buccoadhesive drug delivery system or buccal adhesive drug delivery system
TRANSCRIPT
BUCCOADHESIVE DRUG DELIVERY SYSTEM
1st Year M. Pharm.( Sem.I)
Prepared by Under the guidance ofMiss. Shubhada Avinash Gayake Prof.Chemate S.Z.Roll No. 06 Department of PharmaceuticsSpecialization: Pharmaceutics P. D.V. V. P. FOUNDATION’s COLLEGE OF
PHARMACYVILAD GHAT, AHMEDNAGAR
CONTENTS• Introduction• Advantages• Disadvantages• Buccal Mucosa• Permeability of Drug• Mechanism of Bioadhesion• Buccoadhesive Theories• Factors Affecting Buccoadhesion• Buccoadhesive Polymers• Buccoadhesive Dasage Form• References
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INTRODUCTION DEFINATION:
Buccoadhesive drug delivery system involves delivery of drug through the mucosal lining of oral cavity.
Buccoadhesion defined the term “bioadhesion” as the any bond formed between 2 biological surfaces or a bond between biological & synthetic surface.
• Use of bioadhesive polymers to control the delivery of biologically active agents systematically or locally.
• System is attractive because it avoids significant limitations of traditional route.
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ADVANTAGES1. Rapid absorption because of enormous blood supply and good
blood flow rates.2. Increases the bioavailability.3. Rapid onset of action.4. Drug is protected from degradation in the acidic environment in
the GIT.5. Improved patient compliance.6. Sustained drug delivery.7. The formulation can be removed if therapy is required to be
discontinued.8. Avoid first pass metabolism.9. Permeability of oral mucosa is 4-4000 times greater than skin.
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DISADVANTAGES
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1. Requirement of frequent dosing.2. Occurrence of local ulcerous effects.3. Taste of drug. 4. Drugs may get swallowed with saliva.5. Less permeable than small intestine.
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The buccal mucosa composed of Stratified Squamous Epithelium
Basement Membrane Lamina Propria
Innermost Submucosa
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MUCUS & ITS ROLEROLE• To provide a barrier.• Bioadhesion of buccoadhesive drug delivery systems • Lubrication.CONTENT• Mucus Water (95-99.5%) • Mucins (0.5-5%)• Other substances like enzyme, Salts.• High molecular weight proteins.
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Permeability Of Drugs Through Bucal Mucosa
i.Transcellular (intracellular, passing through the cell) ii.Paracellular (intercellular, passing around the cell).
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MECHANISM OF BIOADHESION
• Buccoadhesion is the attachment of the drug along with a suitable carrier to the mucous membrane.
• For a buccoadhesive to be successful, the attraction forces must dominate.
• secondary chemical interactions, Vander Waals, hydrogen bonds, electrostatic attraction or
hydrophobic interactions.
• 2 steps:1. CONTACT STAGE 2.CONSOLIDATION STAGE
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The two steps of the bioadhesion process
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BUCCOADHESIVE THEORY
4 Types:
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ADSORPTION THEORY
WETTING THEORY
DIFFUSION THEORY
FRACTURE THEORY
1.Adsorption Theory• According to the adsorption theory, the buccoadhesive device
adheres to the mucus by secondary chemical interactions, such as Vander Waals, hydrogen bonds & hydrophobic interactions.
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Secondary interactions resulting from interdiffusion of polymer chains of bioadhesive
device and mucus.
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2. Wetting TheoryThe wetting theory applies to liquid systems which present affinity to the surface in order to spread over it.
This affinity can be found by using techniques such as the contact angle measurement.
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Schematic diagram showing influence of contact angle between device and mucous
membrane on bioadhesion
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3.Diffusion Theory• Diffusion theory describes the interpenetration of both polymer
and mucin chains to a sufficient depth to create a semi-permanent adhesive bond.
• It is believed that the adhesion force increases with the degree of penetration of the polymer chains.
• In order for diffusion to occur, it is important that the components involved have good solubility, that is, both the bioadhesive and the mucus have similar chemical structures.
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Schematic representation of the diffusion theory of bioadhesion. (a) Blue polymer layer and red mucus
layer before contact; (b) Upon contact; (c) The interface becomes diffuse after contact for a period of
time
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4.Fracture Theory• It analyses the force required to separate two surfaces after adhesion
is established.
• Since the fracture theory is concerned only with the force required to separate the parts, it does not take into account the diffusion of polymer chains.
