This document discusses mucoadhesive drug delivery systems (MDDS). It begins by defining MDDS as systems that use the bioadhesive properties of certain polymers to target and prolong the release of drugs at mucous membranes. It then covers the basics of mucous membranes and their structure, composition, and functions. The document discusses the need for MDDS to enhance drug absorption, prolong drug residence time, and target drug delivery. It also outlines the advantages and disadvantages of MDDS, various routes of administration, mechanisms of mucoadhesion, theories of mucoadhesion, mucoadhesive polymers, and methods of evaluating MDDS. In the end, it provides some applications of MDDS such as vaccine delivery, cancer
Mucoadhesive drug delivery system has gained interest among pharmaceutical scientists as a means of promoting dosage form residence time as well as improving intimacy of contact with various absorptive membranes of the bio- logical system
Approaches Of Gastro-Retentive Drug Delivery System or GRDDSAkshayPatane
Approaches Of Gastro-Retentive Drug Delivery System
Includes:
Floating and Non-Floating drug delivery system with their subtypes
Like Non-effervescent system, Effervescent system, Raft forming system,
High Density system, Expandable system, Muco-adhesive system,
Super porous hydrogel system and Magnetic Systems, etc.
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.
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 complaince.
MDDS have been devloped 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.
Mucoadhesiveinner layers called mucosa inner epithelial cell lining is covered with viscoelasticfluid
Composed of water and mucin.
Thickness varies from 40 μm to 300 μm
General composition of mucus
Water…………………………………..95%
Glycoproteinsand lipids……………..0.5-5%
Mineral salts……………………………1%
Free proteins…………………………..0.5-1%
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)
Electronic theory
Wetting theory
Adsorption theory
Diffusion theory
Fracture theory
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
If MDDS are adhere too tightlgy because it is undesirable to exert too much force to remove the formulation after use,otherwise the mucosa could be injured.
-Some patient suffers unpleasent feeling.
-Unfortunately ,the lack of standardized techniques often leads to unclear results.
-costly drug delivery system
Video Lecture is available at https://www.youtube.com/watch?v=DXu_CLgB4q0
Introduction, terminology/definitions and rationale, advantages, disadvantages, selection of drug candidates. Approaches to design-controlled release formulations based on diffusion, dissolution and ion exchange principles. Physicochemical and
biological properties of drugs relevant to controlled release formulations.
Mucoadhesive drug delivery system has gained interest among pharmaceutical scientists as a means of promoting dosage form residence time as well as improving intimacy of contact with various absorptive membranes of the bio- logical system
Approaches Of Gastro-Retentive Drug Delivery System or GRDDSAkshayPatane
Approaches Of Gastro-Retentive Drug Delivery System
Includes:
Floating and Non-Floating drug delivery system with their subtypes
Like Non-effervescent system, Effervescent system, Raft forming system,
High Density system, Expandable system, Muco-adhesive system,
Super porous hydrogel system and Magnetic Systems, etc.
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.
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 complaince.
MDDS have been devloped 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.
Mucoadhesiveinner layers called mucosa inner epithelial cell lining is covered with viscoelasticfluid
Composed of water and mucin.
Thickness varies from 40 μm to 300 μm
General composition of mucus
Water…………………………………..95%
Glycoproteinsand lipids……………..0.5-5%
Mineral salts……………………………1%
Free proteins…………………………..0.5-1%
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)
Electronic theory
Wetting theory
Adsorption theory
Diffusion theory
Fracture theory
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
If MDDS are adhere too tightlgy because it is undesirable to exert too much force to remove the formulation after use,otherwise the mucosa could be injured.
-Some patient suffers unpleasent feeling.
-Unfortunately ,the lack of standardized techniques often leads to unclear results.
-costly drug delivery system
Video Lecture is available at https://www.youtube.com/watch?v=DXu_CLgB4q0
Introduction, terminology/definitions and rationale, advantages, disadvantages, selection of drug candidates. Approaches to design-controlled release formulations based on diffusion, dissolution and ion exchange principles. Physicochemical and
biological properties of drugs relevant to controlled release formulations.
