nasal drop

1. NASAL DRUG
DELIVERY
SYSTEM
Pr e s e n t e d B y : Al e x a J a c o b
2 n d
M . Ph a r m S e m
D e p t . O f Ph a r m a c e u t i c s
S t . J o s e p h ’s C o l l e g e O f Ph a r m a c y, c h e r t h a l a
Al a p p u z h a , k e r a l a 1

2. CONTENTS
• DEFINITION
• ADVANTAGES
• DISADVANTAGES
• FORMULATION
• NASAL DRUG DELIVERY DOSAGE FORMS
• EVALUATION
• REFERENCE
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3. DEFINITION
Nasal administration is a route of administration in which
the drugs are insufflated through the nose for either local
or systemic effect.
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4. ADVANTAGES
• Drug degradation that is observed in the gastrointestinal tract is absent.
• Hepatic first pass metabolism is avoided.
• Rapid drug absorption and quick onset of action can be achieved.
• The bioavailability of larger drug molecules can be improved by means of absorption
enhancer or other approach.
• The nasal bioavailability for smaller drug molecules is good.
• Drugs that are orally not absorbed can be delivered to the systemic circulation by nasal drug
delivery.
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5. DISADVANTAGES
• Nasal administration is primarily suitable only for potent drugs.
• Drugs for continuous & frequent administration may be less suitable because of harmful
long term effects.
• Nasal administration has also been associated with a high variability in the amount of drug
absorbed.
• The histological toxicity of absorption enhancers used in nasal drug delivery system is not yet
clearly established.
• Relatively inconvenient to patients when compared to oral delivery systems since there is a
possibility of nasal irritation & nasal cavity provides smaller absorption surface area whe5n
compared to GIT.

6. FORMULATION
1) BUFFERS :
Isotonic potassium phosphate buffer
Citrate buffer
Acetate buffer
2) OSMOTIC AGENTS :
Sodium chloride
Sodium sulphite
Sodium acid phosphate
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7. 3) GELLING / VISCOSIFYING AGENTS :
Carbopol
Cellulose agents
Starch
Dextran
Chitosan
4) SOLUBILIZERS :
Glycols
Small quantities of alcohol
Transcutol ( Diethylene glycol monoethyl ether)
Medium chain glycerides
Surfactants
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8. 5) PRESERVATIVES :
Parabens
Benzalkonium chloride
Phenyl ethyl alcohol
Benzoyl alcohol
6) ANTI-OXIDANTS :
Sodium metabisulphite
Sodium bisulphite
Butylated hydroxytoluene
Tocopherol
7) HUMECTANTS :
Glycerine
Sorbitol
Mannitol
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9. 8) ABSORPTION ENHANCERS :
(a) Surfactants
Sodium glycocholate
Sodium deoxycholate
(b) Chitosan
(c) Cyclodextrins
Hydroxypropyl-ß-cyclodextrin
Dimethyl-ß-cyclodextrin
(d) Complexing agents
EDTA
Citric acid
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10. (e) Fatty acid salts
Oleic acid
Caprylic acid
Lauric acid
(f) Phospholipids
L-α- lysophosphatidyl choline
(g) Fusidates
Sodium taurodihydrofusidate
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11. NASAL DRUG DELIVERY DOSAGE FORMS
A. LIQUID NASAL FORMULATIONS
• Liquid preparations are the most widely used dosage forms for nasal
administration of drugs.
• They are mainly based on aqueous state formulations.
• Their humidifying effect is convenient and useful, since many allergic and
chronic diseases are often connected with crusts and drying of mucous
membranes.
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12. 1) INSTILLATION & RHINYLE CATHETER :
• Catheters are used to deliver the drops to a specified region of nasal cavity
easily.
• Place the formulation in the tube and kept tube one end was positioned in
the nose, and the solution was delivered into the nasal cavity by blowing
through the other end by mouth
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13. 2) COMPRESSED AIR NEBULIZERS :
• Nebulizer is a device used to administer medication in the form of a mist
inhaled into the lungs.
• The compressed air is filling into the device, so it is called compressed air
nebulizers.
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14. 3) SQUEEZED NASAL BOTTLE :
• Squeezed nasal bottles are mainly used as delivery device for
• They include a smooth plastic bottle with a simple jet outlet.
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15. 4) METERED-DOSE PUMP SPRAYS :
• Most of the pharmaceutical nasal preparations on the market containing
solutions, emulsions or suspensions are delivered by metered-dose pump
sprays.
• Nasal sprays, or nasal mists, are used for the nasal delivery of a drug or
either locally to generally alleviate cold or allergy symptoms such as nasal
congestion.
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16. B. POWDER DOSAGE FORMS
• Dry powders are less frequently used in nasal drug delivery.
• Powder dosage form may be devoleped if solution & suspension dosage
form cannot be devoleped. Eg: due to lack of drug stability
• Major advantages of this dosage form are the lack of preservatives and the
improved stability of the formulation.
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17. 1) INSUFFLATORS :
• Insufflators are the devices to deliver the drug substance for inhalation.
• It can be constructed by using a straw or tube which contains the drug
substance and sometimes it contains syringe also.
• The achieved particle size of these systems is often increased compared to the
particle size of the powder particles due to insufficient deaggregation of the
particles and results in a high coefficient of variation for initial deposition17
areas.

