Naleen Bhandari, Intranasal medication delivery overview.ppt

7/27/2019 Naleen Bhandari, Intranasal medication delivery overview.ppt

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INTRA-NASAL DRUGDELIVERY SYSTEM

A SEMINAR ON

BY:

NALEEN RAJ BHANDARIB-PHARM (2/4)MAHESHWARAINSTITUTE OF PHARMACY


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CONTENTS

INTRODUCTION

ADVANTAGES

FUNDAMENTAL FACTORS MECHANISMS AND PATHWAYS

DELIVERY SYSTEMS

ENHANCEMENT IN ABSORPTION

APPLICATIONS

EXAMPLES

CONCLUSIONS

REFERENCES


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INTRODUCTION

In ancient times the Indian Ayurvedic system of

medicines used nasal route for administration of drug

and the process is called as Nasya

It has been used for local effects extensively in

decongestant and local activity. But, in recent times

intranasal drug delivery is being considered as apreferred route of drug delivery for systemic

bioavailability

Various proteins & peptides have shown a good

bioavailability


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Intranasal Drug Delivery

System: Advantages Its easy and convenient

Can be easily administered to the unconscious patients

Compared to oral medications, intranasal medicationdelivery results in:

Faster delivery to the blood stream and higher blood levels

No destruction by stomach acid and intestinal enzymes

No destruction by hepatic first pass metabolism

Compared to IV medications, intranasal medication

delivery results in:

Comparable blood levels depending on the drug and dose.


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Fundamental Factors Affecting

Nasal Absorption Molecular weight: Absorption of drugs decreases as the

molecular weight of drug molecules increases. Mc Martin et

al reported a sharp decline in drug absorption havingmolecular weight greater than 1000Dalton

Lipophilicity

Drug concentration: Absorption increases as

concentration of drug increases. 1-tyrosine shows increasedabsorption at high concentration in rate..

Particle size:

Particle size 10-50 microns adheres best to the nasal

mucosa.


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MECHANISMS

Two mechanisms are found to be involved:

Fast rate mechanism, which is lipophilicity dependent.

Slow rate mechanism, which is dependent on molecular

weight.

Ex: Nasal delivery ofinsulin, manitol follows a transport

mechanism involving passive diffusion

While, absorption of water soluble molecules like sodium

cromoglycate take place by diffussion through aqueous

pores


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PATHWAYS

Possible drug absorption pathways


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DELIVERY SYSTEMS

Various delivery systems are used like

Nasal spray

Nose drops

Aerosol spray

Metered dose nebulizer

Saturated cotton pledget

The insufflators

Mucosal atomizer device (M.A.D)

Microspheres


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ENHANCEMENT IN

ABSORPTION Use of absorption enhancers

Increase in residence time

Administration of drugs in the form of microspheres

Various enhancers used

Surfactants

Phospholipids

Chelaters

Glycols

Cyclodextrins

Capable of increasing membrane fluidity and leaching of

proteins and lipids from the membrane


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Applications of Intranasal DrugDelivery

Nasal Delivery of Organic based Pharmaceuticals

e.g.: Progesterone, Estradiol, Testosterone, Hydralzine,

Propranolal, Cocain, Naloxon & Nitrogylcerine. These haveshown good Bioavailabilityby this route.

Water-soluble organic based compounds such as Sodium

cromoglycate were also found to be well absorbed.

Nasal Delivery of Peptide-Based Drugs As peptide based drugs are susceptible to hepatogastrointestinal

first pass elimination & instability, they show very low oral

bioavailability thus administered through nasal route.


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EXAMPLES SHOWING DIFFERENT

DELIVERY SYSTEMS

MUCOSAL

AUTOMIZATION

DEVICE (M.A.D)TRADITIONAL & KURVES

DELIVERY


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EXAMPLES

INTRANASAL Naloxone

Accuspray from BDMedicalPharmaceuticalSystems is a single-use nasal sprayer

for monodose orbidose administration


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Conclusions NDDS provides route of drug administration for drugs,

which degrade due to first pass metabolism

Though it also poses many chal lenges such as low

absorption, toxicological problems, high dose

requi rements etc.,, thus use of absorption enhancers is

proving to be useful increasing the absorption.

I nsulin is being extensively investigated for its nasal

absorption, which may prove a major turnaround in

diabetics treatment.

With ongoing efforts to improve bioavailabil i ty of protein

and peptide drug through nasal route, the nasal route can

become the prime route for administration of proteindru s..


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REFERENCES

Shaji J and Marathe S.W.

NASAL DRUG DEL IVERY SYSTEM :OPPORTUNI TIES & CHALLENGES

INDIAN DRUGS Vol. 45 No. 5

May 2008 Pg no (345353)

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Naleen Bhandari, Intranasal medication delivery overview.ppt