Gastro retentive drug delivery system (GRDDS)Shweta Nehate
Oral route is the most acceptable route for drug administration. Apart from conventional dosage forms several other forms were developed in order to enhance the drug delivery for prolonged time period and for delivering drug to a particular target site. Gastro-retentive drug delivery system (GRDDS) has gainned immense popularity in the field of oral drug delivery recently. it is a widely employed approach to retain the dosage form in the stomach for an extended period of time and release the drug slowly that can address many challenges associated with conventional oral delivery, including poor bioavailability. different innovative approaches are being applied to fabricate GRDDS. Gastroretentive drug delivery is an approach to prolong gastric residence time, there by targeting site-specific drugs release in the upper gastrointestinal tract (GIT) for local or systemic effects. It is obtained by retaining dosage form into stomach and by releasing the in controlled manner.
Implantable drug delivery systems are designed to be placed under the skin and
release drugs into the blood circulation without repetitive insertion of needles.
Therefore, IDDS is defined as “a sterile drug delivery device for subcutaneous
implantation having the ability to deliver drugs at a controlled rate over a
prolonged time period, comprising a rod -shaped polymeric inner matrix
with an elongated body and two ends”.
The all the content in this profile is completed by the teachers, students as well as other health care peoples.
thank you, all the respected peoples, for giving the information to complete this presentation.
this information is free to use by anyone.
Gastro retentive drug delivery system (GRDDS)Shweta Nehate
Oral route is the most acceptable route for drug administration. Apart from conventional dosage forms several other forms were developed in order to enhance the drug delivery for prolonged time period and for delivering drug to a particular target site. Gastro-retentive drug delivery system (GRDDS) has gainned immense popularity in the field of oral drug delivery recently. it is a widely employed approach to retain the dosage form in the stomach for an extended period of time and release the drug slowly that can address many challenges associated with conventional oral delivery, including poor bioavailability. different innovative approaches are being applied to fabricate GRDDS. Gastroretentive drug delivery is an approach to prolong gastric residence time, there by targeting site-specific drugs release in the upper gastrointestinal tract (GIT) for local or systemic effects. It is obtained by retaining dosage form into stomach and by releasing the in controlled manner.
Implantable drug delivery systems are designed to be placed under the skin and
release drugs into the blood circulation without repetitive insertion of needles.
Therefore, IDDS is defined as “a sterile drug delivery device for subcutaneous
implantation having the ability to deliver drugs at a controlled rate over a
prolonged time period, comprising a rod -shaped polymeric inner matrix
with an elongated body and two ends”.
The all the content in this profile is completed by the teachers, students as well as other health care peoples.
thank you, all the respected peoples, for giving the information to complete this presentation.
this information is free to use by anyone.
Buccal drug delivery system is part of mucoadhesive drug delivery system and their principal and formulation ,mechanisam of adhesion to mucosa ,use of polymers in BDDS and permiability enhancers and evaluation parameters of buccal tablets and patchs
Avoid first pass effect,
the presentation is on a currently ongoing new system of drug delivary sytem, muca adhesive drug delivary system, for further details please do knock hasnat2484@gmail.com
Introduction to Mucosal Drug Delivery SystemsAshwiniRaikar1
Introduction, Principle of bioadhesion or mucoadhesion, concepts, advantaged and disadvantages, transmucosal permeability and formulation consideration of buccal delivery systems.
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basic review on microspheres.graphics is used so derz slide within a slide ie...slides which find overlapped download for watching overlaped slides for better view
Delivery of drug through buccal mucosa of oral cavity is called BDDS. The buccal mucosa lines the inner cheek
It is placed between the upper gingivae and cheek.
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2. Contents
• Introduction
• What is mucoadhesive DDS
• Basics ,concepts & mucosal membrane.
