1. Prepared by:
Motivaras Ashish
M.Pharm II sem
Roll No: 05
Guided by:
Dr. jaydeep Patel
B.K.MODY GOVT. PHARMACY COLLEGE,
RAJKOT.
BSDDS

2. o INTRODUCTION
o WHY BUCCAL/SUBLINGUAL?
o ANATOMY OF BUCCAL MUCOSA
o TRANSPORT ROUTES
o BIOADHESION MECHANISMS
o BASIC COMPONENTS FOR
BDDS
o FORMULATIONS
o EVALUATION
o RECENT INNOVATIONS
o REFERENCE2

3. The oral mucosa lines includes
inner cheek, sublingual, gingival,
palatal
Sublingual delivery: floor of
the mouth
Buccal delivery: lining of the
cheek
Local delivery:cavity, principally
ulcers, fungal conditions and
periodontal disease.
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4. 4

5. 5

6.  To avoid first-pass metabolism
 Protection from pH and digestive enzymes
 Improved patient compliance
 Rapid onset of action
 Ease of drug administration
 Rapid and extensive drug absorption
 Easy termination of therapy
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7. 7

8. 8

9.  Diffusion Theory Entanglements of the
polymer
 Electronic Theory Attractive forces
 Wetting Theory
 Fracture Theory the force necessary to
seaparate two surfaces
 Adsorption Theory Secondary chemical
bonds
9

10.  Drug substance
 Bioadhesive polymers
 Backing membrane
 Permeation enhancers
 Other excipient
10

11.  dose of the drug should be small
 half-life between 2-8 hours
 exhibit first pass effect or presystemic
drug elimination.
 absorption should be passive when
given orally
Nicotine
Nifedipine
Propranolol
Diclofenac sodium
Cyanocobalamin11

12.  must not decompose on storage
 inert and compatible with the
environment
 polymer and its degradation products
should be non-toxic absorbable from the
mucous layer.
 adhere quickly to moist tissue surface
1.Natural polymers
Ex.: Gelatin, sodium alginate.
2. Synthetic and semisynthetic polymers
Ex.: PVA, PEG, HPMC, PVP, Na-CMC
etc12

13.  plays a major role in the attachment
of bioadhesive devices to the mucus
membrane
 inert, and impermeable to the drug
and penetration enhancer.
Eg.carbopol, magnesium stearate, HPMC,
HPC, CMC, polycarbophil
13

14. Mechanism
 Changing mucus rheology
 Increasing the fluidity of lipid bilayer
membrane
 Acting on the components at tight
junctions
 Increasing the thermodynamic activity of
drugs
14

15. Types
1.Bile salts (Sodium glycocholate, sodium
taurocholate)
2.Fatty acids(oleic acid, capric acid, lauric
acid)
3.Surfactants
4.Chelators(EDTA, citric acid)
5.Others(aprotinin,
hyaluronidases,neuraminidase)
6.Thiolated polymers (chitosan-cysteine,
polycarbophil-cysteine)
15

16. 1)Polymer related factors:
 Molecular weight: bioadhesive strength of a
polymer increases with molecular weights
above 100,000
 Flexibility: substantial degree of flexibility in
order to achieve the desired entanglement
with the mucus
 Hydrogen bonding capacity
 Cross-linking density: increasing density of
cross-linking, diffusion of water into the
polymer net-work occurs at a lower rate
which, causes an insufficient swelling of the
polymer and a decreased rate of
interpenetration between polymer and mucin
16

17.  Charge: Some generalizations about the
charge of bioadhesive polymers have been
made previously, where nonionic polymers
appear to undergo a smaller degree o f
adhesion compared to anionic polymers
 Concentration
 Hydration (swelling): Polymer swelling
permits a mechanical entanglement by
exposing the bioadhesive sites for hydrogen
bonding and/or electrostatic interaction
between the polymer and the mucous network
2)Environmental factors
 Saliva
 pH
 Mucin turnover Rate
17

18.  Buccal and Sublingual Tablets
 Buccal and Sublingual Patches and Films
 Buccal Semisolids (ointments and gels)
 Buccal Powders
18

19.  Fast-disintegrating sublingual tablets:
(Sublingual) there is a need to formulate
a dosage form which gives fast relief from
angina & headache, while at the same
minimising the first pass effect to improve
its bioavailability. Fast disintegration
sublingual tablet fullfil this criteria.
 Bioadhesive Sublingual tablets:a risk that the
patient will swallow part of the dose before
the active substance has been released
 Sublingual vitamin tablet
 Lipid matrix sublingual tablet19

20.  S-DBMP-T(slow dissolving buccal
mucoadhesive plain tablet)
 BCTS(buccal covered tablet system)
Dosage forms are soften and lose its shape
due to mouth movement, which hindered
control of the disintegration of the tablet over
long administration periods .
The improved technology involved covering the
S-DBMP-T system with a polyethylene film
that had a hole in it. We refer to this
technology as the buccal covered-tablet
system (BCTS ) and have demonstrated that
this technology can prolong the duration of
absorption of glyceryl trinitrate and isosorbide
dinitrate.
20

21.  Buccal tablets are small, flat, and
oval, with a diameter of approximately
5–8 mm.
 Tablets are usually prepared by direct
compression, but wet granulation
techniques can also be used
21

22.  Swelling study
 Bioadhesion studies
 In vitro residence time
 In vitro surface pH studies
 In vitro drug release studies
 In vitro permeation studies
 In vitro mucoadhesion strength
 In vivo release studies
 Ex vivo mucoadhesion time
 Ex vivo mucoadhesion force
 Ex vivo transmucosal permeation studies22