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FACTORS AFFECTING BUCCOADHESION
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POLYMER RELATED FACTOR
• i) Molecular weightii) Concentration of polymeriii) Flexibility of polymer chainsiv) Swelling
PHYSIOLOGICAL FACTOR
•i) Mucin turnover•ii)Disease state
ENVIRONMENTAL FACTOR
•i)pH of polymer - substrate interfaceii) Applied strengthiii) Initial contact time
1. Polymer-Related Factors
Molecular weight: • At least 1,00,000 molecular weight.• Buccoadhesiveness increases with increasing molecular weight.Concentration of polymer:• More concentrated buccoadhesive dispersion retain on mucus
membrane for longer period of time. Flexibility of polymer chains:• As water soluble polymers become cross linked, the mobility of an
individual polymer chain decreases.Swelling:
Swelling depends on concentration & presence of water.
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2.Environment-Related FactorspH of polymer–substrate interface:
The pH of the medium is important for the degree of hydration. e. g. polycarbophil does not show adhesive property above pH 5.
Applied strength: The adhesion strength increases with the applied strength.
Initial contact time: Buccoadhesive strength increases as the initial contact time increases.
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3. Physiological FactorsMucin turnover:
Important because of two reasons;• To limit the residence time of the buccoadhesives on the mucus
layer.• Substantial amounts of soluble mucin molecule.
Disease states:Disease states where the mucosa is damaged would also be expected to change in permeability.
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BUCCOADHESIVE POLYMERS
• Buccoadhesive polymers are water-soluble and water insoluble polymers, which are swellable networks, jointed by cross-linking agents.
• Has predominant hydrophilicity, suitable surface property, sufficient flexibility.
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Characteristics of an ideal polymer
1. The polymer and its degradation products should be non-toxic.
2. non-irritant to the mucous membrane.
3. Form a non-covalent bond with mucin-epithelial cell surfaces.
4. Adhere quickly to moist tissue .
5. Allow easy incorporation of the drug.
6. Must not decompose on storage or during the shelf life of the
dosage form.
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Natural Polymers• Gelatin• Chitosan• Tragacanth• Sodium alginate• Proteins
Synthetic Polymer• Cellulose Derivatives• PVP• Poly vinyl alcohol
Polymers used in buccoadhesive dosage
forms
Advantages of natural polymer
• Biodegradable• Biocompatible and non-toxic• Low cost• Environmental-friendly processing.• Local availability. • They have better patient tolerance.
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BUCCOADHESIVE DOSAGE FORMS
Type1 •Single layer device with multidirectional release•Significant loss due to swallowing
Type2 •Impermeable baking layer is superimposed•Prevent drug loss in oral cavity
Type3 •Unidirectional release device, drug loss is minimal•achieved by coating every face except contact face
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DESIGN OF BUCCOADHESIVE DOSAGE FORMS
Matrix Type:• Buccal patches are
designed in matrix configuration contains drug, Adhesives & additives mixed together.
• Bidirectional patches release drug in both the mucosa & mouth.
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• Reservoir Type:The buccal patches are designed in a reservoir system contain cavity for a drug & additives separate from adhesives.Impermeable baking material applied to control the delivery; to reduce patch deformation & disintegration in the mouth & to prevent drug loss.
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Buccal tablets:• Small, flat or concave.• Can be applied to different site of oral cavity.Buccal Lozenges:• For local delivery of drug.• Required multiple dosing in a day.Buccal patches & films:• Flexible & comfortable.• Intimate contact.• Baking layer, reservoir layer, bioahesive surfaceBuccal gels & ointments:• Easy dispersion• Poor retention of gels at the site of application overcome by using
bioadhesive formulation.Bioadhesive liquids:
Commercially available drug for systemic delivery by the oral
Mucosal Route
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Drug Brand name Dosage form
Lidocaine DentiPatch extended-release Patches
Melatonin Cydot Patches
Prochlorperazine Buccastem Tablets
Miconazole Tibozole Tablets
Fentanyl Fentora Tablets
REFERENCES• M.S. Wani, Dr. S.R. Parakh,, V.V. Chopade, V.V. Pande, in: Current
Status In Buccal Drug Delivery System: A review• www.slideshare.net/shivamthakore/buccal-drug-delivery-system-ppt• Anjali Gureja, N Jawahar Mihir Trivedi, Prashant Subhashrao Wake;
Pharmatutor; Buccoadhesive Drug Delivery System.• www.slideshare.net/JaideepSarkar/jaideep-sarkar-buccomucosal-
drug-delivery system• Ahuja A., Dogra M., and Agrawal S.P., 1995. Indian J. Pharm Sci.
57(1), 2630.• Pramod Kumar T.M., Shiva Kumar H.G., Desai K.G., 2004. Oral
Transmucosal Drug Delivery Systems. Indian Drugs ,41(2): 63-75• www.pharmatutor.com/Saumya Samanta et al. Oral Mucoadhesive
Drug Delivery Systems: A Review
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