Novel Approaches For

Mucoadhesive Gel A
Review

By
Mina Mahdi Ahmed
Hiba Hussein Athab
Supervised By
Lecturer. Hiba Sabah Sabry
 Outlines
Introduction MUCOADHESION THEORIES

Gel MUCOADHESIVE POLYMERS

IDEAL PROPERTIES OF TOPICAL GEL FACTORS AFFECTING MUCOADHESION POLYMERS

ADVANTAGES AND DISADVANTAGES OF GEL FORMULATIONS Classification of polymers

MUCUS Examples of commonly used bioadhesive polymers

Composition of Mucus Layer Types of Mocoadhesive

MUCOADHESION APPROACHES FOR MUCOADHESIVE GELS

Mechanisms of Mucoadhesion
Conclusion
 Introduction
 Drug delivery involves administering pharmaceutical
compounds to achieve therapeutic effects while ensuring that
the medication selectively reaches its target site without
affecting non-target cells or tissues. Various drug delivery
systems have been developed for treating human diseases,
such as liposomes, proliposomes, microspheres, gels,
prodrugs, cyclodextrins, and nanoparticles.
 Topical preparations are favored for their reduced side effects,
ease of application, non-invasive nature, and painlessness
compared to other administration routes
 Gel

Typical gels are homogeneous and semi-solid

preparations utilized for treating and preventing skin
conditions.
Gels have a hydrophilic nature, allowing for quick
release of the medicine or active component.
The structural network of gels is created using both
organic macromolecules and inorganic particles.
IDEAL PROPERTIES OF TOPICAL GEL

The gel The gel

The gel
should The gel should not The gel It should
should interact
be clear should be should have anti-
be inert with any
and non- other be microbial
in sticky. activity.
homoge formulation
stable.
nature. component.
nous.
ADVANTAGES AND DISADVANTAGES OF
GEL FORMULATIONS
DISADVANTAGES
ADVANTAGES

 Compared to other formulations,  poor permeability across the skin.

gels are simple to manufacture.  Gels have possibility of allergenic reaction.
 Gel is elegant non-greasy  temperature, humidity, and other
formulation. environmental factors may effect the
 Gels have excellent adherence
rheology of the formulation .
property to application site.
 Gels are biocompatible and eco-  gelling agents may undergo precipitation
friendly. which results in the salting-out effect.
 Have magnificent tolerability to  drying of the gels occur due to the solvent
stress conditions. evaporation.
 MUCUS
 Mucus is a slippery secretion that covers and is produced by mucous
membranes.

 Water (95%)
 Glycoprotein and lipids (0.5-0.3%)
 Mineral salts (1%)
 Free protein (0.5-1%)

Functions of Mucus Layer:

 Protective
 Barrier
 Lubrication
 MUCOADHESION

Mucoadhesion refers to the ability of certain materials to adhere

to mucosal surfaces, such as those found in the gastrointestinal
tract, respiratory tract, or other mucous membranes in the body.

Importance of Mucoadhesive Drug Delivery

 Mucoadhesive drug delivery systems offer several advantages:
 Enhanced drug residence time at the target site
 Improved drug absorption due to prolonged contact with mucosal surfaces
 Reduced dosing frequency and improved patient compliance
 Potential for localized drug delivery to specific sites
 Mechanisms of Mucoadhesion
The mechanism of mucoadhesion is generally divided into
two stage: the contact stage and the consolidation stage.
 MUCOADHESION THEORIES

 Wetting Theory
 Diffusion Theory
 Fracture Theory
 Electronic Theory
 Adsorption Theory
 Mechanical Theory
 MUCOADHESIVE POLYMERS

Polymers play a crucial role in these systems by

enhancing the residence time of the active agent at the
desired. These polymers can be categorized as water-
soluble or water-insoluble.
 MUCOADHESIVE POLYMERS

 Characteristics of an ideal mucoadhesive polymer

 Nontoxic and Non-absorbable
 Nonirritant to Mucous Membranes
 Facilitates Drug Incorporation and Release
 Storage Stability
 Cost-Effectiveness
FACTORS AFFECTING MUCOADHESION POLYMERS

