Buccal drug delivery system by yogita thakare (7).pdf
BUCCAL DRUG DELIVERY SYSTEM
Presented by :
Yogita A. Thakare
M pharm 1st yr.
Dept. of Pharmaceutics
Kncp, Butibori , Nagpur.
Facilitated by :
Dr. J.G. Awari
Dept. of Pharmaceutics
Kncp, Butibori, Nagpur.
• It is the administration of drug via the buccal mucosa. (the lining of the cheek)
to the systemic circulation.
• Buccal cavity mucosa was the most convenient and also easily approachable
site for purpose of delivering the therapeutic agent for both local as well as
• The buccal mucosa lines the inner cheek and buccal formulation are placed in
mouth between the upper gums and cheek to treat local and systemic
Eg:- medication that are available in buccal form include Fentora, belbuca
1. Inner layers called mucosa.
2. Inner epithelial cell living is covered with viscoelastic fluid .
3. Secreted by goblet cells.
4. Composed of water and mucin (An anionic polyelectrolyte).
5. Other components includes Protein, lipids mucopolysaccharides , electrolytes.
6. Main role is protective and lubricates.
PRINCIPLE OF MUCOADHESION :-
1. Avoids 1st pass metabolism
2. Avoids acid/Enzymemetabolism.
3. Large surface area with respect to sub-lingual mucosa
4. Good patient compliancewith respect to parental
5. Easy administration & removal in case of toxicity
6. For unconsciousor comatose patients
1. Drugs with bitter taste or irritant to mucosa or having noxious smell.
2. Not for children.
3. Eating & drinking difficulty .
4. Salivary erosion & it may enter GIT & choke esophagus.
5. Less surface area than skin .
6. Drugs unstableat Buccal pH(6.5 to 7) .
MECHANISM OF DRUG PERMEATION
1. Passive diffusion
A) Transcellular or intracellular route.
B) Paracellular or intercellular route.
2. Carrier mediated transport
A) Active diffusion
B) Facilitated diffusion
3. Endocytosis:- A) Phagocytosis. B) Pinocytosis.
C)Receptor mediated endocytosis
• It is transfer of drug molecules across concentration gradient from a higher
concentration(buccal drug dosage form) to a lower concentration(mucous
* Route of lipophilic drugs.
*Lipid drugs passes through lipid rich mucous membrane.
• Para cellular:
* Primary route for hydrophilic drugs
*Hydrophilic drugs passes through intercellular spaces.
Passive diffusion :-
Carrier mediated transport :-
• Movement which occurs across membranes, such as the blood- brain barrier and
the mucosal membrane with the help of "carrier".
• This mechanism is a rapidly reversible reaction between the drug being
transported and the components of the membrane.
• Active transport:
• Transport of drug molecules across the mucous membrane from region of lower
concentration to a region of higher concentration by using trans membrane proteins
using ATP .
• Facilitated diffusion: - Transport of drug molecules across mucous membrane from
region of higher concentration to a region of lower concentration by means of
trans membrane proteins.
• Endocytosis is the process of actively transporting drug molecules into the
cell by engulfing it with its membrane.
• Phagocytosis : - Intake of solid drug molecules into the cell by forming
• Pinocytosis:- Intake of liquid drug molecules into the cell by forming
• Receptor mediated endocytosis:
• Intake of drug molecules into the cell with the help of receptors present on
the membrane and forming vesicles.
Formulation of BDDS :-
• Solid Dosage forms :-
• Patches/films,Wafers, Solid Dosage forms
• Lozenges , Powders
• Semi-Solid Dasage forms:-
• Liquid dosage forms :-
METHODS OF FORMULATION
Mucoadhesive Polymers :-
• These are the main component for adhesion.
• They attract water from the biological surrounding, get swells & adheer to the
• Normally they should be having hydrophilicity, numerous H-bonding groups,
flexibility, interpenetration with mucus & tissues .
1. Hydrogels:- eg. Polyacrylates, Carbopol, Polycarbophils.
2. Thiolated Polymers :- eg. Thiomers of chitosan and polyacrylic acid.
• Permeation is very limiting factor in BDDS.
• Substances that facilates permeation through Buccal mucosa are called PE.
• Epithelium & Lamina Propria are very effective barrier to absorption.
1. Chelaters :- eg. Citric acid , Sodium salicylate. Surfactant, Methoxy salicylate.
2. Surfactant :- eg. Polyoxiethylene ,Benzalconium,
Mechanisms of PE’s :-
• Increasing fluidity & integrity of cell membrane.
• Extracting inter/intra cellular lipids.
• Altering cellular proteins.
• Altering mucus rheology.
• Acting at the tight junctions.
• Increasing thermodynamic activity of drugs.
• Surface tension decreasing.
Buccal patches film:-
• They are long , flat, thickness, transperant with high surface area
• They can be prepared by two methods
• Solvent casting method
• Direct milling method
Solvent Casting Method :-
• Here drug & all excipients are weighed and dispersed in the suitable
organic solvent & coated on the release liner
• The organic solvent is allowed to evaporate & after evaporation the thin
layer of the backing material is laminated on to the sheet of coated
release liner to form laminate.
• After that the whole patch is ready to cut into required size.
Direct Milling Method:-
• Here, drug & excipients are mixed mechanicallyby milling or kneading.
• After mixing the resultant material is rolled on the release liner till desired
thickness is achieved.
• Finally as the previous method, backing material is laminated .
• Though there is no difference in the patch performance manufactured by
either of the method but with the SOLVENT method there are chance of
• Hence this Solvent free method is highly used .
Evaluation of buccal drug delivery system :-
1)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.
2)Thickness measurements: The thickness of each film is measured at five
different locations (centre and four corners) using an electronic digital micrometer.
3)Folding endurance: The folding endurance of patches is determined by
repeatedly folding 1 patch at the times
4)Thermal analysis study: Thermal analysis study is performed using
differential scanning calorimeter (DSC).
5)Morphological characterization: Morphological characters are studied by
using scanning electron microscope (SEM).
6) Permeation study of buccal patch: The receptor compartment is filled with
phosphate buffer pH 6.8, and the hydrodynamics in the receptor compartment
is maintained by stirring with a magnetic bead at 50 rpm. Samples are
withdrawn at predetermined time intervals and analyzed for
drug content .