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BUCCAL DRUG DELIVERY
SYSTEM
PRESENTING BY,
Ms. Rasika .Walunj
M.Pharm (QAT)
Modern College Of Pharmacy (for ladies) Moshi
Introduction
• Novel drug delivery systems(NDDS) are the system
where the man searches for now method of entry of
drug in to the body in order to show its activity in the
body.
• The new drug delivery system that have been
developed and developing are the mucoadhesive drug
delivery systems, drug patches, transdermal patches
etc.
Buccal drug delivery system
• The buccal mucosa lines the inner cheek and buccal
formulation are placed in mouth between the upper
gums and cheek to treat local and systemic conditions
• It is richly vascularized and more accessible for the
administration and removal of dosage from.
• Additionally ,buccal drug delivery has highly patient
acceptability compared to other non-oral routes of
drug administration.
• Extensive first pass metabolism and drug
degradation in the harsh gastrointestinal environment
can be administering the drug via buccal route.
Continue
• Drug absorption through buccal mucosa is mainly by
passive diffusion into lipoidal membrane.
• After absorption ,the drug is transported through
facial vein which then drains into the general
circulation via jugular vein, by passing the liver and
there by sparing the drug from first pass metabolism.
• Buccal route provides one of the potential routes for
typically large, hydrophilic and unstable proteins,
oligonucleotides and polysaccharides as well as
conventional small drug molecules.
Advantages Of Mucoadhesive Buccal Drug
Delivery Systems
1. Ease of administration.
2. Termination of therapy is easy.
3. Permits localization of drug to the oral cavity for a
prolonged period of time.
4. Can be administered to unconscious patients.
5. Offers an excellent route, for the systemic delivery
of drugs with high first pass metabolism, thereby
offering a greater bioavailability.
6. A significant reduction in dose can be achieved
thereby reducing dose related side effects.
Continue
 Drugs which are unstable in the acidic environment are destroyed
by enzymatic or alkaline environment of intestine can be
administered by this route.
 Drugs which show poor bioavailability via the oral route can be
administered conveniently.
 The presence of saliva ensures relatively large amount of water
for drug dissolution unlike in case of rectal and transdermal
routes.
 Systemic absorption is rapid.
 This route provides an alternative for the administration of
various hormones, narcotic analgesic, steroids, enzymes,
cardiovascular agents etc.
 The buccal mucosa is highly perfused with blood vessels and
offers a greater permeability than the skin.
Disadvantages
• 1. Drugs, which irritate the oral mucosa, have a bitter or unpleasant
taste, odour; can not be administered by this route.
• 2. Drugs, which are unstable at buccal pH can not be administered
by this route.
• 3. Only drugs with small dose requirements can be administered.
• 4. Drugs may swallow with saliva and loses the advantages of buccal
route.
• 5. Only those drugs, which are absorbed by passive diffusion can be
administered by this route.
• 6. Eating and drinking may become restricted.
Limitations:
• The mucus is constantly removed from the
epithelial surfaces. It will eventually wash out the
dosage form from the site of application.
• The mucous turn over rate is different from
person to person so fabrication of the dosage
form is difficult.
• The adhesion rate of dosage form in the body
may not be as per proposed specification due to
disease state, different physiological factors, etc.
Limitations:
• The good mucoadhesive polymers that will
fulfill all the requirements are less.
• Mucoadhesive polymers are poly electrolytes.
Slight variation in pH, charge of the mucus
changes mucoadhesion property of polymer
significantly.
• This type of drug delivery system is not
suitable for drugs that causes tissue irritation
Uses of Buccal Delivery
 The oral cavity can be used for local and
systemic therapy.
Examples of local therapy would be the
treatment of oral infections , dental caries,
mouth ulcers, stomatitis , gingivitis etc.
The buccal route is of particular interest with
regard to the systemic delivery of small
molecules that are subjected to first-pass
metabolism
Drug Delivery Pathways
Two possible routes of drug absorption through
oral mucosa .
Oral Mucosa
Environment Of Buccal Mucosa
• The cells of the oral epithelia are surrounded
by an intercellular ground substance, mucus.
• The oral cavity is marked by the presence of
saliva produced by the salivary glands.
• Mucus which is secreted by the major and
minor salivary glands as part of saliva .
Environment Of Buccal Mucosa
• Role of Saliva•
• Continuous mineralization / demineralization of the
tooth enamel
• Protective fluid for all tissues of the oral cavity
• To hydrate oral mucosal dosage forms
• Role of Mucus•
• Bioadhesion of mucoadhesive drug delivery systems
• Made up of proteins and carbohydrates
• Cell-cell adhesion
• Lubrication
Buccal Drug Delivery And
Mucoadhesivity
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 and
powders.
