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Naqeeba nasal drug delivery system
1.
2. ๏ In ancient time, Indian Ayurvedic system of
medicine used nasal route for administration
of drug, called โNasyaโ.
๏ It has been an accepted form of treatment in
Ayurvedic system of Indian medicine.
๏ Certain drugs are unsuitable for oral
administration.
3. ๏ Parenteral route is also an inconvenient route for
long term therapy due to the potential side
effects.
๏ Psychotropic substances and hallucinogens have
been used in the form of snuffs.
๏ Many drugs have better BA by the nasal route
than by oral route.
๏ This is attributed to a rich vasculature and a
highly permeable structure of the nasal mucosa.
4. ๏ Avoids hepatic first pass metabolism, gut wall
metabolism.
๏ Non- invasive route of administration.
๏ Convenient and easily accessible.
๏ Absorption will be faster producing rapid effect and
better BA.
๏ Drugs with poor oral bioavailability are suitable
candidates.
5. ๏ Nasal pathology
๏ Absorption enhancers used in nasal drug delivery system
may cause toxicity
๏ Nasal cavity provides smaller absorption surface area
when compared to GIT
๏ Immunological reaction
๏ Rapid mucociliary clearance
6. A - superior turbinate
B - middle turbinate
C - inferior turbinate
D - vestibule
E - nasopharynx
Dotted areas - the olfactory
region
7. ๏ Nasal passage, which runs from the nasal
vestibule, to the nasopharynx
๏ Nasopharynx depth 12-14cms
๏ Lining is ciliated, highly vascular, rich in
mucous glands and goblet cells
๏ Cilium-5ฮผm in length & 0.2 ฮผm in diameter and
moves @20beats/sec
๏ Normal pH in the range of 5.5- 6.5 and contain
a variety of enzymes.
8. 1. Nasal vestibule and Ostium
2. Nasal turbinates
3. Mucus and cilia
4. Olfactory region
9. ๏ The rate of diffusion and rate of clearance from the
nasal cavity is influenced by:
1. The physicochemical properties of the
formulation vehicle.
2. The particle size.
3. Surface charge of a drug.
4. Any additives incorporated.
10. 1. Effect of molecular size:
Nasal absorption decreases for drugs with molecular
weight > 1000 dalton.
2. Effect of perfusion rate:
Eg: Phenobarbitol
As the perfusion rate increases, nasal absorption first
increases and then reaches a plateau level,
independent of the rate of perfusion.
11. 3. Effect of solution pH:
The effect of the pH of a perfusion solution on nasal
absorption was examined using a water soluble
ionisable compound such as benzoic acid in the pH
range 2 - 7.1
4. Effect of drug concentration:
Eg: Monitoring the disappearance of 1-tyrosyl 1-
tyrosine and the formation of 1-tyrosine.
The nasal absorption of 1-tyrosine depends upon its
concentration.
12. ๏ This was investigated using SS-6, an octapeptide
and horseradish peroxidase, a protein molecule.
๏ Two mechanisms of transport are involved:
1. Transcellular โ Across the cell
2. Paracellular โ Between the cell
13. ๏ Aqueous route of transport
๏ This route is slow and passive
๏ There is an inverse correlation between intranasal
absorption and the molecular weight of water-soluble
compounds
๏ Good systemic BA can be achieved for molecules with
a molecular wt of up to 1000 daltons with enhancer
14. ๏ Transport through a lipoidal route
๏ Responsible for the transport of lipophilic drugs
that show a rate dependency on their lipophilicity.
๏ Drug also cross cell membranes by an active
transport route via carrier-mediated means or
through the opening of tight junctions.
Eg: Chitosan
15. ๏ Enhancement in Absorption:
To modify the physicochemical properties of a drug.
๏ Salt or ester formation:
Has better trans-nasal permeability
๏ Formulation design:
Proper selection of formulation excipients could enhance the nasal
absorption of drugs.
๏ Surfactants:
Incorporation of surfactants could modify the permeability of nasal
mucosa.
17. ๏ Operates by mechanical actuation.
๏ Delivers a predetermined volume with precision
Eg: Corticosteroids, Tramazoline and nasal decongestant.
๏ They have also been explored as the NDDS for the
systemically โactive drugs
18. ๏ Used for the delivery of insulin
๏ Produces a drug absorption that is more
effective and less irritating than liquid forms.
๏ In the nasal cavity, the powder absorbs nasal
fluid and becomes swollen
19. ๏ For the mucoadhesive powder spray,
The powder mixture was prepared with HPC and
was administered by a special applicator called
โPulizerโ.
๏ The advantages of using HPC:
1) drug dose may be reduced.
2) side effects may be lowered.
3) longer duration of effect is expected.
20. ๏ They do not give reproducible dosing.
๏ They deposit at their impaction site, in the
anterior, unciliated regions of the nasal cavity.
๏ Thus leads to slow transport of the moiety along
the surface.
21. ๏ Rely upon the instillation of one or more drops
of drug solution into the nasal cavity.
๏ Nasal drops if administered correctly, deposit
drug throughout the nasal cavity
๏ Clearance of the drops is faster than spray
22. 1) In vivo nasal absorption model
2) Ex vivo nasal perfusion model.
1) In-vivo nasal absorption model:
Animal models used are:
a)Rat model
b)Rabbit model
c)Dog model
d)Sheep model
e)Monkey model.
23. ๏ An incision is made in the neck and the trachea is
cannulated.
๏ Another tube is inserted through the esophagus
towards the posterior part of the nasal cavity.
๏ Drug solution is delivered to the nasal cavity.
๏ Blood samples are collected from the femoral vein
๏ Gives an idea of the drug absorbed through the
nasal mucosa.
24. ๏ A funnel is provided underneath the nose to lead
the drug solution into the drug reservoir.
๏ Reservoir solution is circulated through the
nasal cavity of the rat.
๏ Perfusion solution passes out from the nostril
and flows into the drug reservoir soln again.
25.
26. ๏ Novel drug delivery system- By Yie.W.Chein,
Page no-229-265.
๏ Targeted and controlled drug delivery systems-
By S.P.Vyas and R.K.Khar, Page no-315-382.
๏ Drug Delivery Systems by Kewal K. Jain,
Pg 9-10.