NDDS TOPICS BY PROF. SHASHANK CHAURASIYA

1. 1
Prepared By: Prof. Shashank Chaurasiya
Asst. Professor
Bansal College of pharmacy, Bhopal

2. Novel drug delivery is one of the
fastest growing healthcare sectors,
with sales of drugs incorporating
novel drug delivery systems
increasing @ an annual rate of 15%
2
ABOUT

3. Oral
Inject-
able Mucosal
Trans-
dermal
Ocular
Vaginal/
Anal
Needle
Needle-
less
Nasal
Buccal
Pulmo-
nary
Active
Passive
Topical
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4. Oral 53%
Inhation 32%
Transdermal 8%
Ocular 2%
Injectable/Impl
ant 3%
Nasal 2%
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5. Nasal Drug Delivery
New Chemical Entity
$50 million
$300-600 million
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6. New Chemical
Entity
Nasal drug Delivery2 –5 years
10 –14 years
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7.  It is also a type of muco-adhesive drug delivery system.
 Intranasal Medication administration offers a truly
“Needleless” solution to drug delivery.
 Therapy through intranasal administration has been an
accepted as form of treatment in the Ayurvedic system
of Indian medicine
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8.  NASAL ENZYMES:
• Cytochrome p-450 dependent oxygenase ,
dehydrogenase , oxydoreductase ,
hydrolases, esterases, lactic dehydrogenases,
lactate
acid
malic
enzymes, lysosomal proteinases, steroid hydroxylases
etc.
 NASAL PH:
• Adult nasal secretion pH: 5.5-6.5
• Infants & children : 5-6.7.
• Lysosome in the nasal secretion helps as antibacterial &
its activity is diminished in alkaline pH.
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9. 1 A noninvasive route.
2. Hepatic first – pass metabolism is absent.
3. Rapid drug absorption.
4. Quick onset of action.
5.The bioavailability of larger drug molecules can be improved by
means of absorption enhancer or other approach.
6. Better nasal bioavailability for smaller drug molecules.
7. Drugs which can not be absorbed orally may be delivered tothe
systemic circulation through nasal drug delivery system.
8.Convenient route when compared with parenteral route for long
term therapy.
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10. 1. The absorption enhancers used to improve nasal drug delivery
system may have histological toxicity which is not yet
clearly established
2. Absorption surface area is less when compared to GIT.
3. Once the drug administered can not be removed.
4. Nasal irritation.
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14.  The olfactory mucosa (smelling area in nose) is in direct
contact with the brain and CSF.
 Medications absorbed across the olfactory mucosa directly
enter the brain.
 This area is termed the nose brain pathway and offers a
rapid, direct route for drug delivery to the brain.
Olfactory
mucosa
Highly vascular
nasal mucosa
Brain
CSF
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15. 15
• Aq route of transport.
• Slow and passive.
• Transport through lipoidal membrane
• Active transport via carrier mediated
means.
Paracellular
transport
Transcellular
transport

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Dosage form
Formulation considerations
Factors affecting drug absorption
Physiological
Pharmaceutical

18. 18
Liquid drop
Gel
Sustained release
Liquid spray/nebulizers
Aerosol
Suspension
spray/nebulizers

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Drug concentration
Mucosal contact time
pH of the absorption site
Size of the drug particle
Relative lipid solubility
Molecular weight of the drug

20. 20
1. Effect of perfusion rate
2. Effect of perfusate volume
3. Effect of solution pH
4. Effect of drug lipophilicity
5. Effect of initial drug concentration.
6. Chemical form
7. Polymorphism
8. Partition coefficient
9. Solubility and dissolution
10. Partical size

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1. Blood flow
2. Enzymatic degradation
3. Volume of administration

22. METHODS TO ENHANCE NASALABSORPTION
OF DRUGS
Structural modification
Formulation design
Salt or ester formation
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1.Improve nasal residence time
• Apply drug anteriorly
• Formulation with polymers
• Use of biodegradable microspheres
2.Enhance nasal absorption
• Increase the rate at which drug passes through nasal
absorption.

