Transcript Nasal Drug Delivery in EMS

A SEMINAR ON
INTRA-NASAL DRUG
DELIVERY SYSTEM
BY:
NALEEN RAJ BHANDARI
B-PHARM (2/4)
MAHESHWARA
INSTITUTE OF PHARMACY
CONTENTS
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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
bioavailability
Various 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:
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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:
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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:
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Particle size 10-50 microns adheres best to the nasal
mucosa.
MECHANISMS
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Two mechanisms are found to be involved:
Fast rate mechanism, which is lipophilicity dependent.
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Slow rate mechanism, which is dependent on molecular
weight.
Ex: Nasal delivery of insulin, manitol follows a transport
mechanism involving passive diffusion
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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
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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 Pharmaceuticals
e.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
TRADITIONAL & KURVE’S
DELIVERY
MUCOSAL
AUTOMIZATION
DEVICE (M.A.D)
EXAMPLES
Accuspray from BD
Medical–
Pharmaceutical
Systems is a singleuse nasal sprayer
for monodose or
bidose administration
INTRANASAL Naloxone
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)