This will provide you information about buccal drug delivery system, mucoadhesion, types of mucoadhesion, permeation enhancers, buccal formulation.

1. Buccal drug delivery system
PRESENTED BY
Vikas Dagar
M.PHARM 1yr

2. Buccal patch

4.  ADHESION
 BIOADHESION
 MUCOADHESION

5.  MUCOADHESION is defined as the
interaction between a mucin surface
and a synthetic or natural polymer .

8. GASTROINTESTINAL
BUCCAL
SUBLINGUAL
VAGINAL
RECTAL
NASAL
OCCULAR

12.  WATER 95%
 GLYCOPROTEINS 0.5-5 %
 LIPIDS 0.5-5%
 MINERAL SALTS 1%
 FREE PROTEINS 0.5-1%

13.  L-fucose
 D-galactose
 N-acetyl-D-
glucosamine
 N-acetyl-D-
galactosamine
 Sialic acid

14.  PROTECTIVE
 BARRIER
 ADHESION
 LUBRICATION

21.  PERMEATION ENHANCERS
 PRODRUG
 pH
 ENZYMES INHIBITORS
 VEHICLES / COSOLVENTS

22.  Increasing the fluidity
 Extracting inter and intracellular lipids
 Disrupting lipid structure e.g.,forming
micelles
 Altering cellular proteins
 Overcoming enzymatic barriers
 Altering surface mucin rheology

24.  •Bile salts
 •Fatty acids and their salts and Esters
 •Azones
 •Surfactants….Polysorbate80
 •ComplexingAgents…cyclodextrin
 •Co-solvents …..Glycol
 •Miscellaneous----Lecithin, Sodium Fusidate,
Chitosan,

26.  maintain it’s position in mouth.
 •release the drug in controlled manners.
 •Provide drug release in unidirection.
 Example..mucoadhesivebuccal tablet of
diltiazem HCL.
 Eg.Verapamilbuccal tablets, Sumatriptan
succinate buccal tablets.

31.  FOR local action the rapid elimination of
drugs due to the flushing action of saliva or
the ingestion of foods stuff may lead to the
requirement for frequent for frequent dosing
 The non- uniform distribution of drugs within
saliva on release from a solid or semisolid
delivery system could mean that some areas
of the oral cavity may not receive effective
levels

32.  For both local and systemic action, patient acceptability in
terms of taste, irritancy and ‘mouth feel’ is an issue.
 •For systemic delivery the relative impermeability of oral
cavity mucosa with regard to drug absorption, especially
for large hydrophilic biopharmaceuticals, is a major
concern.
 •The buccalmucosa also contains proteases that may
degrade peptide-based drugs.
 •In addition, the salivary enzymes may also reduce
stability

33.  ORAL MUCOSAL DRUG DELIVERY IS
CLASSIFIED AS -:
BUCCAL
SUBLINGUAL
LOCAL DELIVERY

35.  1) MATRIX TYPE.
 -CONVENTIONAL BUCCALTABLETS.
 -NOVEL BUCCALADHESIVE TABLETS.
 2) RESERVIOURTYPE.
 -BUCCALPATCHES
 3)BUCCALFILMS.
 4) BUCCALMUCOADHESIVEHYDROGEL.
 5) BUCCALSPRAY.
 6)FAST DISSOLVING BUCCALTABLETS.
 7) BUCCALWAFERS.
 8) BUCCALMICROSPHERE.

36.  •Contains cavity for drug and additives which
are separate from adhesive.
 •Impermeable backing
membrane>>>controls direction ,reduce
patch deformation, and disintegration.

38.  •Buccal adhesive patches are modified release dosage
form that have potential to provide controlled drug delivery
from 1 to 24 hrs.
 •They adhere to buccal mucosa for extended period of
time.
 •They consists of solid matrix ( which are non-dissolvable
or slowly dissolvable ).
 •They may be
 •Uni-directionally.
 •bi-directionally.
 •multi-directionally.

