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BUCCAL DRUG DELIVERY
SYSTEMS
Under the guidance of

Dr.B.Vasudha
M.pharm,Ph.D
Professor
Department of pharmaceutics

Presented by

P.Jeevan reddy
M.Pharm 1styear
Pharmaceutics
Roll no :12H61S0320
CONTENTS
• Introduction
• Buccal drug delivary
• Physiology of buccal environment
• Types
• Bio adhesion
• Mechanism
• Buccal drug delivery systems
• Evaluation
• Conclusion
• References
INTRODUCTION
Adhesion : is the bond produced by interaction between an adhesive and a
surface.
Bioadhesion : is the state of bond formation in which either adhesive or surface is
of biological origin.
 Mucoadhesion : is the interaction of the mucin layer with a polymer .
Buccal Drug Delivery
 The buccal mucosa lines the inner cheek, and buccal

formulations are placed in the mouth between the upper gingivae
(gums) and cheek to treat local and systemic conditions.
 The buccal route provides one of the potential route for typically
large, hydrophilic and unstable proteins, oligonucleotides and
polysaccharides, as well as conventional small drug molecules.
 The oral cavity has been used as a site for local and systemic
drug delivery.
Structure Of Oral Mucosa
Anatomy of oral mucosa
 Structure of oral mucosa

1) Epithelium
- stratum distendum
- stratum filamentosum
- stratum suprabasale
- stratum basale
2) Basal lamina
3) Connective tissue
- lamina propria
- submucosa
ADVANTAGES
LIMITATIONS
Drugs with large dose are difficult to be administered
 Eating and drinking may be restricted
 Possibility of the patient to swallow the tablet
 This route cannot administer drugs,which are unstable at buccal pH.
 This route cannot administer drugs,which irritate,bitter or unpleasant taste
 Small surface area is available for absorption
Buccal drug delivery and mucoadhesivity: :
The term ‘mucoadhesive’ is commonly used for materials that bind to the mucin
layer of a biological membrane.
Mucoadhesive polymers have been utilized in many different dosage forms in
efforts to achieve systemic delivery of drugs through the different mucosae.
These dosage forms include
Tablets, patches, tapes, films, semisolids and powders
Mechanisms of bioadhesion
 Wetting theory
 Diffusion theory
 Electronic theory
 Adsorption theory
 Fracture theory
FORMULATION OF BDDS

The basic components of buccal drug delivery system
Drug substance
Bioadhesive polymers
Backing membrane
Permeation enhancers
Bioadhesive polymers
IDEAL CHARACTERISTICS:
 Non toxic, non irritable, free from leachable impurities.
Polymer pH should be biocompatible.
Quick adherence, and suffice 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.
Backing membrane

Backing membrane plays a major role in the attachment of bioadhesive devices to the
mucus membrane.
The materials used as backing membrane should be inert, and impermeable to the
drug and penetration enhancer.
Such impermeable membrane on buccalbioadhesive 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
Permeation enhancers
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.
sodium lauryl sulfate,
sodiumlaurate
Bile salts:
Sodium glycodeoxycholate, sodium glycocholate, sodium taurodeoxycholate, sodium
taurocholate
Types of buccal
formulation
1) Buccal Tablets
2) Buccal Patches and Films
3) Buccal Semisolids (ointments and gels)
4) Buccal Powders
Evaluation of buccal
tablets
In vitro
 Swelling rate and bioadhesion studies

Surface pH studies
 Drug release studies
 Permeation studies
Mucoadhesion strength
 Residence time

In vivo
Drug release studies
Stability studies in human saliva

Ex vivo
Mucoadhesion time
Mucoadhesion force
 Transmucosal permeation studied.
Possible designs of buccal drug
delivery systems
Drugs given as buccal tablets
• Propranalol
• Metoprolol
• Metoclopromide
• Insulin
• Nitroglycerine
• Codeine
• Morphine
• Diltiazem
• Chlorpheniramine maleate
Types of Buccal Dosage
forms
Matrix type :
Drug, Adhesive, Additives are mixed together. Bidirectional patches. i.e.
release drug both in Mucosa, and Mouth.

