Administration of a drug via buccal mucosa (lining of cheek) to the systemic circulation is defined as buccal delivery.

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Buccal and Sublingual Drug Delivery
System [BDDS & SDDS]
Mr. Sagar Kishor Savale
[Department of Pharmaceutics]
avengersagar16@gmail.com
2015-2016
Department of Pharmacy (Pharmaceutics) | Sagar Savale
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Contents
 Introduction
 Advantages
 Disadvantages
 Ideal Candidates for BDDS
 Anatomy of Buccal mucosa
 Formulation of buccal dosage form
 Evaluation of buccal dosage form
 References
 Conclusion
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Introduction
• Administration of a drug via buccal mucosa (lining of
cheek) to the systemic circulation is defined as buccal
delivery.
• The buccal mucosa lies in
inner cheek.
• Placed between upper
gingivae.
• To treat locally or
systemically
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Within the oral mucosal cavity, delivery of drugs is classified into three
categories:
a) Subligual delivery
b) Buccal delivery
c) Local delivery
a) Sublingual delivery :
It is the delivery of drugs or dosage form which is placed below or under the
tongue and allowed to dissolve.
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b) Buccal delivery:
• Delivery of drug or dosage form to the place between the cheek and the gum.
c) Local delivery:
• Which is drug delivery into the oral cavity .
• For the treatment of periodontal disease, ulcer, bacterial infection etc.
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Advantages of Buccal Drug Delivery
 Avoids first pass metabolism.
 Avoids acid/Enzyme metabolism.
 Permeation is faster with respect to skin & TDDS (4-
4000)
 Large surface area with respect to sub-lingual mucosa.
 Good patient compliance with respect to parenteral.
 Easy administration & removal (termination) in case of
toxicity.
 For unconscious or non compatible patients.
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 Drugs with bitter taste or irritant to mucosa or having
noxious smell are poor candidates.
 Not for children.
 Eating & drinking difficulty.
 Salivary erosion & it may enter GIT & choke esophagus.
 Less surface area than skin.
 Drugs unstable at Buccal pH (6.5 to 7)
Disadvantages
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• Mucoadhesion of the device is a key element.
• The term ‘mucoadhesive’ is commonly used for
materials that bind to the mucin layer of a biological
membrane.
• Achieve systemic delivery of drugs include tablets,
patches, tapes, films, semisolids (gels and
ointments) and powders. Some times spray and
lotions are also used.
BDDS and Mucoadhesivity
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Mechanism of Buccal Drug Delivery
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1. Molecular size 75-100 Daltons.
2. Dose of drug should be small enough to deliver across the
Buccal mucosa.
3. Drug should be hydrophilic/hydrophobic in nature.
4. Drug should be stable in Buccal pH (6.4-7.2)
5. Drug should be free from bitter taste and odorless.
6. Drug which are absorbed only by passive diffusion.
Ideal Candidates For Buccal Drug Delivery System
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Anatomy of Buccal Mucosa
Structure of oral mucosa
1) Epithelium
- stratum distendum
- stratum filamentosum
- stratum suprabasale
- stratum basale
2) Basal lamina
3) Connective tissue
- lamina propria
- submucosa
Fig- Anatomy of buccal mucosa
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ANATOMY & PHYSIOLOGY OF ORAL CAVITY
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Three different types of oral mucosa are recognized:
• Masticatory mucosa: (25% of the total oral mucosa)
1. Covers gingiva/ hard palate regions
2. keratinized epithelium
• Lining mucosa: (60% of the total oral mucosa )
1. cover soft palate, floor of mouth, under side of tongue,
labial & buccal mucosa.
2. non-keratinized epithelium.
• Specialized mucosa: (15% of the total oral mucosa)
1.The dorsal surface of the tongue
2. Highly keratinised.
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14. Overview of the Oral Mucosa
a) STRUCTURE:
fig: structure of oral mucosa .
 The turn over time for the buccal epithelium : 5 - 6 day
 The epithelium of buccal mucosa – about 40 to 50 cell layer
thick
 The oral mucosal thickness-buccal (500 to 800 μm)
sublingual (100 to 200 μm)
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b) ENVIORNMENT
The feature of the environment of the oral cavity is the presence of saliva &
mucus.
