BUCCAL DRUG DELIVERY

SYSTEM
GENERAL OVERVIEW
BASIC INTRODUCTION
Buccal drug delivery : the delivery large

of drug into systemic circulation via

buccal mucosa i.e. through the
inner lining cheeks is called buccal Other small
drug delivery. drugs
hydrophillic
Potential

Such dosage forms are placed route for

drugs that
between cheeks and upper gums. are:

Intended purpose of use is

generally treatment of local or
systemic conditions Proteins, oligo-
nucleotides,
unstable
Poly-
saccharides
 WHY AND WHEN TO FORMULATE AS
BDDS ?
1. Some drugs have very short half life and therefore need to be
administered multiple times in a day. This reduces patient compliance.
2. Some drugs may undergo enzymatic degradation in GIT
3. Some drugs suffer great loss in bioavailability as they undergo first pass
metabolism

Due to above mentioned reasons BDDS is employed

 ADVANTAGES
1. Easy to administer
2. Therapy can be stopped whenever required
3. For unconscious and trauma patients it is easy to administer
4. Bypass first pass metabolism
5. Drugs unstable in environment of GIT can be given through BDDS
6. Flexibility in physical state, shape, size and surface
7. Rapid onset of action
 DISADVANTAGES
1. Cannot administer drugs that are unstable at buccal pH
2. Not suitable for drugs with bitter taste, obnoxious odor, or irritant to
mucosa
3. Only small dose can be administered
4. Eating and drinking may become restricted
5. Only those drugs that are absorbed via passive diffusion can be given
through BDDS
ANATOMY OF BUCCAL
CAVITY
ANATOMY OF BUCCAL
CAVITY
From top to down, following are the tissues
that line the buccal cavity:
1.Mucus membrane
2.Epithelium (stratified/non-stratified)
3.Lamina propria
4.Submucosa
 WHY DOES THE PRESENCE OF
KERATIN MATTER?
Keratinised parts:
Mucosae of gingivae and hard
palate

Non-keratinized parts:

Mucosae of soft palate,

sublingual regions and buccal
regions

Keratinization decreases water

permeability
 WHAT IS THE ROLE PLAYED BY
SALIVA ?

 Absorption of drugs through moist mucosa takes place more readily.

 Most drugs administered through BDDS are solids. They must be first
dissolved before they can be absorbed. This is brought out by saliva
 VASCULATURE

Absorbed
Internal Superior
drug through Heart Entire body
jugular vein vena cava
mucosa

Liver is by-passed
DOSAGE FORMS
Type 1 :
Drug loaded single bioadhesive
layer device. Multidirectional drug
release. Loss due to swallowing
is more

Type 2 :
Double layered device.
Impermeable backing layer on
top. Prevents drug loss from top
surface.

Type 3 :
Every face covered with
impermeable membrane but © PANKHIL GANDHI
Matrix type
A buccal patch in the form of a
matrix of adhesive, drug and
other additives
Reservoir type
Buccal patch contains a separate
cavity that contains drug and
additives from the adhesive
membrane.
An impermeable backing is added
on one side and adhesive
membrane on another
1. Solids – lozenges and tablets. Dissolve in saliva and absorbed from
throughout the oral mucosa
2. Gum – chewing gums. Offers controlled drug delivery over an extended
time. These are very convinient
3. Gel forming liquids and in situ gels
4. Powders – mixture of bioadhesive polymers and drugs sprayed onto
buccal mucosa
5. Patches – attached to buccal region
i. With dissolvable matrix
ii. With non-dissolvable backing
iii. With dissolvable backing
DOSAGE DESIGN AND PART 1 – GENERAL
CONSIDERATIONS
FORMULATION IN FORMULATION
PHYSIOLOGICAL CONSIDERATIONS
1. Surface area
2. Device size
3. Drug load
4. Duration
5. Interaction of ingredients with salivary enzymes
 PHARMACOLOGICAL
CONSIDERATIONS
1. Lipophilic drugs – absorbed via transcellular route
2. Hydrophilic drugs – absorbed via paracellular routes
 PHARMACEUTICAL
CONSIDERATIONS
1. Drug release rate
2. Organoleptic factors
3. Effects of excipients like irritation at site of application
4. Incorporation of penetration enhancers, mucoadhesives, enzyme
inhibitors
DOSAGE DESIGN AND BASIC

FORMULATION COMPONENTS
BASIC COMPONENTS OF BDDS :

1. Drug substance
2. Bioadhesive polymers
3. Backing membrane
4. Permeation enhancer
 Prolonged

DRUG SUBSTANCE
release

Systemic effect

release
Rapid
The drug should have the following
characteristics :
acti on

1. Small single dose Local

2. Fluctuations in blood levels when

given orally
3. Exhibits first pass metabolism
4. Shows passive absorption
5. Have half life between 2-8 hours
 BIOADHESIVE POLYMER

1. These serve the purpose of

adhering the dosage form to the
buccal region
2. Also employed to form matrix in
which drug is incorporated
3. May be synthetic or natural
4. May be water soluble or insoluble
 PERMEATION ENHANCERS
These are the substances that facilitate or enhance the permeation of the
drug through the buccal mucosa

MOA :
1.Reducing the viscosity of mucus
2.Increase fluidity of bilipid membrane
3.Inhibiting various peptidases and proteases in the mucus
membrane to overcome enzymatic barrier
4.Increase solubility of drug
 BACKING MEMBRANES
The materials used as backing membrane should be inert, and
impermeable to the drug and penetration enhancer. Such impermeable
membrane on buccal bioadhesive patches prevents the drug loss and
offers better patient compliance.

The commonly used materials in backing membrane include carbopol,

magnesium stearate, HPMC, HPC, CMC, polycarbophil etc
 OTHER ADDITIVES
1. Diluents
2. Sweetening agents
3. Flavouring agents
MANUFACTURING
METHODS
 METHODS FOR FILMS/PATCHES

1. Solvent casting
2. Direct milling
3. Hot melt extrusion of films
EVALUATION
 MOISTURE ABSORPTION
It gives an indication about the relative moisture absorption capacities of
polymers and an idea whether the buccal patches maintain their integrity
after absorption of moisture.
Patches are placed on agar plates for 2 hr at 37oC. Moisture absorbed is
calculated using the formula:

Initial Weight – Final Weight

% Moisture content =
Initial Weight
 SWELLING AND EROSION

Initial Weight – Final Weight

x 100 SI =
Initial Weight
SURFACE PH
Buccal patches are left to swell for 2 hrs on the surface of an agar plate.
The surface pH is measured by means of a pH paper placed on the
surface of the swollen patch.
 DETERMINATION OF THE
RESIDENCE TIME
Ex vivo residence time
Ex vivo residence time is determined using a modified USP disintegration
apparatus. It is composed of 800 ml phosphate buffer of pH 6.6 maintained at
37°C. The porcine buccal tissue is tied to the surface of a glass slab, vertically
attached to the apparatus. The time which was taken for complete
erosion or detachment of the tablet from the mucosal surface was recorded and
considered as ex vivo residence time.

In vivo residence time

The experiment is performed on volunteers. The volunteers are asked to
record the residence time of the film on buccal mucosa in the oral cavity,
which is taken as the time for the patch to dislodge completely from the buccal
mucosa by continual sensation of the patch as well as the backing membrane.