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MUCOADHESIVE DRUG DELIVERY SYSTEM
By
Chayan Mahata
UNDER THE GUIDENCE AND SUPERVISION OF
KAUSHIK MUKHERJEE
Assistant Professor
Department of Pharmaceutical Technology
JADAVPUR UNIVERSITY
Kolkata-700032
INDIA
 Content
 Introduction
 Basics ,concepts & mucosal membrane.
 Mechanism of mucoadhesion
 Theories mucoadhesion
 Sites of mucoadhesion
 Mucoadhesive polymer
 Factor affecting mucoadhesion
 Advantages & Disadvantages
 Mucoadhesive dosage from
 References
What is Mucoadhesive drug delivery
system?
• Mucoadhesive drug delivery system interact with the
mucus layer covering the mucosal epithelial surface, &
mucin molecules & increase the residence time of the
dosage form at the site of the absorption.
• Mucoadhesive drug delivery system is a part of
controlled delivery system.
Introduction
 Since the early 1980,the concept of Mucoadhesion
has gained considerable interest in pharmaceutical
technology.
 combine mucoadhesive with enzyme inhibitory &
penetration enhancer properties & improve the
patient compliance.
 • MDDS have been developed for buccal ,nasal,
rectal &vaginal routes for both systemic & local
effects.
 Hydrophilic high mol. wt. such as peptides that
cannot be administered & poor absorption, then
MDDS is best choice.
Muco + adhesive
 Inner layers called mucosa
 Inner epithelial Cell lining
 Covered with viscoelastic fluid.
 -Secreted by Goblet cells
 Composed of water and mucin
 Other components include
proteins, lipids and
mucopolysaccharides ,electrolytes
 Main role is protective and
lubricates
 -Tendency substance to remain
adhered to surface
 If substance adhere to Biological
mucosal layers is called as
Mucoadhesion
What is mucus ?
 Mucoadhesive inner layers called mucosa inner epithelial cell lining is
covered with viscoelastic fluid
 Composed of water and mucin.
 Thickness varies from 40 µm to 300 μm
 General composition of mucus
 Water.............................................................95%
 Glycoproteins and lipids.................0.5-5%
 Mineral salts............................................................1%
 Free proteins.............................................................0.5-1%
Mechanisms of Mucoadhesion
The mechanism responsible in the formation of mucoadhesive
bond
• Step 1: Wetting and swelling of the polymer(contact stage)
• Step 2: Interpenetration between the polymer chains and the
mucosal membrane.
• Step 3: Formation of bonds between the entangled chains (both
known as consolidation stage)
Theories mucoadhesion
 Electronic theory:--Attractive electrostatic forces between glycoprotein
mucin network & the bio adhesive material.
 Wetting theory:--Ability of bio adhesive polymers to spread & develop
intimate contact with the mucous membrane.
 Adsorption theory:--Surface forces (covalent bond, ionic bond, hydrogen
bond & van der waals forces) resulting in chemical bonding
 Diffusion theory:--Physical entanglement of mucin strands and flexible
polymer chains.
 Fracture theory:--Analyses the maximum tensile stress develop during
detachment of the BDDS from mucosal surfaces
Mucoadhesive polymers
• They are water soluble and water insoluble polymers which are swellable
networks joined by cross linking agent
Characteristic of ideal polymer.
 Degradation products should be non toxic and non absorbable from GIT
 Good spreadibility, wetting, swelling and biodegradableе properties
 Optimum molecular weight
 Non irritant to mucous membrane
 Form a strong non-covalent bond with mucin epithelial cell surface
Polymer classification
According to their source
Synthetic
Natural and semisynthetic
Carbopol
Agarose
PVA
Chitosan
PVP
Gelatin
Thiolates polymer
Pectin
Methacrylic acid
CMC
Polycarbophil
Thiolate CMC
Factors affecting mucoadhesion
A)Polymer related factors:•
 Molecular weight
 Conc. of polymer
 Flexibility of polymer chains
 Presence of functional group
 Spatial conformation
 Cross linking density
B) Environment related factors:
 pH of polymer substrate interface .
 Applied strength
C) Physiological factors:
 Mucinturn over
 Disease state
Advantages
 Advantages over other controlled oral controlled release systems by virtue of
prolongation of residence of drug in GIT.
 Targeting & localization of the dosage form at a specific site
 Painless administration.
 Low enzymatic activity & avoid of first pass metabolism
Disadvantages
 If MDDS are adhere too tightly because it is undesirable to exert too much
force to remove the formulation after use, otherwise the mucosa could be
injured.
 Some patient suffers unpleasant feeling.
 Unfortunately, the lack of standardized techniques often leads to unclear
results.
 costly drug delivery system.
Mucoadhesive dosage form
Semisolid Solid
 Gels & ointment Tablet
 Films Matrix Tablet
 Patches Bio adhésive microparticles
Bio adhésive inserts
Liquid
Suspensions
Gel forming liquids
References
 Seema Badhaña, Navneet Garud, Akanksha Garud (2013) Colon specific drug
delivery of mesalamine using eudragit S100-coated chitosan microspheres for
the treatment of ulcerative colitis. International Current
Pharmaceutical Journal .42-45.
 Flávia Chiva Carvalho, Marcos Luciano Bruschi (2010) Mucoadhesive drug
delivery systems. Brazilian Journal of Pharmaceutical Sciences. 1-9.
