MUCOADHESIVE DRUG DELIVERY SYSTEM

PRESENTED BY MRS.KAMBLE V.H.

GUIDEDE BYMISS.DASWADKAR S.C.

PAD.DR.D.Y.PATIL COLLEGE OF PHARMACY AKURDI PUNE.

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Contents

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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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What is mucus ?DIMENSIONThickness varies from 40 μm to 300 μmGeneral composition of mucus•Water…………………………………..95%•Glycoprotein and lipids……………..0.5-5%•Mineral salts……………………………1%•Free proteins…………………………..0.5-1%

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Functions

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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.

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Avoidance of

First pass Metabolism

Better absorption of peptide by

penetration enhancer

Prolong

residence time

Localization of drug at given site

WHY ?

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Theories Mucoadhesion

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MECHANISMS OF MECHANISMS OF MUCOADHESIONMUCOADHESION

STAGE -I

STAGE-II

STAGE -III

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MUCOADHESIVE POLYMER They are water soluble and water insoluble polymers which are

swellable networks joined by cross linking agentCHARACTERISTIC 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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Polymer classification

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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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DIFFERENT ROUTES OF TARGETING MDDS

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Prolongation of residence of drug in GIT.Targeting & localization of the dosage form at a specific sitePainless 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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Mucoadhesive dosage form

Mucoadhesive

dosage form

LiquidSuspensionsGel forming liquids

SolidTabletsMatrix tabletMucoadhesive micro particles /microspeare Bioadhesive inserts

SemisolidGels & ointmentFilmsPatches

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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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Method of preparation

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Coating material phase

Core material phase

Phase separation

1.Complex coacervation

2.Hot melt microencapsulation

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3.Solvent evaporation method

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4.Spray drying

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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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METHODS OF EVALUATION

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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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• 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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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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Material Repaglinide

Sodium alginate

Carbapol 334

Calcium chloride

Chloroform

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Method of preparation of microsphere Method used ionic gelation method Stirring speed=1000rpmMethod

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Formula

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Formulation code

Drug Sodium alginate

Carbapol334

Calcium chloride

chloroform

F1 50 mg

1% 0.5% 15% 100 ML

• Particle size-determine by using optical microscope

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• Particle under compound microscope

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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 .

ReferencesGarg 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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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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