Design Of Buccal Dosage Form
• Matrix type :
The Buccal patch designed in a matrix
configuration contains drug, adhesive, and
additives mixed together.
Bi-directional patches release drug in both the
mucosa and the mouth
Drug + Mucoadhesive Matrix
Design Of Buccal Dosage Form
• Reserviour type: The buccal patch designed
in a reservoir system contains a cavity for the
drug and additives separate from the adhesive.
• Impermeable backing is applied to control the
direction of drug delivery; to reduce patch
deformation and disintegration while in the
mouth; and to prevent drug loss.
Design Of Buccal Dosage For
BUCCAL MUCOADHESIVE
DOSAGE FORMS
• Three types based on their geometry
Type-l
1.Single layer device with multidirectional release.
2.Significant drug loss due to swallowing.
Type-ll
1.Impermeable backing layer is superimposed.
2.Preventing drug loss into the oral cavity.
Type-lll
1. Unidirectional release device, drug loss is minimal.
2. Achieved by coating every face except contact face.
BUCCAL FORMULATION
• Buccal tablets :
• Buccal tablets are small, flat, and oval shaped dosage
form.
• Unlike conventional tablets, buccal mucoadhesive
tablets allow for drinking and speaking without major
discomfort .
• They soften, adhere to the mucosa , and are retained in
position until dissolution and/or release is complete .
These tablets can be applied to different sites in the oral
cavity, including the palate, the mucosa lining the
cheek, as well as between the lip and the gum .
Buccal tablets
• These tablets are usually prepared by direct compression , but wet
granulation techniques can also be used.
• Multilayered tablet may be prepared by sequentially adding and
compressing the ingredients layer by layer.
• Some newer approaches use tablets that melt at body temperature.
• The two buccal bioadhesive tablets Commercially available
buccoadhesive tablets in UK are " Bucastem “ (Nitroglycerine)
and " Suscard buccaP '(Prochloroperazine).
• Examples:
• a) Nitroglycerin bioadhesive tablets for the treatment of
anginapectories.
• b )Sumatriptan succenate buccal adhesive tablet which is effective
in the acute treatment of mygrain and cluster headache.
Buccal Patch/Film
• Buccal Patch/Film are laminates consisting of an
impermeable backing layer, a drug-containing reservoir
layer from which the drug is released in a controlled
manner, and a bioadhesive surface for mucosal
attachment .
• Two methods used to prepare adhesive patches include
solvent casting and direct milling .
• In the solvent casting method , the intermediate sheet
from which patches are punched is prepared by casting
the solution of the drug and polymer(s) onto a backing
layer sheet and subsequently allowing the solvent(s ) to
evaporate.
CONT…
• In the direct milling method , formulation constituents are
homogenously mixed and compressed to the desired
thickness, and patches of predetermined size and shape are
then cut or punched out.
• An impermeable backing layer may also be applied to
control the direction of drug release , prevent drug loss, and
minimize deformation and disintegration of the device
during the application period.
• Example: a) Isosorbid dinitrate in the form of
unidirectional erodible buccal film are developed and
characterized for improving bioavailability. b) Buccal film
of salbutamol sulphate and terbutalin sulphate for the
treatment of asthma. c) Buccoadhesive film of clindamycin
used for pyorrhoea treatment
Buccal Gel/Ointment
• Buccal Gel/Ointment Such semisolid dosage
forms have the advantage of easy dispersion
throughout the oral mucosa .
• Has been overcome by using bioadhesive
formulations .
• Certain bioadhesive polymers undergo a phase
change from a liquid to a semisolid; this
change enhances the viscosity , which results
in sustained and controlled release of drugs
Evaluation Of Buccal Tablets
• Parameters of Evaluation :
• Determination of residence time.
• Permeation studies.
• Swelling studies.
• Release rate studies.
• Toxicity and irritation study.
• Bioadhesion measurement.
• Folding Enduance Content uniformity.
• Surface pH: 1% agar solution for 2 hrs and equill.
for 1 min.
PRODUCT
1. Oral bioadhesive formulation :
Corlan – hydrocortisone succinate
Bonjela – hypromellose
Daktarin – miconazole
Corsodyl – chlorohexidine
2. Buccal mucosa formulation :
Buccastem – nausea , vomiting, vertigo
Suscard- angina
CONCLUTION
• Buccal drug delivery is a promising area for
systemic delivery of orally inefficient drugs as
well as an attractive alternative for
noninvasive delivery of potent peptide and
perhaps protein drug molecules
REFRENCES
• 1. International journal of pharmaceutics,
Mucoadhesive Drug Delivery System; Sep 2003,Pg
no-175.
• 2. International journal of pharmaceutics,
Mucoadhesive Drug Delivery System; March 2009,Pg
no-208.