 Phanindra B, B Krishna (2013) Recent advances in mucoadhesive drug deliver
system: A review. Int. J. Pharm. Med. & Bio. Sc. 1 - 15

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MUCOADHESIVE DRUG DELIVERY System PPT JADAVPUR UNIVERSITY

  • 1. MUCOADHESIVE DRUG DELIVERY SYSTEM By Chayan Mahata UNDER THE GUIDENCE AND SUPERVISION OF KAUSHIK MUKHERJEE Assistant Professor Department of Pharmaceutical Technology JADAVPUR UNIVERSITY Kolkata-700032 INDIA
  • 2.  Content  Introduction  Basics ,concepts & mucosal membrane.  Mechanism of mucoadhesion  Theories mucoadhesion  Sites of mucoadhesion  Mucoadhesive polymer  Factor affecting mucoadhesion  Advantages & Disadvantages  Mucoadhesive dosage from  References
  • 3. What is Mucoadhesive drug delivery system? • Mucoadhesive drug delivery system interact with the mucus layer covering the mucosal epithelial surface, & mucin molecules & increase the residence time of the dosage form at the site of the absorption. • Mucoadhesive drug delivery system is a part of controlled delivery system.
  • 4. Introduction  Since the early 1980,the concept of Mucoadhesion has gained considerable interest in pharmaceutical technology.  combine mucoadhesive with enzyme inhibitory & penetration enhancer properties & improve the patient compliance.  • MDDS have been developed for buccal ,nasal, rectal &vaginal routes for both systemic & local effects.  Hydrophilic high mol. wt. such as peptides that cannot be administered & poor absorption, then MDDS is best choice.
  • 5. Muco + adhesive  Inner layers called mucosa  Inner epithelial Cell lining  Covered with viscoelastic fluid.  -Secreted by Goblet cells  Composed of water and mucin  Other components include proteins, lipids and mucopolysaccharides ,electrolytes  Main role is protective and lubricates  -Tendency substance to remain adhered to surface  If substance adhere to Biological mucosal layers is called as Mucoadhesion
  • 6. What is mucus ?  Mucoadhesive inner layers called mucosa inner epithelial cell lining is covered with viscoelastic fluid  Composed of water and mucin.  Thickness varies from 40 µm to 300 μm  General composition of mucus  Water.............................................................95%  Glycoproteins and lipids.................0.5-5%  Mineral salts............................................................1%  Free proteins.............................................................0.5-1%
  • 7. Mechanisms of Mucoadhesion The mechanism responsible in the formation of mucoadhesive bond • Step 1: Wetting and swelling of the polymer(contact stage) • Step 2: Interpenetration between the polymer chains and the mucosal membrane. • Step 3: Formation of bonds between the entangled chains (both known as consolidation stage)
  • 8. Theories mucoadhesion  Electronic theory:--Attractive electrostatic forces between glycoprotein mucin network & the bio adhesive material.  Wetting theory:--Ability of bio adhesive polymers to spread & develop intimate contact with the mucous membrane.  Adsorption theory:--Surface forces (covalent bond, ionic bond, hydrogen bond & van der waals forces) resulting in chemical bonding  Diffusion theory:--Physical entanglement of mucin strands and flexible polymer chains.  Fracture theory:--Analyses the maximum tensile stress develop during detachment of the BDDS from mucosal surfaces
  • 9. Mucoadhesive polymers • They are water soluble and water insoluble polymers which are swellable networks joined by cross linking agent Characteristic of ideal polymer.  Degradation products should be non toxic and non absorbable from GIT  Good spreadibility, wetting, swelling and biodegradableе properties  Optimum molecular weight  Non irritant to mucous membrane  Form a strong non-covalent bond with mucin epithelial cell surface
  • 10. Polymer classification According to their source Synthetic Natural and semisynthetic Carbopol Agarose PVA Chitosan PVP Gelatin Thiolates polymer Pectin Methacrylic acid CMC Polycarbophil Thiolate CMC
  • 11. Factors affecting mucoadhesion A)Polymer related factors:•  Molecular weight  Conc. of polymer  Flexibility of polymer chains  Presence of functional group  Spatial conformation  Cross linking density B) Environment related factors:  pH of polymer substrate interface .  Applied strength C) Physiological factors:  Mucinturn over  Disease state
  • 12. Advantages  Advantages over other controlled oral controlled release systems by virtue of prolongation of residence of drug in GIT.  Targeting & localization of the dosage form at a specific site  Painless administration.  Low enzymatic activity & avoid of first pass metabolism Disadvantages  If MDDS are adhere too tightly because it is undesirable to exert too much force to remove the formulation after use, otherwise the mucosa could be injured.  Some patient suffers unpleasant feeling.  Unfortunately, the lack of standardized techniques often leads to unclear results.  costly drug delivery system.
  • 13. Mucoadhesive dosage form Semisolid Solid  Gels & ointment Tablet  Films Matrix Tablet  Patches Bio adhésive microparticles Bio adhésive inserts Liquid Suspensions Gel forming liquids
  • 14. References  Seema Badhaña, Navneet Garud, Akanksha Garud (2013) Colon specific drug delivery of mesalamine using eudragit S100-coated chitosan microspheres for the treatment of ulcerative colitis. International Current Pharmaceutical Journal .42-45.  Flávia Chiva Carvalho, Marcos Luciano Bruschi (2010) Mucoadhesive drug delivery systems. Brazilian Journal of Pharmaceutical Sciences. 1-9.  Phanindra B, B Krishna (2013) Recent advances in mucoadhesive drug deliver system: A review. Int. J. Pharm. Med. & Bio. Sc. 1 - 15