Transcript An Overview On Buccal Drug Delivery System

Hasina Basharat
09-arid-1505
PhD Scholar Of Zoology
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Introduction
Definition
Concepts
Structural and functional
features of oral mucosa
Advantages
Disadvantages
Categories of drug delivery
system
Novel buccal dosage forms
Novel mucoadhesive
polymers
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Market products
Research activity
Conclusion
Future Aspects
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Noninvasive systemic administration .Placing a drug or drug
delivery system in a particular region of body for extended
period of time
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Local targeting / systemic drug delivery
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Recent approaches : Bioadhesive polymers
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Mucoadhesive dosage forms : Wet adhesives
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Mucoadhesion is defined as the interaction between a mucin
surface and a synthetic or natural polymer
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Bioadhesion is the state in which two materials, are
held together for an extended period of time by
interfacial forces.
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The term bioadhesion implies attachment of drugcarrier system to specific biological location.
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If adhesive attachment is to mucous coat then
phenomenon is referred to as mucoadhesion.
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These drug delivery systems utilize property of
bioadhesion of certain water soluble polymers which
become adhesive on hydration and hence can be used for
targeting particular site.
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Definition:- Buccal delivery is the administration of the
drug via buccal mucosa (lining of the cheek) to the
systemic circulation.
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STRUCTURAL FEATURES OF ORAL CAVITY
Outer oral vestibule, which is bounded by cheeks,
lips, teeth and gingiva.
Oral cavity is that area of mouth delineated by the
lips, cheeks, hard palate, soft palate and floor of
mouth.
Oral cavity proper, which extends from teeth and
gums back to the faces with the roof comprising the
hard and soft palate.
The tongue projects from the floor of the cavity.
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FUNCTIONS OF ORAL CAVITY
It helps in chewing, mastication and mixing of food stuff.
Helps to lubricate the food material and bolus.
To identify the ingested material by taste buds of tongue.
To initiate the carbohydrate and fat metabolism.
As a portal for intake of food material and water.
To aid in speech and breathing process.
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Vascular system have been
described by Stablein & Meyer
(1984)
Mucous membrane of buccal
cavity is highly vascular
Blood supply to mouth : External
carotid artery
Maxillary artery
(Cheek, hard palate)
Lingual artery
(Tongue, gingiva,
Mouth floor)
Facial artery
(Lips, soft palate)
Table:- Blood flow in the various
regions of the oral mucosa
TISSUE
BLOOD
FLOW
Ml/min/100 cm2
Buccal
2.40
Sublingual
3.14
Floor of mouth
0.97
Ventral tongue
1.17
Frenulum
1.00
Gingival
1.47
Palatal
0.89
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The oral mucosa has a rich blood supply.
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Buccal administration, the drug gains direct entry into the
systemic circulation there by passing the first pass effect. like
insulin or other proteins, peptides and steroids.
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It is good accessibility to the membranes that line the oral
cavity, which makes application painless and with comfort.
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In case of emergencies. Patients can control the period of
administration.
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Increased ease of drug administration
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Relatively small absorptive surface area(0,01sq m vs.
100sq m in GIT)
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Movement affects mucoadhesive system
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Less permeable than small intestine
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Salivation and swallowing
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Taste of the drug
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1. Sublingual delivery: It is the administration of the
drug via the sublingual.
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2. Buccal delivery: It is the administration of drug via
the buccal mucosa to the systemic circulation.
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3. Local delivery: for the treatment of conditions of the
oral cavity, ulcers, fungal conditions and periodontal
disease .
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The novel type buccal dosage forms include:
Buccal adhesive patches,
Tablets,
Films,
Semisolids (ointments and gels)
Powders.
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1. Patches and Films
Patches is consists of:
 Two laminates,
 With an aqueous solution of the adhesive polymer being
cast onto an impermeable backing sheet,
The film which is applied to the oral mucosal can be
retained in place for at least 12 hours even when it is
challenged with fluids.
 E.g. buccal film of salbutamol.
