2. Novel Drug Delivery System
Nasal Drug Delivery System
Medical aspects
Formulation Development
Applications
Conclusion
CONTENTS
2
3. 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%
3
4. By 2010, the US drug
delivery market alone will
be worth $30 billion
4
5. Why Novel Drug
Delivery system?
To optimize drug’s therapeutic
effect, convenience and dose
To enhance a product’s life-cycle
To improve `patient compliance
To target drug delivery
To control overall healthcare costs
To facilitate biological drug delivery
5
9. Inhalation/pulmonary drug delivery system includes
Metered dose inhalers
Dry powder inhalers
Inhalation nasal sprays
Inhalation solutions & suspensions (for nebulizers)
9
10. Nasal Drug Delivery System
&
Opportunity
Annual market growth
Merits
Limitations
10
11. Annual growth of
locally acting
products
Annual growth of
systemically acting
products
11%
30%
11
12. Lower dose & hence lower side effects
Merits...
For CNS drugs, better site for rapid onset of
action
Eg. Inhalation anesthesia, Morphine etc.
Useful for both local & systemic drug delivery
12
13. Limitations
Pathologic conditions such as cold or allergies
may alter significantly the nasal bioavailability
Once administered, rapid removal of the
therapeutic agent from the site of absorption is
difficult
13
15. The respiratory tract, which includes the
nasal mucosa
hypopharynx
large airways &
small airways
provides a relatively large mucosal surface
area of approx. 100 m2 (in normal adult)
for drug absorption
15
DRUG DELIVERY TO RESPIRATORY SYSTEM
17. Cross-sectional view
17
a – nasal vestibule d – middle turbinate
b – palate e – superior turbinate (olfactory mucosa)
c – inferior turbinate f – nasopharynx
19. Pathways for nasal absorption
Absorption into the cerebrospinal fluid
Absorption through the supporting cells & the
surrounding capillary bed
- venous drainage
19
29. Physiological effects
- Drug metabolism in the respiratory tract &
reduction of systemic effect
- Local toxic effects of the drug
Eg., edema, cell injury, or altered tissue defenses
Local or systemic effects of propellants, preservatives,
or carriers
29
31. 1. Effect of particle size
2. Effect of molecular size
3. Effect of solution pH
5. Effect of drug concentration
4. Effect of drug lipophilicity
31
32. 1. Effect of particle size
(aerodynamic size distribution)
- Large particles (> 7 microns) will be lost in the
gastrointestinal tract
- Intermediate particles (3 to 7 microns) reach the
actual site of action
- Small particles (< 3 microns) will be lost in exhaled
breathe
32
33. 2. Effect of molecular size
- Higher the molecular size, lower the nasal absorption
Absorption enhancers:
Polyacrylic acid
Sodium Glycocholate
Sodium Deoxycholate
Polysorbate 80 etc.
33
34. 3. Effect of solution pH
- Nasal absorption is pH dependent
- Absorption is higher at a pH lower than the
dissociation constant (pKa) of the molecule.
34
35. 4. Effect of drug lipophilicity
-
- Lipid soluble drugs are absorbed more rapidly
than water soluble drugs
5. Effect of drug concentration
- Absorption depends on the initial concentration of
the drug
35
36. Methods to enhance nasal absorption of drugs
Structural modification
Formulation design
Salt or ester formation
36
41. 1. Delivery of non-peptide pharmaceuticals
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%
41
42. 2. Delivery of peptide-based pharmaceuticals
Eg. Insulin, Calcitonin, Pituitary hormones etc.
Nasal route is proving to be the best route for
such biotechnological products
3. Delivery of
diagnostic drugs
Diagnostic agents such as
• Phenolsulfonphthalein – kidney function
42
44. Nasal route is a part of drug delivery
strategy that is emerging to be a fastest
growing drug delivery system with an
annual growth of
11% for locally acting drugs
&
30% for systemically acting drugs
44
45. Nasal drug delivery offers such benefits as
Rapid onset of action with lower dose &
minimal side effects
Has an advantage of site-specific delivery
with improved therapeutic effects
45