Role of mucus.
1 cell-cell adhesion.
2 Lubrication.
3 Adhesion of mucoadhesive drug delivery systems.
Role of saliva.
1 Protective fluid for all tissues of the oral cavity.
2 Continuous mineralization/demineralization of the tooth enamel.
3 To hydrate oral mucosal dosage forms.
c) PERMIABILITY
 4-4000 times greater than that of skin.
 Permeability of oral mucosa :
sublingual > Buccal > parenteral6/19/2016 Sagar Kishor Savale

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The basic components of buccal drug delivery
system-
 Drug substance
 Bio adhesive polymers
 Backing membrane
 Permeation enhancers
Formulation of BDDS – Patch/Film/Adhesive Tape
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 Ability to attachment of bio adhesive device to mucus
membrane
Backing membrane
 Inert in nature and impermeable to the drug
 Such impermeable membrane prevent dug loss and
good patient compliances
 Examples – Carbapol, Magnesium sterate, Polycarbapol
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IDEAL CHARACTERISTICS:
 Non toxic, non irritable, free from leachable impurities.
 Polymer pH should be biocompatible.
 Quick adherence, and sufficient mechanical strength.
 Bioadhesive in both dry and liquid state.
 Acceptable shelf life.
 Optimum molecular weight.
TYPES:
1 st generation polymers : PAA, NaCMC, HPMC,
Carbapol, Chitosan, Xanthan gum, PVA etc.
2 nd generation polymers : Lectins, Multifunctional
polymers, Thiolated polymers etc.
Bioadhesive polymer
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Sr. no Theory Mechanism of muco/Bioadhesion
1 Electronic
Attractive electrostatic force between glycoprotein mucin
network & the Bioadhesive material.
2 Adsorption
Surface force (Covalent bond, hydrogen bond, van der
Waals forces) resulting In chemical bonding.
3 Wetting Ability of bioadhesive polymer to spread & develop intimate
contact with the mucous membranes.
4 Diffusion Physical entanglement of mucin strands & the flexible
polymer chains.
5 Fracture
theory
Analyses the maximum tensile stress developed during
detachment of the BDDS from the mucosal surface.
Theories of Muco/Bio-adhesion
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FACTOR AFFECTIG MUCOADHESION
a. Polymer related factor :1. Molecular weight
2. Flexibility
3. H-bonding capacity
4. Cross linking density
5. Charge
6. Concentration
b. Drug related factor: 1. Molecular weight
2. Lipophilicity
c. Patient related factor: 1. Salivary secretion rate
2. pH of buccal cavity
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 Substances that help to promote drug permeation through the
buccal epithelium are referred to as penetration enhancers,
permeation promoters or absorption enhancers.
 Most of the compounds used as buccal mucosal penetration
enhancers are the ones generally used to compromise barrier
function.
Examples - sodium lauryl sulfate, sodiumlaurate
Bile salts: Sodium glycodeoxycholate, sodium glycocholate,
sodium taurodeoxycholate, sodium taurocholate
Permeation Enhancers
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22. Buccal penetration enhancer
• Chemical methods:
Transiently altering the lipid bilayer
membrane.
Increasing cell membrane fluidity.
Extracting structural lipids.
Altering cellular proteins.
Overcoming the enzymatic barrier.
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Physical Methods:
Mechanically by: Removal of the outermost layers of the
epithelium to decrease the barrier thickness.
Sonophoresis
Electrically by: Iontophoresis, Electro-poration.
 Classification & example of penetration enhancer:-
a. Bile salts and there steroidal detergents:-
Sodium glycocholate, sodium taurocholate, saponins, etc
b. Surfactants:-
1) Nonionic - Polysorbate 80,sucrose ester, etc.
2) Cationic - Cetyltrimethyl ammonium bromide.
3) Anionic - SLS,fatty acids.
3) c. Other enhancers:-
Azone, chelating agent , sulfoxide.