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2. Buccal mucoadhesive tablets
Mucoadhesive tablets are :
dry dosage forms
 it is to be moistened prior to placing in contact with buccal mucosa.
 It is double layer tablet, consisting of adhesive matrix layer of
polyacrylic acid and hydroxy propyl, cellulose with an inner core of
cocoa butter containing
 insulin
 and a penetration enhancer (sodium glycocholate)
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3. Semisolid Preparations (Ointments and Gels)
Consists of finely ground pectin, gelatin and
sodium carboxy methyl cellulose dispersed in a poly
(ethylene) and a mineral oil gel base.
 Which can be maintained at its site of application
for 15-150 minutes.
Example.chitosan glutamate buccal hydrogel with
local anaesthetics activity .
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4. Powders
Beclomethasone and Hydroxpropyl cellulose in
powder form when sprayed onto the oral mucosa of
rats.
 A significant increase in the residence time relative
to an oral solution is seen.
 And 2.5% of beclomethasone is retained on buccal
mucosa for over 4 hours (Edsman K et al,2005)
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5. BUCCAL SPRAYS.
Generex bio technology have been introduced
insulin spray.
This technology is being used to develop a
formulation for buccal delivery of insulin for the
treatment of type -1 diabetes.
 Buccal spray delivers a mist of fine droplets onto
mucosal membrane probably on to mucin layer.
E.g. Estradiol spray.
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Factors Affecting Buccal Absorption
1. Membrane Factors:
This involves degree of keratinization.
 Surface area available for absorption.
Mucus layer of salivary pellicle.
Intercellular lipids of epithelium.
 Basement membrane and lamina propria.
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In addition, the absorptive membrane thickness, blood
supply/ lymph drainage,
 Cell renewal and enzyme content will all contribute to
reducing the rate and amount of drug entering the
systemic circulation.
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2. Environmental Factors
A. Saliva
The thickness of salivary film is 0.07 to
0.10 mm.
 The thickness, composition and movement
of this film affect the rate of buccal
absorption.
It coats throughout the lining of buccal
mucosa and is called salivary pellicle or film.
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B. Movement of Buccal Tissues
Buccal region of oral cavity shows less
active movements.
 The mucoadhesive polymers are to be
incorporated to keep dosage form at buccal
region for long periods to withstand tissue
movements during talking and if possible
during eating food or swallowing.
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C. Salivary glands
It is located in epithelial or deep
epithelial region of buccal mucosa.
 They constantly secrete mucus on
surface of buccal mucosa.
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Active Ingredients of Drugs Delivered Via Buccal Route
Morphine sulphate,
 Nicotine,
Nifedipine,
 Omeprazole,
Oxytocin,
Piroxicam,
Acitretin,
Acyclovir Arecoline,
 Buprenorpine,
Carbamazepine,
 Chitosan,
Chlorpheniramine maleate,
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Novel mucoadhesive polymers
Capable of forming covalent bonds with the mucus and
the underlying cell layers
 New generation of mucoadhesives, except thiolated
polymers, can adhere directly to the cell surface, rather
than to mucus.
 Interact with the cell surface by means of specific
receptors or covalent bonding instead of non-specific
mechanisms, which are characteristic of the previous
polymers
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Thiolated mucoadhesive polymers
•Provide much higher adhesive properties than polymers generally
considered to be mucoadhesive
•Interact with cysteine-rich sub domains of mucus glycoproteins
via disulfide exchange reactions or via simple oxidation process.
•Carbodiimide-mediated thiol bond, exhibit much improved
mucoadhesive properties
•Tensile strength, high cohesive properties, rapid swelling and
water uptake behavior
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Target-specific mucoadhesive polymers
•Able to selectively create specific molecular interactions with a
particular target, such as a receptor on the cell membrane of a
specific tissue, is a very attractive potential for targeted delivery.
•Specific proteins or glycoproteins, such as lectins, which are
able to bind certain sugars on the cell membrane, can increase
bioadhesion and potentially improve drug delivery via specific
binding and increase the residence time of the dosage
Form.
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CONTI……
•Application of tomato lectin in oral drug delivery for the first
time.