• Need of mucoadhesive DDS
• Advantages & Disadvantages
• Different routes of mucoadhesion
• Mechanism of mucoadhesion
• Theories mucoadhesion
• Penetration enhancer
• Mucoadhesive polymer
• Factor affecting mucoadhesion
• Mucoadhesive dosage form
• Evaluation Tests
3. 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 complaince.
• MDDS have been devloped 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.
4. What is mucoadhesive drug delivery
system ?
“Mucoadhesive drug delivery system are the system which
utilizes the property of bioadhesion of certain polymers which
became adhesive on hydration and can be used for targeting a
drug to a particular region of the body for prolonged period of
time”.
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.
5. Basics concepts & structure of mucosal
membrane.
Mucoadhesive inner layers called mucosa inner epithelial cell
lining is covered with viscoelasticfluid.
Composed of water and mucin.
Thickness varies from 40 μm to 300 μm.
6. General composition of mucus
Water…………………………………..95%
Glycoprotein and lipids……………..0.5-5%
Mineral salts……………………………1%
Free proteins…………………………..0.5-1%
Protective : Particularly from its hydrophobicity.
Barrier : In tissue absorption of the drugs and influence the
bioavailability.
Adhesion : Mucus has strong cohesion properties.
Lubrication :keep mucosal membrane moist.
Functions of mucus
7. Need of mucoadhesive DDS
WHY?
Avoidance
of
First pass
Metabolism
Localization
of drug at
given site
Prolong
residence time
Better absorption
of peptide by
penetration
enhancer
Reduction in
fluctuation of
CSS
Target &
localized drug
delivery
Avoidance of
drug degradation
Controlled release
8. Advantages
› A prolonged residence time at the site of drug action or
absorption.
› An increase in the drug concentration gradient due to the
intense contact of particle with the mucosal.
› Systemic absorption is rapid.
› Targeting & localization of the dosage form at a specific site.
› Painless administration.
› Low enzymatic activity & avoid of first pass metabolism.
› Less dosing frequency.
› Shorter treatment period.
› Increased safety margin of high potency drugs due to better
control of plasma levels.
› Improved patient convenience and compliance due to less
frequent drug administration.
9. Disadvantages
1. 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.
2. Some patient suffers unpleasant feeling.
3. Unfortunately ,the lack of standardized techniques often leads
to unclear results.
4. costly drug delivery system.
10. Different routes of mucoadhesion
Nasal delivery system.
Ocular delivery system.
Rectal delivery system.
Buccal delivery system.
Vaginal delivery system
Sublingual delivery system.
Gastrointestinal delivery system.
11. Mechanism of mucoadhesion
The mechanism responsible in the formation of mucoadhesive
bond include two stages:
1. Contact stage
2. Consolidation stage
12. Mechanism of mucoadhesion
• 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
(consolidation stage).
13. Step-I
Wetting and swelling step occurs when polymer spreads over
the surface of mucosal membrane to develop intimate contact.
Swelling of polymer occur because the components of polymer
have an affinity for water.
14. • Mucosal surface composed of high
mol. Wt polymer Glycoproteins.
• In this step the interdiffusion and
interpenetration of mucoadhesive
polymer chain and the mucosal
polymer chains occurs and they
entangles to form adhesive bonds.
• Strength of bonds depends upon the
degree of penetration of the two
polymer groups.
Step-II
15. Step-III
This step involves formation of weak
chemical bonds between the entangled
polymer chains.
Bonds includes primary bonds such as
covalent bonds and secondary
interactions such as van der Waals and
hydrogen bonds.
17. Theories mucoadhesion
Electronic theory :
• The electron transfer between the mucus and the mucoadhesive
results in the formation of a double layer of electrical charges at the
mucus and mucoadhesive interface. The net result of such a process
is the formation of attractive forces within this double layer.
18. Wetting theory :
• States that if the contact angle of liquids on the substrate surface is
lower then there is greater affinity for the liquid to the substrate
surface.
• Ability of bioadhesive polymers to spread & develop intimate contact
with the mucous membrane.
