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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)