• 3. Advances in controlled and novel drug delivery, N.
K. JAIN,1 st edition, Pg no-78 & 79.

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buccal drug delivery system

  • 1. BUCCAL DRUG DELIVERY SYSTEM PRESENTING BY, Ms. Rasika .Walunj M.Pharm (QAT) Modern College Of Pharmacy (for ladies) Moshi
  • 2. Introduction • Novel drug delivery systems(NDDS) are the system where the man searches for now method of entry of drug in to the body in order to show its activity in the body. • The new drug delivery system that have been developed and developing are the mucoadhesive drug delivery systems, drug patches, transdermal patches etc.
  • 3. Buccal drug delivery system • The buccal mucosa lines the inner cheek and buccal formulation are placed in mouth between the upper gums and cheek to treat local and systemic conditions • It is richly vascularized and more accessible for the administration and removal of dosage from. • Additionally ,buccal drug delivery has highly patient acceptability compared to other non-oral routes of drug administration. • Extensive first pass metabolism and drug degradation in the harsh gastrointestinal environment can be administering the drug via buccal route.
  • 4. Continue • Drug absorption through buccal mucosa is mainly by passive diffusion into lipoidal membrane. • After absorption ,the drug is transported through facial vein which then drains into the general circulation via jugular vein, by passing the liver and there by sparing the drug from first pass metabolism. • Buccal route provides one of the potential routes for typically large, hydrophilic and unstable proteins, oligonucleotides and polysaccharides as well as conventional small drug molecules.
  • 5. Advantages Of Mucoadhesive Buccal Drug Delivery Systems 1. Ease of administration. 2. Termination of therapy is easy. 3. Permits localization of drug to the oral cavity for a prolonged period of time. 4. Can be administered to unconscious patients. 5. Offers an excellent route, for the systemic delivery of drugs with high first pass metabolism, thereby offering a greater bioavailability. 6. A significant reduction in dose can be achieved thereby reducing dose related side effects.
  • 6. Continue  Drugs which are unstable in the acidic environment are destroyed by enzymatic or alkaline environment of intestine can be administered by this route.  Drugs which show poor bioavailability via the oral route can be administered conveniently.  The presence of saliva ensures relatively large amount of water for drug dissolution unlike in case of rectal and transdermal routes.  Systemic absorption is rapid.  This route provides an alternative for the administration of various hormones, narcotic analgesic, steroids, enzymes, cardiovascular agents etc.  The buccal mucosa is highly perfused with blood vessels and offers a greater permeability than the skin.
  • 7. Disadvantages • 1. Drugs, which irritate the oral mucosa, have a bitter or unpleasant taste, odour; can not be administered by this route. • 2. Drugs, which are unstable at buccal pH can not be administered by this route. • 3. Only drugs with small dose requirements can be administered. • 4. Drugs may swallow with saliva and loses the advantages of buccal route. • 5. Only those drugs, which are absorbed by passive diffusion can be administered by this route. • 6. Eating and drinking may become restricted.
  • 8. Limitations: • The mucus is constantly removed from the epithelial surfaces. It will eventually wash out the dosage form from the site of application. • The mucous turn over rate is different from person to person so fabrication of the dosage form is difficult. • The adhesion rate of dosage form in the body may not be as per proposed specification due to disease state, different physiological factors, etc.
  • 9. Limitations: • The good mucoadhesive polymers that will fulfill all the requirements are less. • Mucoadhesive polymers are poly electrolytes. Slight variation in pH, charge of the mucus changes mucoadhesion property of polymer significantly. • This type of drug delivery system is not suitable for drugs that causes tissue irritation
  • 10. Uses of Buccal Delivery  The oral cavity can be used for local and systemic therapy. Examples of local therapy would be the treatment of oral infections , dental caries, mouth ulcers, stomatitis , gingivitis etc. The buccal route is of particular interest with regard to the systemic delivery of small molecules that are subjected to first-pass metabolism
  • 11. Drug Delivery Pathways Two possible routes of drug absorption through oral mucosa .
  • 13. Environment Of Buccal Mucosa • The cells of the oral epithelia are surrounded by an intercellular ground substance, mucus. • The oral cavity is marked by the presence of saliva produced by the salivary glands. • Mucus which is secreted by the major and minor salivary glands as part of saliva .
  • 14. Environment Of Buccal Mucosa • Role of Saliva• • Continuous mineralization / demineralization of the tooth enamel • Protective fluid for all tissues of the oral cavity • To hydrate oral mucosal dosage forms • Role of Mucus• • Bioadhesion of mucoadhesive drug delivery systems • Made up of proteins and carbohydrates • Cell-cell adhesion • Lubrication
  • 15. Buccal Drug Delivery And Mucoadhesivity 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 and powders.
  • 16.
