INTRA-NASAL DRUG DELIVERY SYSTEM A SEMINAR ON BY: NALEEN RAJ BHANDARI B-PHARM (2/4) MAHESHWARA INSTITUTE OF PHARMACY.

INTRA-NASAL DRUG DELIVERY SYSTEM

A SEMINAR ON

BY:NALEEN RAJ BHANDARIB-PHARM (2/4)MAHESHWARA INSTITUTE OF PHARMACY

CONTENTS

INTRODUCTION ADVANTAGES FUNDAMENTAL FACTORS MECHANISMS AND PATHWAYS DELIVERY SYSTEMS ENHANCEMENT IN ABSORPTION APPLICATIONS EXAMPLES CONCLUSIONS REFERENCES

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 a preferred route of drug delivery for systemic bioavailabilityVarious proteins & peptides have shown a good bioavailability

Intranasal Drug Delivery System: Advantages

Its easy and convenient Can be easily administered to the unconscious patients

Compared to oral medications, intranasal medication delivery 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.

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 having molecular weight greater than 1000Dalton

Lipophilicity Drug concentration: Absorption increases as

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

Particle size: Particle size 10-50 microns adheres best to the nasal

mucosa.

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 of insulin, manitol follows a transport mechanism involving passive diffusion

While, absorption of water soluble molecules like sodium cromoglycate take place by diffussion through aqueous pores

PATHWAYS

Possible drug absorption pathways

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

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

Applications of Intranasal Drug Delivery

Nasal Delivery of Organic based Pharmaceuticalse.g.: Progesterone, Estradiol, Testosterone, Hydralzine,

Propranolal, Cocain, Naloxon & Nitrogylcerine. These have shown good Bioavailability by 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.

EXAMPLES SHOWING DIFFERENT DELIVERY SYSTEMS

MUCOSAL AUTOMIZATION DEVICE (M.A.D)

TRADITIONAL & KURVE’S DELIVERY

EXAMPLES

INTRANASAL Naloxone

Accuspray from BD Medical–Pharmaceutical Systems is a single-use nasal sprayer for monodose or bidose administration 

Conclusions NDDS provides route of drug administration for drugs,

which degrade due to first pass metabolism Though it also poses many challenges such as low

absorption, toxicological problems, high dose requirements etc.,, thus use of absorption enhancers is proving to be useful increasing the absorption.

Insulin is being extensively investigated for its nasal absorption, which may prove a major turnaround in diabetic’s treatment.

With ongoing efforts to improve bioavailability of protein and peptide drug through nasal route, the nasal route can become the prime route for administration of protein drugs..

REFERENCES

Shaji J and Marathe S.W.

NASAL DRUG DELIVERY SYSTEM: OPPORTUNITIES & CHALLENGES

INDIAN DRUGS Vol. 45 No. 5

May 2008 Pg no (345 – 353)