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Contents:
Introduction. Approaches To Gastric Retention. Muco-adhesive Systems. Need For Mucoadhesive Microsphere. Advantages. Mechanism of Mucoadhesion. Theories of Mucoadhesion. Polymers Used In Mucoadhesive Microsphere. Factors Affecting Mucoadhesion. Techniques of Formulation Mucoadhesive Microspheres. Evaluation Method of Mucoadhesive Microsphere. Limitation of Gastroretentive Mucoadhesive System.
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Introduction
The control of gastrointestinal transit of orally administered dosage form
Gastroretentive drug delivery systems (GRDDS) can improve the bioavailability of drugs that exhibit site-specific absorption. Adhesion : sticking of materials with one to another by producing Bond in between them. Bioadhesion : it is defined as the attachment of synthetic or biological
Floating Systems.
Floating Drug Delivery Systems (FDDS) have a bulk density lower than gastric fluids thus remain buoyant in stomach. the system floats on gastric contents, the drug is released slowly at a desired rate from the system
Gastric contents have a density close to water (~1.004). A density close to 2.5g cm-3 is necessary for significant
The commonly used excipients in high density system includes barium sulphate, zinc oxide, iron powder, and titanium dioxide.
Bio/Muco-adhesive Systems.
The technique involves coating of microcapsules with bioadhesive polymer, which enables them to adhere to intestinal mucosa and
remain for longer time period in the GI while the active drug is
released from the device matrix.
The cationic chitosan polymers are pharmaceutically acceptable to be used in the preparation of bioadhesive formulations owing to their known ability to bind well to gastric mucosa.
Advantages
Prolongs the residence time of the dosage form at the site of absorption. Due to an increased residence time it enhances absorption and hence the therapeutic efficacy of the drug. Excellent accessibility. Rapid absorption because of enormous blood supply and good blood flow rates. increase in drug bioavailability due to first pass metabolism avoidance. Drug is protected from degradation in the acidic environment in the GIT. Improved patient compliance- ease of drug administration. faster onset of action is achieved due to mucosal surface.
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MECHANISM OF MUCOADHESION
Mucoadhesion has the following mechanism, Intimate contact between a bioadhesive and a membrane (wetting or swelling phenomenon). Penetration of the bioadhesive into the tissue or into the surface of the mucous Membrane (interpenetration).
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THEORIES OF MUCOADHESION
Electronic theory
Electron transfers occur upon contact of adhesive polymer with a mucus glycoprotein network because of difference in their electronic structures. This results in the formation of electrical double layer at the interface and provides an intimate contact between a dosage form and absorbing tissue.
Absorption theory
After an initial contact between two surfaces, the material adheres
Diffusion theory
The polymer chains and the mucus mix to a sufficient depth to create a semi permanent adhesive bond.
Wetting theory
If two substrate surfaces are brought in contact with each other in
the presence of the liquid, the liquid may act as an adhesive among
the substrate surface.
Cohesive theory
The cohesive theory proposes that the phenomena of bioadhesion are mainly due to intermolecular interaction amongst like molecule
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Hot Melt Microencapsulation Solvent Removal Hydrogel Microspheres Phase Inversion Microencapsulation Solvent Evaporation Spray Drying
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II. III.
IV. V.
VI.
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Spray Drying
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2.
3. 4.
5.
6. 7. 8. 1. 2.
3.
4. 5.
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Bioadhesion in the acidic environment and high turnover of mucus may raise questions about the effectiveness of this technique.
Not suitable for drug that may cause gastric lesions eg. Non- steroidal antiinflammatory drug.
The mucus on the walls of the stomach is in a state of constant, resulting in unpredictable adherence.
Drugs that are irritant to gastric mucosa are not suitable for GRDDS. The bioadhesion system in patients with achlorhydria can be questionable in case of swellable system, faster swelling properties are required and complete swelling of the system should be achieved well before the gastric emptying time.
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Rferences
Deshpande, A. A., Shah, N.H., Rhodes, C.T., Malick, W.,
References
Atyabi, F., Sharma, H.L., Mohammad, H., Fell, J. T., In-vivo
systems. In: Jain NK. editor. Progress in controlled and novel drug
delivery systems. CBS Publishers and Distributors. New Delhi. 2004. p. 76-97.
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