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Mucosal Drug Delivery

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MUCOSAL DRUG DELIVERY

SYSTEMS
INTRODUCTION
• For drug delivery purpose, the term bioadhesion implies attachment of a
drug carrier system to a specific biological location.
• The biological surface can be epithelial tissue. If adhesive attachment is to a
mucus coat, the phenomenon is referred to as mucoadhesion.
• Hence a bacterial attachment is to tissue surfaces, and mucoadhesion can be
modeled after the adherence of mucus on epithelial tissue.
• Mucoadhesion is the relatively new and emerging concept in drug delivery.
• Mucoadhesion keeps the delivery system adhering to the mucus membrane.
By this definition, the mucosal routes for drug delivery are:
1. Buccal /oral route
2. Nasal route
3. Ocular route
4. Vaginal route
5. Gastrointestinal route
NEED OF MUCOADHESIVE DELIVERY
• As compared to oral controlled release systems, mucoadhesive delivery system have
several advantages by virtue of prolongation of residence time, drug targeting,
intimate contact between dosage form and the absorptive mucosa
• Mucoadhesive dosage forms have been used to target local disorders at the mucosal
surface to reduce dose and to minimize the side effects.
• Mucoadhesive formulations use polymers as the adhesive component. These polymers
are often water soluble and when used in a dry form, they attract water from the
mucosal surface and this water transfer leads to a strong interaction further increasing
the retention time over the mucosal surfaces and leads to adhesive interactions.
• Prolonged contact time of a drug with a body tissue through the use of a bioadhesive
polymer can significantly improve the performance of many drugs
MECHANISM OF MUCOADHESION

• The mechanism of mucoadhesion between hydrogels and mucosa can be


described in three steps.
1. Wetting and swelling
2. Interpenetration of the bioadhesive polymer
3. Formation of weak chemical bonds

MUCOADHESIVE POLYMERS PROPERTIES
• Swell in the aqueous biological environment of the delivery–absorption site.
• Interact with mucus or its components for adequate adhesion.
• When swelled they allow, controlled release of the active compound.
• Be excreted unaltered or biologically degraded to inactive, non-toxic
oligomers.
• Sufficient quantities of hydrogen bonding chemical groups.
• Possess high molecular weight.
• Possess high chain flexibility.
• Surface tension that will induce spreading into mucous layer
CLASSIFICATION MUCOADHESIVE
POLYMERS

• Polymer are classified as follows:


1. First generation polymer: Anionic polymer: poly(-acrylic acid), carbopol,
polycarbophil, Cationic polymer: Chitosan
2. Second generation polymer: Lecitins, bacterial adhesion
3. New generation polymer: Thiomers
BUCCAL DRUG DELIVERY

• The buccal cavity offers many advantages for drug delivery application
• Various polymers such as sodium carboxymethylcellulose,
hydroxypropylcellulose and polycarbophil are used for delivery of peptides,
protein and polysaccharides by this routes have been examined
• Although gel and ointments are the most patient convenient; tablets, patches
and films have also been examined
EVALUATION PARAMETERS FOR BUCCAL
DDS

• Dosage form dependent evaluation


• Buccal Mucoadhesive force, strength,
• Diffusion
• Drug release etc
OPTHALMIC DRUG DELIVERY
• The delivery of therapeutic agents to the eye may be achieved using various
types of dosage forms including liquid drops, gels, ointments and solid ocular
inserts (both degradable and nondegradable)
• Mucoadhesive polymers would be expected only to attach to conjunctival
mucus in vivo.
VAGINAL DRUG DELIVERY SYSTEMS

• Vaginal drug delivery offers many advantages such as


1. The avoidance of hepatic first-pass metabolism,
2. A decrease in hepatic side effects and avoidance of tissue damage, and
infection commonly observed for parenteral drug delivery routes
3. Typical bioadhesive polymers that have been in vaginal formulations
include polycarbophil, hydroxypropylcellulose and polyacrylic acid
NASAL DRUG DELIVERY

• The nasal cavity provides a large highly vascularised surface area through
which first-pass metabolism can be avoided,
• As blood is drained directly from the nose into the systemic circulation.
• Successful nasal delivery has been obtained using solutions, powders, gels
and microparticles.
EVALUATION OF MUCOADHESIVE DRUG
DELIVERY SYSTEMS

1. Measuring the force of attachment


2. In vitro residence time study
3. Thumb test

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