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