MPharm pharmaceutics ppt nasal drug deliery system

2.  In ancient time, Indian Ayurvedic system of
medicine used nasal route for administration
of drug, called “Nasya”.
 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-5μm in length & 0.2 μm 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 – Across the cell
2. Paracellular – 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.

16. 1. Metered dose nebulizer
2. Mucoadhesive powder sprays
3. Sustained release formulations
4. Nasal sprays
5. Nasal drops
6. The saturated cotton pledget
7. The insufflator

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 –active 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
‘Pulizer’.
 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.

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.