is the administration of the drug via the sublingual
mucosa (the membrane of the ventral surface of the tongue
and the floor of the mouth) to the systemic circulation.
2)BUCCAL DELIVERY:
It is the administration of drug via the buccal mucosa (the
lining of the cheek) to the systemic circulation.
3)LOCAL DELIVERY:
For the treatment of conditions of the oral cavity, principally
aphthous ulcers, fungal conditions, and periodontal
disease. 4
STRUCTURE OF ORAL MUCOSA
The unique environment of oral cavity offers its
potential as site for drug delivery, because of the rich
blood supply & direct access to systemic circulation .
The oral route is suitable for drugs, which are
susceptible to acid hydrolysis in the stomach or
extensively metabolized in liver i.e. first pass
metabolism.
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The continuous secretion of saliva results in rapid
release of drugs.
The buccal & gingival regions are associated with a
smaller flow of saliva, as compared to the sublingual
region, thus the duration of adhesion of delivery
system would be longer at these area than at
sublingual region.
Thus buccal & gingival membranes offer a platform for
localizing drug delivery system for prolong systemic
delivery of drugs.
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The oral mucous is consisted of an outer most layer of
stratified squamous epithelium, which is covered with
mucous.
Stratified squamous epithelium consist of –
1. stratum distendum
2. stratum filamentosum
3. stratum suprabasale
4. stratum basale
The area below the basal lamina, covered with lamina
propria & submucosa.
The epithelium serves as the mechanical barrier that
protect underlined tissues.
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Where as the lamina propria provides a mechanical support
& also carries the blood vessel & nerves.
Some regions of oral mucosa are keratinized.
The non- keratinized regions, such as buccal mucosa is
more permeable than keratinized region, this due to the
composition of intercellular lipids comprising the
particular region.
Where as keratinized regions contain predominantly
neutral lipids (ceramides) & non-keratinized regions are
composed of a glycosyl ceramide.
The mucous membranes have a total area of 100 cm2
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THE MUCOUS LAYER
Mucous is translucent & viscid secretion which forms a
thin, continuous gel blanket adherent to the mucosal
epithelial surface.
The mean thickness of this layer varies from 50 to 450 µm
in humans.
It is secreted by the goblet cells, lining of epithelia.
Beside the mucous, the mucosal layer of oral cavity is kept
moist by the saliva secreted by the submaxillary, the parotid
& the sublingual glands.
The pH of the saliva ranges from about 6.2 to 7.4 with an
average of 6.6.
About 1.5 liters of saliva secreted per day. 10
FUNCTIONS OF MUCOUS LAYER
Protection of mouth
Acts as barrier
Helps in adhesion
Lubrication of mouth
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ADVANTAGES OF BUCCAL DELIVERY
Bypasses the hepatic first pass metabolism and
degradation in the stomach and intestine, thereby
greater bioavailability.
Excellent accessibility:
- Precise dosage by which localization is possible.
- Allows localized modification of tissue permeability
- Facilitates removal in emergencies (termination)
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ADVANTAGES OF BUCCAL DELIVERY
Delivery device can be made unidirectional; only oral
mucosa absorption.
Buccal mucosa is less prone to damage or irritation
than nasal mucosa.
Extent of perfusion is more ,therefore quick and
effective absorption.
Nausea and vomiting are greatly avoided.
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ADVANTAGES OF BUCCAL DELIVERY
Used in case of unconscious and less co-operative
patients.
It offers a passive systems which does not require
activation and the therapeutic serum concentration
can be achieved rapidly.
Since the formulation is light;
- Less packing cost.
- Less transport cost.
-Economy of raw material.
-Cheap 14
ADVANTAGES OF BUCCAL DELIVERY
Drugs, which show poor bioavailability via the oral
route, can be administered conveniently.
The presence of saliva ensures relatively large amount
of water for drug dissolution unlike in case of rectal
and transdermal routes.
Drugs, which show poor bioavailability via the oral
route, can be administered conveniently.
Better patient compliance than vaginal, rectal or nasal
routes.
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DISADVANTAGES
Relatively smaller area of absorption.
The thickness of delivery system should be limited to a
few millimeters in order to avoid inconveniences for
patient.
Part of the drug may be dissolved in the saliva and may
be swallowed.
Drugs which irritate oral mucosa or have bitter taste,
or cause allergic reactions, discoloration of teeth
cannot be formulated.
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DISADVANTAGES
If formulation contains antimicrobial agents, affects
the natural microbes in the buccal cavity.
The patient cannot eat/ drink/ speak.
Only those drugs which are absorbed by passive
diffusion can be administered by this route.
Drugs which are unstable at buccal pH cannot be
administered by this route.
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DIFFERENT FORMULATIONS OF BDDS
1. Bio adhesive buccal tablets
2. Hydrogel and Laminated Systems
3. Chewing Gums
4. Buccal Patches
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BIO ADHESIVE BUCCAL TABLETS
They are immobilized DDS.
They can be formulated into monolithic, partially
coated or multi-layered matrices.
In case of Bi-layered tablets, drug can be incorporated
in the adhesive layer, which comes in contact with the
mucosal surface.
This drug containing mucoadhesive layer is then
protected from the oral cavity environment by a
second upper inert layer, which faces into the oral
cavity.
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Alternately, the drug can be incorporated into the
upper non-adhesive layer to release the drug into oral
cavity.
LIMITATIONS:
1. The small surface of contact with mucosa.
2. Lack of physical flexibility.
3. It is difficult to obtain high release rates, which is
required for some drugs.
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HYDROGEL AND LAMINATED SYSTEMS
To alleviate and circumvent the drawback of tablets,
different flexible, adhesive films and hydrogels
formulations were developed.
Different polymers can be used like cellulose
derivates (MC, Sod.CMC, HEC), natural gums (guar
gum, karaya gum and agarose), polyacrylates like
polyacrylic acid, polyethylene, glycol and gelatin.
These polymers exhibit mucoadhesive properties in
the presence of water.
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CHEWING GUMS
Chewing gums are mobile DDS.
The main target mucosa for drug absorption is
sublingual mucosa.
However, drug is released into saliva and subsequent
spreading may cause the drug to be absorbed across
other mucosa of the oral cavity.
They consists generally of a gum base of cellulosic or
acrylic polymer.
The polymer is blended with sugar as well as drug.
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BUCCAL PATCHES
Can be designed either for unidirectional or for multi-
directional release into the oral cavity as well as into
the oral mucosa.
The adhesive part of the system can be used as drug
carrier or as an adhesive for retention of a drug loaded
non-adhesive layer.
The use of an impermeable backing layer will
maximize the drug conc. gradient and prolong
adhesion because the system is protected from saliva.
Buccal mucoadhesive patches are two-ply laminates or
multilayered thin film, round or oval.
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REFERENCES
1. Controlled drug delivery. S.P. Vyas. Page no: 292-299
2. Controlled and Novel Drug Delivery. N.K. Jain. Page
no: 353-373.
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