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• Propranalol
• Nitrites and nitrates
• Nefidipine
• Fenoterol
• Estradiol
• Oxytocin
• Metoprolol
• Metoclopromide
• Insulin
• Nitro glycerine
• Codeine
• Morphine
• Diltiazem
• Chlorpheniramine maleate
Drugs administered as buccal tablets
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Mechanism of Drug Absorption or Transport Routes
Mostly
drugs are
absorbed by
passive
diffusion
mechanism.
Nutrients
are
absorbed by
carrier
mediated
mechanism.
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26. BUCCAL ROUTE OF DRUG ABSORPTION
• There are two permeation pathways for passive drug transport across the
oral mucosa:
1.Transcellular route : Route for lipophilic compounds.
2. Paracellular route : Route for hydrophilic drug.
Fig : Transportation route of drug molecule 266/19/2016 Sagar Kishor Savale

27. BUCCAL DOSAGE FORM
1. Tablet
Tablets is small, flat, generally oval shape with 5-8mm diameter.
 Monolithic and two-layered matrix tablets have been designed for
buccal delivery of drugs.
Monolithic tablets is consist of a mixture of drug with a swelling
bioadhesive/sustained release polymer.
They can be coated on the outer or on all sides but one face with water
impermeable hydrophobic substances to allow an unidirectional drug
release for systemic delivery.
Two-layered tablets comprise an inner layer based on a bioadhesive
polymer and an outer non-bioadhesive layer containing the drug for a
bi-directional release but mainly for local action.
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Limitation of adhesion of tablet:
1. Small mucosal surface for contact.
2. Extent & frequency of contact might causes irritation.
2.Patches
• They are long ,flat, thin & transparant with high surface area.
• Patches are laminated and generally consist of an impermeable backing layer and a
drug-containing layer that has mucoadhesive properties and from which the drug is
released in a controlled manner.
They can be prepared by two method :
1. Solvent casting method
2. Direct milling method
Example: Melatonin (cydot)
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3. Chewing Gum :
Advantage:
Ability to retain in the oral cavity for long periods for prolong drug
delivery.
Gum base consist of Resin, fats, emulsifier, filler & antioxidant .
4. Gels & ointment:
They typically contain bioadhesive polymer (HEC, carbomer, etc)&
Drug plus any required excipients dissolved or suspended as fine
Powder in aqueous or non- aqueous base.
Example-Metronidazole (zidovel).
5. Buccal Spray : - The drugs may be administered by a buccal spray
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In vitro
 Swelling rate and bio adhesion studies
 Surface pH studies
 Drug release studies
 Permeation studies
 Mucoadhesion strength
 Residence time
Evaluation test
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Ex vivo studies
Animals are sacrificed.
Buccal mucosa with underlying connective tissue is surgically
removed, and then isolated.
Placed and stored in ice-cold (4°C) buffers. (usually Krebs
buffer) .
Generally dogs, monkeys and pigs are used.
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In vivo
Drug release studies
Stability studies in human saliva
Ex vivo
Mucoadhesion time
Mucoadhesion force
 Transmucosal permeation studied.
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In vivo method
First originated by Beckett & Triggs .
The methodology involves the swirling of a 25 ml sample of the test
solution for up to 15 minutes by human volunteers followed by the
expulsion of the solution.
The amount of drug remaining in the expelled volume is determined
in order to assess the amount of drug absorbed.
Drawback:
1 . Salivary dilution of the drug.
2. Accidental swallowing of a portion of the sample solution.
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34. Applications
1. Smoking cessation therapy.
2. Hormone replacement therapy .
3. Hypertention.
4. Angina pectoris.
5. Cancer.
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References
1.Shojaei Amir H., Buccal Mucosa As A Route For Systemic Drug Delivery: A
Review,
University of Alberta, Faculty of Pharmacy and Pharmaceutical Sciences, Edmonton,
Alberta, Canada, J Pharm Pharmaceut Sci 1 (1):15-30, 1998
2.Hans E. Junginger , Janet A. Hoogstraate, J. Coos Verhoef, Recent advances in
buccal drug delivery and absorption — in vitro and in vivo studies, Journal of
Controlled Release 62 (1999) 149–159
3.N.Chidambaram and A.K.Srivatsava, buccal drug delivery systems, Drug
development and industrial pharmacy, 21(9), 1009-1036 (1995)
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