3. WHAT IS MUCUS ?
Inner layers called mucosa Covered with viscoelastic fluid. This
fluid Secreted by Goblet cells and it composed of water and
mucin.
Other components include proteins, lipids and
mucopolysaccharides ,electrolytes
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4. WHAT IS MUCUS ?
DIMENSION
Thickness varies from 40 μm to 300 μm
General composition of mucus
•Water…………………………………..95%
•Glycoprotein and lipids……………..0.5-5%
•Mineral salts……………………………1%
•Free proteins…………………………..0.5-1%
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6. 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.
Hydrophilic high mol. wt. such as peptides that cannot be
administered & poor absorption ,then MDDS is best choice.
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7. Avoidance
of
First pass
Metabolism
Avoidance
of
First pass
Metabolism
Better absorption
of peptide by
penetration enhancer
Better absorption
of peptide by
penetration enhancer
Prolong
residence time
Prolong
residence time
Localization
of drug at
given site
Localization
of drug at
given site
WHY ?
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10. MUCOADHESIVE POLYMER
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 biodegradable
properties
Optimum molecular weight
Non irritant to mucous membrane
Form a strong non-covalent bond with mucin epithelial cell
surface
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12. 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
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14. 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
Advantages
Drug , which irritate the oral mucosa ,have a bitter or unpleasant
taste ,odor cannot be administer by this rout.
Some patient suffers unpleasant feeling.
Costly drug delivery system.
Disadvantages
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16. MUCOADHESIVE MICROSPHERES
A controlled release system designed to increase its
residence time in the stomach with contact with the mucosa was
achieved through the preparation of Mucoadhesive
microspheres
Microspheres are small spherical particles (typically 1 μm to
1000 μm), sometimes referred to as micro particles. The
microspheres can be made up of either natural or synthetic
polymers.
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21. Drug loaDing
DRUG LOADING IN MICROSPHERE
The drugs are loaded in the microspheres principally using two
methods i.e. during the preparation of the microsphere or after
the preparation of the microsphere
The loading of drug after the preparation of microspheres may
be achieved by incubating them with high concentration of the
drug in a suitable solvent.
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23. CaSE STuDY
• Design and evaluation of Mucoadhesive microspheres of
repaglinide for oral controlled release by Vimal K. Yadav, Brajesh
Kumar, S.K. Prajapati , Kausar shafaat
• They devlope,characterize and evaluate Mucoadhesive
microspheres of repaglinide employing Mucoadhesive polymer
for prolonged GIT absorption.
• Method used=Solvent evaporation method
• Polymer used =Eudragit RS-100 and chitosan
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24. • Other ingredient used =liquid paraffin,acetone,magnesium
sterate,methanol,DCM.
• Stirring speed =1000 rpm
• Conclusion =drug loaded Mucoadhesive microsphere are
sutaible for repaglinide.
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25. Sustained release dosage form is essential for diabetic patient
which marked by continues therapy along with high margin of
safety, patient compliance and fulfil economical feature.
PROBLEM WITH REPAGLINIDE
Its have very short biological half life
Low bioavailability about 50%
Poor absorption in upper intestinal tract
So it is indicated for the development of dosage form with
increase gastric residence time
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32. 04/05/2016 32
Sr no Particle size in micrometre
1 35.47
2 38.9
3 27.2
4 41.23
5 43.42
6 47.51
SURFACE MORPHOLOGY
Particle is rough irregular shape most of circular shape.
FURTHER STUDY
To prepare various formulation of mucoadhesive microsphre and select best formulation .
33. RefeRences
Garg Ankita , Upadhyay Prashant ,Mucoadhesive microspheres: a
short review ,Published by Asian Journal of Pharmaceutical and
Clinical Research, Vol 5, Suppl 3, 2012, ISSN - 0974-2441.
Tangri Pranshu , Mucoadhesive drug delivery: mechanism and
methods of evaluation, Published by International Journal of
Pharma and Bio Sciences,Vol-2/Issue-1/Jan-March-2011,ISSN
0975-6299
Flávia Chiva Carvalho , Marcos Luciano Bruschi et al ,
Mucoadhesive drug delivery systems, Published by Brazilian
Journal of Pharmaceutical Sciences, vol. 46, n. 1, jan./mar., 2010.
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34. Yadav Vimal K.,Kumar Brajesh,Prajapati S.K.,shafaat Kausar,
Design and evaluation of Mucoadhesive microspheres of
repaglinide for oral controlled release,Published by
International Journal of Drug Delivery 3 (2011) 357-370, ISSN:
0975-021.
Nazir Imran, Bashir Sajid et al, Development and Evaluation of
Sustained Release Microspheres of Repaglinide for
Management of Type 2 Diabetes Mellitus,Published By,
Journal of Pharmacy and Alternative Medicine, Vol 1, 2012,
ISSN 2222-4807
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