Theories mucoadhesion
19. Theories mucoadhesion
Adsorption theory :
• Adhesion occurs due to surface forces acting between the atoms
present in two different surfaces.
• Two type of chemical bonds resulting from these forces.
( primary : covalent bond, secondary: ionic bond, hydrogen bond
& van der waals forces).
20. Theories mucoadhesion
Diffusion theory :
• The polymer chains and mucus mix at a depth to creat semi-
permanant adhesive bonds.
• Penetration of polymer chains depends on diffusion coefficient
and time of contact.
• Physical entanglement of mucin strands and flexible polymer
chains.
polymer
chains
mucus
Interdiffusion
21. Theories mucoadhesion
Mechanical theory :
• Mechanical theory considers adhesion to be due to the filling of
the irregularities and microcracks on a rough surface by a
mucoadhesive liquid forming an interlocked structure.
22. Theories mucoadhesion
Cohesive theory :
• States that process of bioadhesion occurs due to
intermolecular interactions amongst like-molecules within
two different layers.
23. Penetration enhancer
Substances that facilitate the permeation through mucosa
are referred as permeation enhancers .
Safe and non toxic, non irritating and non allergenic
Pharmacologically and chemically inert.
They should have no pharmacological activity within the
body.
Eg. Benzalkonium chloride , Dextran sulfate ,Fatty acid ,
Propyleneglycol, Sodium EDTA etc.
24. Mucoadhesive polymer
They are water soluble and water insoluble polymers which are
swellable networks joined by cross linking agent.
Characteristic of ideal polymer
o Degradation products should be non toxic and non
absorbable from GIT.
o Good spreadibility, wetting, swelling and biodegradable
properties.
o Optimum molecular weight.
o Non irritant to mucous membrane.
o Form a strong non-covalent bond with mucin epithelial cell
surface.
25. Factor 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:
• Mucin turn over
• Disease state
26. Mucoadhesive dosage form
Gels & ointment
Films
Patches
Tablets
Matrix tablet
Bioadhesive
microparticles
Bioadhesive inserts
Suspensions
Gel forming liquids
27. Evaluation Tests
A) In vitro/ Ex vivo methods
• Methods determining tensile strength
• Methods determining shear stress
• Adhesion weight method
• Fluorescent probe method
• Flow channel method
• Mechanical spectroscopic method
• Filling liquid film method
• Colloidal gold staining method
• Viscometer method
• Thumb method
• Adhesion number
• Electrical conductance
• Swelling properties
• In vitro drug release studies
• Muco retentability studies
B) In Vivo methods
• Use of radioisotopes
• Use of gamma scintigraphy
• Use of pharmacoscintigraphy
• Use of electron paramagnetic
resonance
•(EPR) oximetry
28. Applications
for treatment of diseases like; hepatitis, influenza,
pertussis (whooping cough), ricin toxoid, diphtheria, birth control.
Microsphere in vaccine delivery have specific application like improved
antigenicity by adjuvant action, modulation of antigen release,
stabilization of antigen.
of leaky tumour vessels, active targeting of tumour
cells, antigens, by intravenous /intra-arterial application.
( an endovascular therapy) involves selective
arterial embolization of tumour along with local delivery of
chemotherapeutic agent.
29. Applications
various cells, cell lines, tissues and organs can be
imaged using radio labelled microspheres.
Release of and peptides over extended
period of time.
at particular site of action.
DNA plasmids and also delivery of insulin.
.
30. Questions
1. What is mucoadhesive DDS.
2. Write down the reasons behind designing of MDDS.
3. Explain the Singer nicolson model for the mucosal membrane.
4. Write down the general composition and functions of mucosal
membrane
5. Explain the theories of mucoadhesion.
6. Write down the advantages and disadvantages of MDDS.
7. Explain the mechanism of mucoadhesion.
8. Write a short note on mucoadhesive polymers.
9. Enlist the different mucoadhesive dosage forms.
10. Write down the applications of MDDS.