Mucosal Drug Delivery System
Mucosal Drug Delivery System
Mucosal Drug Delivery System
SYSTEM
SUBMITTED TO PRESENTED BY
V.B. POKHARKAR DEBJANI BAIDYA
HOD OF PHARMACEUTICS M.PHARM(2ND SEM)
INDEX
INTRODUCTION
BIOLOGICAL MEMBRANE
STAGES
MECHANISM
THEORIES
BIOADHESIVE POLYMERS
RESEARCH ARTICLE
REFERENCES
INTRODUCTION
ALL BIOLOGICAL MEMBRANES ARE COVERED WITH THICK GEL LIKE STRUCTURE KNOWN AS
MUCIN.
IT POSSESSES CONSIDERABLE BINDING PROPERTIES.
MUCUS IS A NETWORK OF MUCIN GLYCOPROTEINS.
AT PHYSIOLOGICAL PH IT HAS NEGATIVE CHARGE DUE TO THE PRESENCE OF SIALIC
ACID(PKA_-2.6)
HIGHLY HYDRATED
CROSS LINKED
LINEAR AND FLEXIBLE
THICKNESS VARY FROM 50-450 MICROMETRE TO 1 MICROMETRE.
STAGES INVOLVED IN BIOADHESION:
CONTACT STAGE: the contact between the mucoadhesive and the mucous membrane,
with spreading and swelling of the formulation, initiating its deep contact with the
mucus layer
CONSOLIDATION STAGE: the mucoadhesive materials are activated by the presence of
moisture. Moisture plasticizes the system, allowing the mucoadhesive molecules to
break free and to link up by weak van der Waals and hydrogen bonds
MECHANISM
The mechanisms responsible in the formation of bioadhesive bonds are not
fully known, however most research has described bioadhesive bond
formation as a three step process:-
STEP1: Wetting and swelling of polymer
The vagina is the lower part of the female reproductive tract. It is a muscular tube lined with mucous
membrane which is covered with a layer of stratified squamous epithelium with an underlying layer of
connective tissue (lamina propria) .
Vaginal Mucoadhesive Formulations:
The intravaginal route has been used to deliver contraceptives as well as anti-infective agents such as
antifungal drugs to exert a local effect
Agents targeted for the vaginal route have been formulated into various dosage forms including creams,
gels and vaginal tablets.
Bioadhesive polymers are incorporated into vaginal formulations to aid the adhering of the dosage form to
its target site
Rectal Mucoadhesive Formulation :
Examples of Products
Anacal Is a rectal ointment used to relieve the symptoms associated with hemorrhoids. It contains the
bioadhesive agent polyethylene high polymer 1500.
Germoloids Is a rectal ointment used to relief the pain, swelling, itchiness and irritation associated with
hemorrhoids. It contains the polymer propylene glycol.
Bioadhesive Polymer
Characteristic of Bioadhesive polymer:
Flexibility- The flexibility of bioadhesive polymers is important because it controls the
extent of the interpenetration between the polymers and mucosal/epithelial surfaces.
Hydrophilicity Polymers that are hydrophilic in nature are able to form strong
adhesive bonds with mucosal membranes because the mucus layer contains large amounts
of water.
Hydrogen bonding Hydrogen bonding between the entangled polymer chains forms
strong adhesive bonds, therefore the presence of hydrogen bond forming groups such as
OH and COOH groups are vital in large quantities.
High molecular weight Polymers with a high molecular weight are desirable because
they provide more available bonding sites.
Degree of cross linking- it influences chain mobility and resistance to dissolution
Long chain polymers-chain length must be long enough to promote the
interpenetration and it should not be too long that diffusion becomes a problem
Concentration of the polymer-an optimum concentration is required to promote
the muco adhesive strength. It depends however, on the dosage form.
Charge and degree of ionization-mucoadhesive strength can be attributed as
anion>cation>non-ionic
Optimum hydration- excessive hydration leads to decreased mucoadhesive
strength due to formation of a slippery mucilage.
Synthetic:
I) Biodegradable polymers
A) Polyesters: Polylactic acid, Polyglycolic acid, Polyhydroxyl butyrate,
Polycaprolactone, Poly Doxanones
B) Polyanhydride: Polyadipic acid,Polyterphthalicacid,Polysebacic acid and Various
copolymers
C) Polyamides: Poly iminocarbonates, Poly amino acids.
D) Phosphorous Based polymers: Polyphosphates, Polyphosphonates,
Polyphosphazenes.
E) Others: Poly cyanoacrylates, Poly urethanes, Poly ortho esters, Polyacetals.
II) Non biodegradable polymers
A)Cellulose derivatives: Carboxymethylcellulose, Ethyl cellulose, Cellulose acetate
HPMC.
B) Silicones: Polydimethyl siloxanes, Colloidal silica, Polymethacrylates
C) Others: PVP, EVA, Poloxamines
Thiolated Polymers*
Derived from hydrophilic polymers such as chitosan
Thiol groups allows the formation of covalent bonds with cysteine-rich sub domains of
the mucus gel layer, leading to increased residence time and improved bioavailability
THE PREPARED PATCHES WERE SMOOTH, UNIFORM IN THICKNESS, MASS AND DRUG CONTENT. PATCHES
SHOWED NO VISIBLE CRACKS OR FOLDS.
THE THICKNESS OF THE MEDICATED PATCHES RANGED BETWEEN 0.23 0.008 AND 0.59 0.007 MM AND
THE MASS VARIED BETWEEN 65.23 3.3 AND 117.92 4.2 MG,
PATCHES WITH PEG-400 AS A PLASTICIZER SHOWED INCREASED MASS
THIS OBSERVATION COULD BE CORRELATED TO THE HIGH MOLECULAR WEIGHT OF PEG-400 WHEN COMPARED
TO PG
THE SURFACE PH OF THE PATCHES RANGED BETWEEN 6 AND 7 AND NO MUCOSAL IRRITATION WAS EXPECTED.
PATCHES SHOWED FAVOURABLE DRUG LOADING WHICH VARIED BETWEEN 9.0 0.3 AND 10.05 0.82
MG/2 CM2 PATCHES (I.E. DRUG LOADING EFFICACY OF 90100%).
ALL THE PATCHES HAD SATISFACTORY FOLDING ENDURANCE OF >240. FORMULATIONS E7, E12, F7 AND F12
SHOWED HIGH FOLDING ENDURANCE OF OVER 300, AND HENCE WERE SELECTED FOR FURTHER EVALUATION
AND CHARACTERIZATION.
Swelling behaviour of selected SS patches. Values
presented as mean SD, n = 3.
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