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MUCOADHESIVE DRUG
DELIVERY SYSTEM
PRESENTED BY
MRS.KAMBLE V.H.
GUIDEDE BY
MISS.DASWADKAR S.C.
PAD.DR.D.Y.PATIL COLLEGE OF
PHARMACY AKURDI PUNE.
04/05/2016 1
CONTENTS
04/05/2016 2
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
04/05/2016 3
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%
04/05/2016 4
FUNCTIONS
04/05/2016 5
Protective
Barrier
Adhesion
Lubrication
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.
04/05/2016 6
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 ?
04/05/2016 7
THEORIES MUCOADHESION
04/05/2016 8
MECHANISMS OFMECHANISMS OF
MUCOADHESIONMUCOADHESION
STAGE -I
STAGE-II
STAGE -III
04/05/2016 9
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
04/05/2016 10
POLYMER CLASSIfICAtIOn
04/05/2016 11
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
04/05/2016 12
DIFFERENT ROUTES OF
TARGETING MDDS
04/05/2016 13
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
04/05/2016 14
MUCOADHESIVE DOSAgE fORM
Mucoadhe
sive
dosage
form
Liquid
Suspensions
Gel forming liquids
Solid
Tablets
Matrix tablet
Mucoadhesive micro
particles /microspeare
Bioadhesive inserts
Semisolid
Gels & ointment
Films
Patches
04/05/2016 15
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.
04/05/2016 16
MEtHOD Of PREPARAtIOn
04/05/2016 17
Coating material
phase
Core material phase
Phase separation
1.Complex coacervation
2.Hot melt microencapsulation
04/05/2016 18
3.Solvent evaporation method
04/05/2016 19
4.Spray drying
04/05/2016 20
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.
04/05/2016 21
METHoDS oF EValuaTion
04/05/2016 22
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
04/05/2016 23
• Other ingredient used =liquid paraffin,acetone,magnesium
sterate,methanol,DCM.
• Stirring speed =1000 rpm
• Conclusion =drug loaded Mucoadhesive microsphere are
sutaible for repaglinide.
04/05/2016 24
 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
04/05/2016 25
Material
Repaglinide
Sodium alginate
Carbapol 334
Calcium chloride
Chloroform
04/05/2016 26
Method of preparation of microsphere
Method used ionic gelation method
Stirring speed=1000rpm
Method
04/05/2016 27
 Formula
04/05/2016 28
Formulation
code
Drug Sodium
alginate
Carbapol3
34
Calcium
chloride
chloroform
F1 50
mg
1% 0.5% 15% 100 ML
• Particle size-determine by using optical microscope
04/05/2016 29
04/05/2016 30
• Particle under compound microscope
04/05/2016 31
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 .
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.
04/05/2016 33
 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
04/05/2016 34
04/05/2016 35

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MUCOADHESIVE DRUG DELIVERY SYSTEM

  • 1. MUCOADHESIVE DRUG DELIVERY SYSTEM PRESENTED BY MRS.KAMBLE V.H. GUIDEDE BY MISS.DASWADKAR S.C. PAD.DR.D.Y.PATIL COLLEGE OF PHARMACY AKURDI PUNE. 04/05/2016 1
  • 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 04/05/2016 3
  • 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% 04/05/2016 4
  • 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. 04/05/2016 6
  • 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 ? 04/05/2016 7
  • 9. MECHANISMS OFMECHANISMS OF MUCOADHESIONMUCOADHESION STAGE -I STAGE-II STAGE -III 04/05/2016 9
  • 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 04/05/2016 10
  • 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 04/05/2016 12
  • 13. DIFFERENT ROUTES OF TARGETING MDDS 04/05/2016 13
  • 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 04/05/2016 14
  • 15. MUCOADHESIVE DOSAgE fORM Mucoadhe sive dosage form Liquid Suspensions Gel forming liquids Solid Tablets Matrix tablet Mucoadhesive micro particles /microspeare Bioadhesive inserts Semisolid Gels & ointment Films Patches 04/05/2016 15
  • 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. 04/05/2016 16
  • 17. MEtHOD Of PREPARAtIOn 04/05/2016 17 Coating material phase Core material phase Phase separation 1.Complex coacervation
  • 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. 04/05/2016 21
  • 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 04/05/2016 23
  • 24. • Other ingredient used =liquid paraffin,acetone,magnesium sterate,methanol,DCM. • Stirring speed =1000 rpm • Conclusion =drug loaded Mucoadhesive microsphere are sutaible for repaglinide. 04/05/2016 24
  • 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 04/05/2016 25
  • 27. Method of preparation of microsphere Method used ionic gelation method Stirring speed=1000rpm Method 04/05/2016 27
  • 28.  Formula 04/05/2016 28 Formulation code Drug Sodium alginate Carbapol3 34 Calcium chloride chloroform F1 50 mg 1% 0.5% 15% 100 ML
  • 29. • Particle size-determine by using optical microscope 04/05/2016 29
  • 31. • Particle under compound microscope 04/05/2016 31
  • 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. 04/05/2016 33
  • 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 04/05/2016 34