40.  •Size>>>>generally 1-16 cm2
 •But 1-3 cm2 used .
 •Large sized patches are placed at central
position of buccal mucosa.

41.  SOLVENT CASTING
 DIRECT MILING
 HOT MELT EXTRUSION

42.  •Thin film which are being placed on or
under the tongue or along the inside of the
cheek.
 •As the strip dissolves, the drug can enter
the blood stream , buccally or sublingually.
 •Buccal mucosa preferred over sub
lingual mucosa for such delivery forms.

43.  •It consists of film forming polymer .
 •Plasticizer.
 •API
 •Stabilizing and thickningagents.
BUCCAL FILM
MARKETED PRODUCT:
ONSOLIS (FANTANYL BUCCAL
SOLUBLE FILM) WHICH IS
USED IN MANAGEMENT OF
SEVERE PAIN OF CANCER.
BUCCAL FILM

44.  •These are hydrophilic matrices that are capable of swelling when
placed in aqueous media.
 •Hydrogels, which release the drug by swelling and thereby
allowing drug transport through the spaces in the polymer network,
are being widely studied for their use in bioadhesivegels.
 •Examples:
 1. Polyarylic-based hydrogels have also been extensively studied.
 2. An example of a commercially available device is the OTS (oral
transmucosalsystem, TheraTech), which has been used to deliver
glucagon-like insulin tropic peptide.
 3. Chitosan glutamate buccal hydrogel with local
anaestheticsactivity

46. •GENEREX BIO TECHNOLOGY have
introduced insulin spray .which is used
for type -1 diabetes patients.

47.  •Fast dissolving buccal tablets for administering a
medicament.includes active ingredients, a lubricant
and water soluble sugar like sorbitol such that buccal
tablets dissolves in about one minute
 It includes:
 -buccally absorbable active ingredients
-a lubricant (magnesium stearate, SDS)
 -soluble, directly compressible excipients(spray dried
sorbitol)
 ***Such rapid delivery is useful for delivering a bolus dose
to achieve a rapid rise in blood level.

48.  to•Bioadhesivemicrospheres offer unique carrier system
for many pharmaceuticals and can be tailored to
adhere to any mucosal tissue
 •The bioadhesivemicrospheres can be used not only for
controlled release but also for targeted delivery of the
drugs to specific sites in body.
 •Bioadhesivemicrospheres exhibit a prolonged
residence time at site of application or absorption and
facilitate an intimate contact with underlying absorption
surface and thus contribute improved and/or better
therapeutic performance of drugs
 •E.g. Bio adhesive polymer grafted starch microsphere
bearing isosorbide dinitritefor buccal delivery

50.  I)Organic nitrites. (glyceryltri nitrites )
 II)NASAIDS. (Diclofenacsodium )
 III)Local anaesthetics.
 IV)Bronchodilators (salbutamol)
 V)Antibiotics.
 VI)Anti-Diabetic (insulin)
 VII)Hormonal products (estradiols)

51.  •Thickness and weight uniformity.
 •Surface PH study.
 •Content uniformity.
 •Folding endurance….Folding endurance can be
 •done by folding the patches upto200 times without breaking
 •% Swelling studies.
 •Tensile strength.
 •In vitro residence time.
 •Mucoadhesivestrength.
 •In vitro release study and kinetics.
 •Analytical studies like: SEM,FTIR(Liquid), Zeta potential
 •Cytotoxicity tests(MTT assay)

52.  Water absorption capacity
 Permeation study of buccal patch
 Thumb test
 Viscosity
 Crosslinking density, Density
 Adhesion number

55.  •The most commonly used in vitro method to
study oral mucosal permeability is the use of
a permeability chamber like Franz type.

56.  •The most commonly used animal models
are dogs, rabbits, and pigs.
 •A general criterion for selecting an in vivo
animal model isthe >>>>> the resemblance of
the animal mucosa to the oral mucosa of
human beings in both ultrastructure and
enzyme activity, which represent physical
and metabolic barriers of the oral mucosa.
 •Porcine buccal mucosa and rabbit buccal
mucosa are mostly used.