Molecular Spatial
Chain length Flexibility
weight arrangement

Hydrogen Polymer
Hydration of
bonding concentration
polymer

Charge and
degree of
ionization of
polymer
 Classification of polymers
 Anionic polymers are favored for mucoadhesive applications due to
strong hydrogen bonding with mucin, but they can precipitate with
multivalent cations, reducing adhesion. Their swelling and adhesive
properties are pH-dependent.
 Cationic polymers like chitosan interact well with mucosal surfaces due
to ionic attractions with anionic groups on the membranes. Chitosan is
particularly notable for its low cost and permeation-enhancing
properties.
 Non-ionic polymers adhere via polymer chain interpenetration with
mucin, though they are generally less adhesive than anionic and cationic
polymers and are not pH-dependent.
 Classification of polymers

 Amphoteric polymers, possessing both anionic and

cationic properties, like gelatin and N-
carboxymethylchitosan, are used but may exhibit lower
adhesion due to self-neutralization.
 Thiolated polymers, containing free thiol groups that
form disulfide bonds with mucin cysteine-rich
subdomains, enhance mucoadhesion, exemplified by
poly(acrylic acid) and chitosan.
Examples of commonly used bioadhesive polymers

 1- Carbopol/carbomer (Cp): is a synthetic polymer with a high

molecular weight, soluble in water, alcohol, and glycerine, with a pH
range of 2.5 to 3 in a 1% aqueous solution. It serves as a thickening,
emulsifying, and gelling agent, capable of undergoing gelation
triggered by pH
 2- Chitosan (CS): a natural copolymer derived from crustacean shells,
exhibits good biocompatibility and mucoadhesive properties through
hydrogen bonding and electrostatic interactions. Sodium alginate
 3- Sodium alginate (Na Alg.): extracted from brown seaweed, forms
viscous solutions in water with a pH of 7.2 in a 1% aqueous solution.
Hydroxy propyl methylcellulose
Examples of commonly used bioadhesive polymers

 4- Hydroxy propyl methylcellulose (HPMC): a hydrophilic mucoadhesive polymer,

is soluble in cold water, insoluble in alcohol, ether, and chloroform, contributing to
prolonged drug residence time. Boronate-containing copolymers
 5- Boronate-containing copolymers (BCCs): are water-soluble mucoadhesive
polymers forming insoluble complexes with mucin, offering potential for targeted
drug delivery to tumor cells. Sodium carboxymethyl cellulose
 6-Sodium carboxymethyl cellulose (Na CMC): a commercial derivative of
cellulose, enhances mucoadhesive properties in various formulations. Poly Vinyl
Alcohol
 7- poly vinyl alcohol (PVA): finds applications in water-soluble films and is
classified into partially hydrolyzed and fully hydrolyzed categories with diverse
industrial uses.
 Types of Mocoadhesive

Gels &
Tablets Films patches
Ointment
 Types of Mocoadhesive
 Gels and Ointment: Semisolid dosage forms like gels
and ointments offer advantages in easy dispersion
throughout the oral mucosa, although dosing accuracy
may not be as precise as with tablets, patches, or films.
Poor retention of gels at application sites can be
addressed with mucoadhesive formulations. For
example Lidocaine
APPROACHES FOR MUCOADHESIVE GELS

Niosomal Gel
M i cr o pe ns i o n
emuls s
ion Nanosu l
Gel Ge
Mucoadhesive

r e s Nan
s pe opa
r o l r
i
M G
c e Gel ticle
Liposomal Gel
 EVALUATION OF MUCOADHESIVE GEL

Tests measuring Mucoadhesive Strength

Determination of Shear Strength
Thumb test
Falling Liquid Film Method
Particle size measurement
 Conclusion
 Microparticulate mucoadhesive systems are beneficial because they
provide protection to therapeutic substances and enhance absorption
by increasing contact time through mucoadhesion.
 Microparticulate systems and mucoadhesive drug delivery systems use
various approaches to improve drug bioavailability.
 Development of liposomal, microemulsion, microspheres, and
nanoparticle mucoadhesive drug delivery systems aims to enhance
bioavailability of poorly absorbed drugs by prolonging residence time
and facilitating intimate contact with absorption membranes.
 These systems can also reduce the frequency of dosing, leading to
increased patient compliance with the treatment regimen.
Thanks for listening