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.
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 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.