18. 2) DRY POWDER INHALER :
• Dry powder inhalers (DPIs) are devices through which a dry powder
formulation of an active drug is delivered for local or systemic effect via the
pulmonary route.
• These are commonly used to treat respiratory diseases such as asthma,
bronchitis, emphysema an
d COPD.
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19. C. PRESSURIZED METERED DOSE INHALERS
• A metered-dose inhaler (MDI) is a device that delivers a specific amount of
medication to the lungs, in the form of a short burst of aerosolized medicine
that is inhaled by the patient.
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20. D. NASAL GELS
• Nasal gels are high-viscosity thickened solutions or suspensions.
• The advantages of a nasal gel include the reduction of post-nasal drip due
high viscosity, reduction of taste impact due to reduced swallowing,
of anterior leakage of the formulation,reduction of irritation by using
soothing/emollient excipients and target delivery to mucosa for better
absorption.
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21. E. NASAL VACCINES
• Nasal mucosa is the first site of contact with inhaled antigens and therefore ,
it is used for respiratory infections.
• Nasal vaccination is a promising alternative to the parentral route , because
is able to enhance the systemic levels of specific immunoglobulin G & nasal
secretary immunoglobulin A.
Eg : Nasal vaccines against influenza A & B Virus
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22. EVALUATION
A. IN-VITRO NASAL DIFFUSION STUDIES :
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23. B. IN-VIVO NASAL ABSORPTION MODELS :
1) RA
T MODEL
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24. 2) RABBIT MODEL :
• Rabbit is anaesthetized by intramuscular injection of a combination of
ketamine and xylazine.
• The rabbit's head is held in an upright position and the drug solution is
administered by nasal spray into each nostril.
• The blood samples are collected by an indwelling catheter in the marginal ear
vein.
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25. 3) DOG MODEL :
• The dog is anaesthetized by intravenous injection of sodium thiopental and
the anesthesia is maintained with sodium Phenobarbital.
• A positive pressure pump through a cuffed endotracheal tube gives the
ventilation.
• The blood sampling is carried out from the jugular vein.
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26. 4) SHEEP MODEL :
• Sheep model for studying nasal drug delivery is prepared using basically the
same procedure as that described for dog model.
• Male in-house bred sheep are employed since they are free from nasal
infections.
• Practical and suitable for investigating nasal delivery formulations. 26

27. 5) MONKEY MODEL :
• The monkey is tranquillized by intramuscular injection of ketamine
hydrochloride or anaesthetized by intravenous injection of sodium
Phenobarbital.
• The head of the monkey is held in an upright position and the drug solution
is administered into each nostril.
• The blood samples are collected through an indwelling catheter in the vein.
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28. C. EX-VIVO NASAL PERFUSION MODEL :
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29. REFERENCE
• Controlled & Novel Drug delivery by N.K Jain ; Pg no : 235-267
• Textbook of industrial Pharmacy by Shobha Rani R Hiremath ; Pg no : 60-71
• https:/www.slideshare.net.in
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