• Lectin-mediated mucoadhesive polymers, as second-generation
mucoadhesives, contain an enormous potential for future use in
drug delivery which, unfortunately, have not yet been fully
explored.
•The recent idea of developing blectinomimetics Q (lectin-like
molecules) based on lectins, and even biotechnologically
generated derivatives of such molecules, holds an interesting
future for this class of bioadhesion molecules
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Bacterial adhesion
•The adhesive properties of bacterial cells, as a more complicated
adhesion system, have recently been investigated.
•The ability of bacteria to adhere to a specific target is rooted from
particular cell-surface components or appendages, known as fimbriae,
which facilitate adhesion to other cells or inanimate surfaces.
•The attractiveness of this approach lies in the potential increase in the
residence time of the drug on the mucus and its receptor-specific
interaction, similar to those of the plant lectins.
•As an example, Escherichia coli have been reported to specifically
adhere to the lymphoid follicle epithelium of the ileal Peyer’s patch in
rabbits. Additionally, different staphylococci possess the ability to adhere
to the surface
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Biopolymers
•The use of polymers from natural sources in drug delivery
systems has become a very popular field of research;
•However, the oral transmucosal drug delivery system is
most common among all other delivery systems.
• Recently, more than 50 biopolymers have been identified
and isolated
•For oral transmucosal drug delivery system and most of
them are used frequently in various drug delivery systems.
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Marketed products
STRIANT
Manufactured by - Columbia Labs,
Uses: it is a testosterone extended-release buccal tablet that
delivers testosterone systemically for hormone replacement in
hypogonadal men.
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Buccal Methyltestosterone
Metandren
Manufactured by- Ciba Pharmaceuticls
Uses- Avoids first-pass hepatic metabolism
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Marketed Preparations
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RESEARCH ACTIVITY
Buccal drug delivery various research activity is going on in the
pharmaceutical industries are as follow.
1. Chitosan Based Sustained Release Mucoadhesive Buccal Patches
Containing Verapamil Hcl.
2. Formulation and Evalutation of Ropinitrole Buccal patches using
Different Mucoadhesive Polymers.
3. Developmement Of Mucoadhesive Buccal Patch Containing
Aceclofenac: In Vitro Evaluations
4. Design and evaluation of buccal patches of valsartan
5. Formulation and Evaluation of Mucoadhesive Buccal Patches of
Aceclofenac.
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CONCLUSION
Buccal drug delivery is a promising area for continued research
with the aim of systemic delivery of orally inefficient drugs
 Buccal drug delivery system is having the several advantages for
controlled drug delivery for extended periods of time in that mucosa
is well supplied with both vascular and lymphatic drainage and
first-pass metabolism in the liver and pre-systemic elimination in
the gastrointestinal tract are avoided.
However, with the developments of new formulations, such as
bioadhesive preparations may increases in the future.
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Future aspects
In mucoadhesive placebo buccal patches we can use any
potent drugs which fulfill the criteria for buccal patch as drug
delivery system.
 We can perform the dissolution of medicated
mucoadhesive buccal patch for drug release profile studies.
 We can further perform the in-vivo studies for the
prepared mucoadhesive buccal patches.
 We can perform the stability test for the prepared
mucoadhesive buccal patches
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D.K. Sanghi and Rakesh Tiwle.2015. An overview on buccal drug delivery
system, Inter. J. of Pharmacotherapy ,5(1): 8-16.
Nishan N Bobade, Sandeep C Atram, Vikrant P Wankhade, Dr. SD Pande, Dr. KK
Tapar.2013. A Review on Buccal Drug Delivery System. International Journal of
Pharmacy and Pharmaceutical Science Research, 3(1): 35-40.
Recent trends in oral transmucosal drug delivery systems: an emphasis
on the soft palatal route Nookala Venkala Satheesh Madhav, Ravindra
Semwal†, Deepak Kumar Semwal & Ruchi B Semwal †Dehradun Institute of
Technology, Faculty of Pharmacy, Makkawala, Dehradun, Uttarakhand, India
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