23. Bioadhesion studies
Swelling study
Percentage hydration = [(W2-W1)/ W1] ×100
23

24. Residence time (in vitro)
Modified
Disintigration
Apparatus
Glass
slab
Buccal
tissue
Tablet
Isotonic buffer
24
Glass
Beaker

25. Release rate study(in vitro)
Composition of
simulated saliva
KH2PO4 12mM
NaCl 40mM
CaCl2 1.5mM
NaOH To pH 6.2
25

26. 26

27. 27

28.  Matrix type
 Reservoir type
28

29. 29

30. Thin film drug delivery is a process of
delivering drugs to the systemic
circulation via a thin film that dissolves
when in contact with liquid, often referred
to as a dissolving film or strip.
Thin film strips are typically designed for
oral administration, with the user placing
the strip on or under the tongue. As the
strip dissolves, the drug can enter the
blood stream enterically, or sublingually.
30

31.  Drug
 Polymers (Mucoadhesive
polymers, polymers controlling rate of
release and Polymers to prepare backing
membrane)
 Backing membrane
 Plasticizer
 Penetration enhancer
31

32. Methods for patch preparation
 Solvent casting method
 Semisolid casting
 Hot melt extrusion
 Solid dispersion extrusion
 Rolling method
32

33. EVALUATION OF BUCCAL PATCHES
Physical properties
 Physical appearance and surface texture
of patch
 Weight uniformity of patches
 Thickness of patches
 Folding endurance of patches
 Swelling index of patches
 Surface pH of patches
33

34. CONT…
Mechanical properties
 Bursting strength of patches
 In vitro residence time of patches
 Drug polymer interaction study of patches
 Drug content uniformity of patches
 In vitro drug release
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35. 35

36.  Gels are usually clear, transparent,
semisolids containing solubilized active
substances . e.g.Methylcellulose,
carbopols, hydroxyethylcellulose etc
 Glibenclamide gel
Buccal bioadhesive powder dosage forms are
a mixture of bioadhesive polymers and the
drug and are sprayed onto the buccal
mucosa. eg hydroxypropylcellulose and
beclomethasone- diproprionate
36

37.  BUCCAL WAFERS novel periodontal drug
delivery system that is intended for the
treatment of microbial infections associated
with peridontitis. The delivery system is a
composite wafer with surface layers
possessing adhesive properties, while the bulk
layer consists of antimicrobial agents,
biodegradable polymers and matrix polymers.
37

38.  GEL FORMING LIQUIDS: This type of a
formulation is liquid upon instillation and
undergoes a phase transition to form a
viscoelastic gel in response to stimulus such as
temperature, ionic stength or pH. Carbomers
become more viscous upon increased pH.
Gellan gum and alginate both form gel in
response to increased ionic strength
(particularly with Ca+2 ions). Poloxamers and
smart hydrogel are gel at approximately body
temperature.
 BIOADHESIVE SPRAY: Buccoadhesive
sprays are gaining popularity over other
dosage forms because of flexibility, comfort,
high surface area availability of drug in
solution form. Drugs genrally given by these
routes are fentanyl, buprenorphine. Naloxone
etc.
38

39.  flushing action of saliva
 Taste, Irritancy and ‘mouth feel’ is an
issue.
 Allergic reactions, discoloration of teeth
 Antimicrobial agents, affects the natural
microbes
 Patient cannot eat/drink/speak
 Swallowing of saliva lead to the loss of
drug
39

40.  Write about buccal & sublingual drug delivery
systems. (DEC. 2010)
 Explain the structure of buccal mucosa. Give
a brief account of mucoadhesive polymers for
buccal delivery. (JULY 2010)
 Discuss the merits and demerits of
mucoadhesive buccal drug delivery. How one
can evaluate mucoadhesive buccal
formulation? (JULY 2010)
 Which are potential sites and dosage forms
for bioadhesion? Draw a general schematic
diagram for BDDS and classify them.
 Write a note on exvivo and invivo methods to
study BDDS system. (January 2011)40

41.  Drug Delivery to the Oral Cavity,Drugs and
The Pharmaceutical Sciences, Executive Editor
James Swarbrick PharmaceuTech,
Inc.Pinehurst, North Carolina
 Enhancement in Drug DeliveryEdited by Elka
Touitou Brian W. Barry, Page no: 173-215
 Encyclopedia of PHARMACEUTICAL
TECHNOLOGY, Third Edition, VOLUME 1, Page
no:2664-2676
 Marcel Dekker, Inc. Modified-Release Drug
Delivery Technology, chapter no: 30
 Patel V. F., Liu F., et al. (2011). "Advances in
oral transmucosal drug delivery." Journal of
Controlled Release 153: 106-116.41

42.  Miller N., Chittchang M., et al. (2005). "The
use of mucoadhesive polymers in buccal drug
delivery." Advanced Drug Delivery Reviews
57: 1666– 1691.
 Sudhakar Y., Kuotsu K., et al. (2006). "Buccal
bioadhesive drug delivery — A promising
option for orally less efficient drugs " Journal
of Controlled Release 114: 15-40.
 Pankil A. Gandhi,Dr. M.R.Patel, Dr. K.R.
Patel, Dr. N. M. Patel , 2011, A REVIEW
ARTICLE ON MUCOADHESIVE BUCCAL DRUG
DELIVERY SYSTEM IJPRD, 2011; Vol
3(5): July 2011 (159 - 173)
42

43.  http://www.novadel.com/pipeline/index.htm
 http://www.medpharm.co.uk
 http://www.biodeliverysciences.com/pipeline.
php
 http://www.generex.com/technology.php
 http://www.snoreeze.com/the-snoreeze-
range/snoreeze-oral-strips
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