Reservoir type :
Contains a cavity for drug, and additives separate from drug adhesive. Has an
impermeable backing. For regulating direction of drug flow. Also prevents
patch deformation, disintegration in mouth. Prevents drug loss.
Patch designs
Commercially available bioadhesive
buccal delivery systems
• Buccal mucosal delivery of Proclorperazine: Buccastem

• Buccal mucosal delivery of nicotine: Nicorette
Reported buccoadhesive drug delivery system
Drug

Dosage

Action

polymer

Benzydamine

Patch

Local

Pectin, PAA

Benzocaine

Bioadhesive gel

Local

HPMC

Carvedilol

Buccal patch

Systemic

HPMC

Clotrimazole

liposome gel

Local

Carbopol

Captopril

Tablet

Systemic

Carbopol, chitosan

Clotrimazole
Diltiazem HCL

Disk

local

Carbopol, HPMC
Conclusion
The buccal mucosa offers several advantages over controlled drug delivery for
extended periods of time.
First pass metabolism in the liver and presystemic elimination in the
gastrointestinal tract are avoided.
With the right dosage form design and formulation, the permeability and the
local environment of the mucosa can be controlled and manipulated in order to
accommodate drug permeation.
Buccal drug delivery is a promising area for continued research with the aim of
systemic delivery of orally inefficient drugs as well as a feasible and attractive
alternative for non-invasive delivery of potent peptide and protein drug
molecules. However, the need for safe and effective buccal permeation absorption
enhancers is a crucial component for a prospective future in the area of buccal
drug delivery
References
 Edith mathiowitz. Encyclopedia of controlled drug delivery.In: mucosal

drug delivery, buccal.A wiley-interscience publication.P.555-557
 Yie W.Chien.Novel drug delivery systems.In: buccal drug delivery.2 nd
ed.CBS publishers & distributors.New Delhi.P.210-215
 S.P Vyas,Roop K.Khar.controlled drug delivery,concepts and
advances.vallabh prakashan.P.291-299
 Anay R.patel,Dhagash v. patel,sharad v. choudry.Mucoadhesive drug
delivery system,International journal of pharmacy and life
sciences.2(6).2011.848-856
• Kumar V, Aggarwal G,Zakir F,Choudry A.Buccal bioadhesive

drug delivery-A novel technique.International journal of
pharmacy and biological sciences.1(3).2011.89-102

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Buccal bioadhesive drug delivery system G1ppt