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Buffer capacity-citrate buffer
Osmolarity-sodium acid phosphate
Viscosifying agent-carbapol,cellulose
Solublizer-labrasol,surfactants
Preservatives-benzalkonium cl,parabens
Antioxidants-tocopherols,sodium metabisulphide
Humectants-glycerine,sorbitol

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Delivery of non-peptide pharmaceuticals
Delivery of diagnostic drugs
Delivery of peptide-based pharmaceuticals
Cns delivery through nasal route
Nasal vaccination

26.  Drugs with extensive pre-systemic metabolism, such as
- progesterone
- estradiol
- propranolol
- nitroglycerin
- sodium chromoglyate
can be rapidly absorbed through the nasal mucosa with a systemic
bioavailability of approximately 100% 26

27. Peptides & proteins - low oral bioavailability because of
their physico-chemical instability and susceptibility to hepato
gastrointestinal first-pass elimination
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for such
Eg. Insulin, Calcitonin, Pituitary hormones etc.
Nasal route is proving to be the best route
biotechnological products

28. Diagnostic agents such as
Phenolsulfonphthalein – kidney function
Secretin – pancreatic disorders
Pentagastrin – secretory function of gastric acid
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29. The delivery of drugs to the CNS from the nasal route may
occur via olfactory neuroepithelium
Drug delivery through nasal route into CNS has been
reported for
i. Alzheimer’s disease
ii. brain tumours
iii. epilepsy
iv. pain and sleep disorders. 29

30. Fast and extended drug absorption
Ex.- analgesics (morphine),
i. cardiovascular drugs(propranolol)
ii. hormones (levonorgestrel, progesterone)
iii. antiviral drugs
Marketed formulation- zolmitriptan and sumatriptan
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31.  Nasal mucosa is the first site of contact with inhaled antigens
and therefore, its use for
 vaccination, especially against respiratory infections,
has been extensively evaluated.
 Ex. Human efficacy of intranasal vaccines include those
against influenza A and B
 virus, proteosoma‐influenza, adenovirus‐vectored influenza,
group B meningococcal native, attenuated respiratory syncytial
virus and parainfluenza 3 virus.
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32. SPRAY PUMPDEVICES
- Bidose
- Multidose
32

33. Liquid drop
Liquid spray/nebulizers
Aerosol
Suspension
spray/nebulizers
Gel
Sustained release
33

34. Most simple and convenient systems
developed for nasal delivery.
It has been reported that nasal drops
deposit human serum albumin in the
nostrils more efficiently than nasal sprays.
 Disadvantage-lack of the dose precision .
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40. Presently in India anti-vomiting treatments are available in the
conventional form of tablet and injection which take longer
time to bring relief.
LPL becomes the first company in India to introduce an
anti-vomiting treatment in the form of a Nasal spray pump.
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Nasal gels are high-viscosity thickened solutions or
suspensions.
Advantages of a nasal gel
Reduction of post-nasal drip due to high viscosity,
Reduction of taste impact due to reduced swallowing,
Reduction of anterior leakage of the formulation,
Reduction of irritation by using soothing/emollient
excipients and target to mucosa for better absorption.

42. Mucosal Atomization Device (MAD)
 Device designed to
allow emergency
personnel to delivery
nasal medications as
an atomized spray.
 Broad 30-micron
spray ensure
excellent mucosal
coverage.
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43. Nasal mucosa is first site of contact with inhaled antigens
and, therefore, its use for vaccination, especially against
respiratory infections
Promising alternative to the classic parenteral route, because
it is able to enhance the systemic levels of specific
immunoglobulin G and nasal secretary immunoglobulinA.
Examples of human efficacy of intranasal vaccines include
those against influenza A and B virus, proteosoma influenza
e 40
Intra nasal H1N1 vaccine Nasovac by Serum Institut

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21. adrenergic agonists
2. Corticosteroids
3. Antiviral
4. Antibiotics
5. Antifungal
6. More recently, vaccines

46. An accessible alternative route for drug administration.
Provides future potential for several drugs through the development of safe
and efficacious formulations for simple, painless and long‐term therapy.
Drugs can be directly target to the brain in order to attain a good
therapeutic effect in CNS with reduced systemic side effects.
Much has been investigated and much more are to be investigated for the
recent advancement of nasal drug deliverysystem.
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47. THANK YOU…