  • 17. Design Of Buccal Dosage Form • Matrix type : The Buccal patch designed in a matrix configuration contains drug, adhesive, and additives mixed together. Bi-directional patches release drug in both the mucosa and the mouth Drug + Mucoadhesive Matrix
  • 18. Design Of Buccal Dosage Form • Reserviour type: The buccal patch designed in a reservoir system contains a cavity for the drug and additives separate from the adhesive. • Impermeable backing is applied to control the direction of drug delivery; to reduce patch deformation and disintegration while in the mouth; and to prevent drug loss.
  • 19. Design Of Buccal Dosage For
  • 20. BUCCAL MUCOADHESIVE DOSAGE FORMS • Three types based on their geometry Type-l 1.Single layer device with multidirectional release. 2.Significant drug loss due to swallowing. Type-ll 1.Impermeable backing layer is superimposed. 2.Preventing drug loss into the oral cavity. Type-lll 1. Unidirectional release device, drug loss is minimal. 2. Achieved by coating every face except contact face.
  • 21. BUCCAL FORMULATION • Buccal tablets : • Buccal tablets are small, flat, and oval shaped dosage form. • Unlike conventional tablets, buccal mucoadhesive tablets allow for drinking and speaking without major discomfort . • They soften, adhere to the mucosa , and are retained in position until dissolution and/or release is complete . These tablets can be applied to different sites in the oral cavity, including the palate, the mucosa lining the cheek, as well as between the lip and the gum .
  • 22. Buccal tablets • These tablets are usually prepared by direct compression , but wet granulation techniques can also be used. • Multilayered tablet may be prepared by sequentially adding and compressing the ingredients layer by layer. • Some newer approaches use tablets that melt at body temperature. • The two buccal bioadhesive tablets Commercially available buccoadhesive tablets in UK are " Bucastem “ (Nitroglycerine) and " Suscard buccaP '(Prochloroperazine). • Examples: • a) Nitroglycerin bioadhesive tablets for the treatment of anginapectories. • b )Sumatriptan succenate buccal adhesive tablet which is effective in the acute treatment of mygrain and cluster headache.
  • 23. Buccal Patch/Film • Buccal Patch/Film are laminates consisting of an impermeable backing layer, a drug-containing reservoir layer from which the drug is released in a controlled manner, and a bioadhesive surface for mucosal attachment . • Two methods used to prepare adhesive patches include solvent casting and direct milling . • In the solvent casting method , the intermediate sheet from which patches are punched is prepared by casting the solution of the drug and polymer(s) onto a backing layer sheet and subsequently allowing the solvent(s ) to evaporate.
  • 24. CONT… • In the direct milling method , formulation constituents are homogenously mixed and compressed to the desired thickness, and patches of predetermined size and shape are then cut or punched out. • An impermeable backing layer may also be applied to control the direction of drug release , prevent drug loss, and minimize deformation and disintegration of the device during the application period. • Example: a) Isosorbid dinitrate in the form of unidirectional erodible buccal film are developed and characterized for improving bioavailability. b) Buccal film of salbutamol sulphate and terbutalin sulphate for the treatment of asthma. c) Buccoadhesive film of clindamycin used for pyorrhoea treatment
  • 25. Buccal Gel/Ointment • Buccal Gel/Ointment Such semisolid dosage forms have the advantage of easy dispersion throughout the oral mucosa . • Has been overcome by using bioadhesive formulations . • Certain bioadhesive polymers undergo a phase change from a liquid to a semisolid; this change enhances the viscosity , which results in sustained and controlled release of drugs
  • 26. Evaluation Of Buccal Tablets • Parameters of Evaluation : • Determination of residence time. • Permeation studies. • Swelling studies. • Release rate studies. • Toxicity and irritation study. • Bioadhesion measurement. • Folding Enduance Content uniformity. • Surface pH: 1% agar solution for 2 hrs and equill. for 1 min.
  • 27. PRODUCT 1. Oral bioadhesive formulation : Corlan – hydrocortisone succinate Bonjela – hypromellose Daktarin – miconazole Corsodyl – chlorohexidine 2. Buccal mucosa formulation : Buccastem – nausea , vomiting, vertigo Suscard- angina
  • 28. CONCLUTION • Buccal drug delivery is a promising area for systemic delivery of orally inefficient drugs as well as an attractive alternative for noninvasive delivery of potent peptide and perhaps protein drug molecules
  • 29. REFRENCES • 1. International journal of pharmaceutics, Mucoadhesive Drug Delivery System; Sep 2003,Pg no-175. • 2. International journal of pharmaceutics, Mucoadhesive Drug Delivery System; March 2009,Pg no-208. • 3. Advances in controlled and novel drug delivery, N. K. JAIN,1 st edition, Pg no-78 & 79.