  • 1. BUCCAL DRUG DELIVERY SYSTEMS Under the guidance of Dr.B.Vasudha M.pharm,Ph.D Professor Department of pharmaceutics Presented by P.Jeevan reddy M.Pharm 1styear Pharmaceutics Roll no :12H61S0320
  • 2. CONTENTS • Introduction • Buccal drug delivary • Physiology of buccal environment • Types • Bio adhesion • Mechanism • Buccal drug delivery systems • Evaluation • Conclusion • References
  • 3. INTRODUCTION Adhesion : is the bond produced by interaction between an adhesive and a surface. Bioadhesion : is the state of bond formation in which either adhesive or surface is of biological origin.  Mucoadhesion : is the interaction of the mucin layer with a polymer .
  • 4. Buccal Drug Delivery  The buccal mucosa lines the inner cheek, and buccal formulations are placed in the mouth between the upper gingivae (gums) and cheek to treat local and systemic conditions.  The buccal route provides one of the potential route for typically large, hydrophilic and unstable proteins, oligonucleotides and polysaccharides, as well as conventional small drug molecules.  The oral cavity has been used as a site for local and systemic drug delivery.
  • 6. Anatomy of oral mucosa  Structure of oral mucosa 1) Epithelium - stratum distendum - stratum filamentosum - stratum suprabasale - stratum basale 2) Basal lamina 3) Connective tissue - lamina propria - submucosa
  • 8. LIMITATIONS Drugs with large dose are difficult to be administered  Eating and drinking may be restricted  Possibility of the patient to swallow the tablet  This route cannot administer drugs,which are unstable at buccal pH.  This route cannot administer drugs,which irritate,bitter or unpleasant taste  Small surface area is available for absorption
  • 9. Buccal drug delivery and mucoadhesivity: : The term ‘mucoadhesive’ is commonly used for materials that bind to the mucin layer of a biological membrane. Mucoadhesive polymers have been utilized in many different dosage forms in efforts to achieve systemic delivery of drugs through the different mucosae. These dosage forms include Tablets, patches, tapes, films, semisolids and powders
  • 10. Mechanisms of bioadhesion  Wetting theory  Diffusion theory  Electronic theory  Adsorption theory  Fracture theory
  • 11.
  • 12. FORMULATION OF BDDS The basic components of buccal drug delivery system Drug substance Bioadhesive polymers Backing membrane Permeation enhancers
  • 13. Bioadhesive polymers IDEAL CHARACTERISTICS:  Non toxic, non irritable, free from leachable impurities. Polymer pH should be biocompatible. Quick adherence, and suffice 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.
  • 14. Backing membrane Backing membrane plays a major role in the attachment of bioadhesive devices to the mucus membrane. The materials used as backing membrane should be inert, and impermeable to the drug and penetration enhancer. Such impermeable membrane on buccalbioadhesive 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
  • 15. Permeation enhancers 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. sodium lauryl sulfate, sodiumlaurate Bile salts: Sodium glycodeoxycholate, sodium glycocholate, sodium taurodeoxycholate, sodium taurocholate
  • 16.
  • 17. Types of buccal formulation 1) Buccal Tablets 2) Buccal Patches and Films 3) Buccal Semisolids (ointments and gels) 4) Buccal Powders
  • 18. Evaluation of buccal tablets In vitro  Swelling rate and bioadhesion studies Surface pH studies  Drug release studies  Permeation studies Mucoadhesion strength  Residence time In vivo Drug release studies Stability studies in human saliva Ex vivo Mucoadhesion time Mucoadhesion force  Transmucosal permeation studied.
  • 19. Possible designs of buccal drug delivery systems
  • 20. Drugs given as buccal tablets • Propranalol • Metoprolol • Metoclopromide • Insulin • Nitroglycerine • Codeine • Morphine • Diltiazem • Chlorpheniramine maleate
  • 21. Types of Buccal Dosage forms Matrix type : Drug, Adhesive, Additives are mixed together. Bidirectional patches. i.e. release drug both in Mucosa, and Mouth. Reservoir type : Contains a cavity for drug, and additives separate from drug adhesive. Has an impermeable backing. For regulating direction of drug flow. Also prevents patch deformation, disintegration in mouth. Prevents drug loss.
  • 22.
  • 24. Commercially available bioadhesive buccal delivery systems • Buccal mucosal delivery of Proclorperazine: Buccastem • Buccal mucosal delivery of nicotine: Nicorette
  • 25. Reported buccoadhesive drug delivery system Drug Dosage Action polymer Benzydamine Patch Local Pectin, PAA Benzocaine Bioadhesive gel Local HPMC Carvedilol Buccal patch Systemic HPMC Clotrimazole liposome gel Local Carbopol Captopril Tablet Systemic Carbopol, chitosan Clotrimazole Diltiazem HCL Disk local Carbopol, HPMC
  • 26. Conclusion The buccal mucosa offers several advantages over controlled drug delivery for extended periods of time. First pass metabolism in the liver and presystemic elimination in the gastrointestinal tract are avoided. With the right dosage form design and formulation, the permeability and the local environment of the mucosa can be controlled and manipulated in order to accommodate drug permeation. Buccal drug delivery is a promising area for continued research with the aim of systemic delivery of orally inefficient drugs as well as a feasible and attractive alternative for non-invasive delivery of potent peptide and protein drug molecules. However, the need for safe and effective buccal permeation absorption enhancers is a crucial component for a prospective future in the area of buccal drug delivery
  • 27. References  Edith mathiowitz. Encyclopedia of controlled drug delivery.In: mucosal drug delivery, buccal.A wiley-interscience publication.P.555-557  Yie W.Chien.Novel drug delivery systems.In: buccal drug delivery.2 nd ed.CBS publishers & distributors.New Delhi.P.210-215  S.P Vyas,Roop K.Khar.controlled drug delivery,concepts and advances.vallabh prakashan.P.291-299  Anay R.patel,Dhagash v. patel,sharad v. choudry.Mucoadhesive drug delivery system,International journal of pharmacy and life sciences.2(6).2011.848-856
  • 28. • Kumar V, Aggarwal G,Zakir F,Choudry A.Buccal bioadhesive drug delivery-A novel technique.International journal of pharmacy and biological sciences.1(3).2011.89-102