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Guided By :-
Dr. Vaishali Kilor
Presented By :-
Shubham Kamble
GURUNANAK COLLEGE OF PHARMACY 1
CONTENT
✔ Introduction
✓ Anatomy of Nasal Cavity
✓ Mechanism of Drug Absorption
✓ Advantages & Limitations
✓ Preparation/Formulation Consideration
✓Types/Dosage Forms
✓ Evaluation
✓ Applications
GURUNANAK COLLEGE OF PHARMACY 2
INTRODUCTION
✓ Nasal Drug Delivery System is administration of drug through Nasal route.
✓ Nasal mucosa has been considered as a potential route of administration to achieve faster & higher level
of drug absorption.
 Ideal & non-invasive alternative to the parenteral route for systemic drug delivery; since it offers a truly
"Needleless" drug delivery.
 This route has been a convenient and reliable route.
 Several new formulations are used to deliver drugs to the brain by olfactory, neuronal, and trigeminal
pathways.
GURUNANAK COLLEGE OF PHARMACY 3
ANATOMY OF NASAL CAVITY
✓ It is divided into 2 halves big nasal septum.
 It contains 3 regions:
a) Nasal vestibule
b) Olfactory region
c) Respiratory region
Nasal cavity is covered with mucous membrane which contains goblet cells that secrets mucous.
GURUNANAK COLLEGE OF PHARMACY 4
NOSE BRAIN PATHWAY
The olfactory mucosa (smelling area in nose) is in direct contact with the brain & CSF.
✓ Medications absorbed across the olfactory mucosa directly enter the brain.
✓ This is termed as nose brain pathway which offers a rapid, direct route for drug delivery to the brain.
GURUNANAK COLLEGE OF PHARMACY 5
GURUNANAK COLLEGE OF PHARMACY 6
NOSE BRAIN PATHWAY.
 Another way of drug absorption is through Trigeminal
Nerve Pathway with the help of Pons.
✓ Besides the direct nose-to-brain pathways, there are other
routes for the drugs to penetrate the brain.
✓ Such as from the respiratory route, drug can be
transported partially to the circulation & reach the brain by
the "nose-to-blood-to- brain" pathway.
GURUNANAK COLLEGE OF PHARMACY 7
GURUNANAK COLLEGE OF PHARMACY 8
MECHANISM OF DRUG ABSORPTION
 The 1st step in absorption is passage of absorbed drug through the mucus layer.
 2 mechanisms have been primarily used-
1) PARACELLULAR TRANSPORT
 Aqueous Route of Transport
 Slow and Passive
2) TRANSCELLULAR TRANSPORT
 Transport through lipoidal membrane
 Active transport via carrier mediated means
GURUNANAK COLLEGE OF PHARMACY 9
GURUNANAK COLLEGE OF PHARMACY 10
GURUNANAK COLLEGE OF PHARMACY 11
VARIOUS APPROACHES:
1. Prodrug Approach:
The absorption of peptides like angiotensin II, Bradykinin, Vasopressin, and Calcitonin is improved when
prepared into enamine derivatives.
2. Structural Modification:
Chemical modification of Salmon Calcitonin to elcatonin (C-N bond replaces the S-S bond) showed
better bioavailability.
3. Particulate drug Delivery:
1. Microspheres, Nanoparticles, and Liposomes.
2. Nasal Enzyme Inhibitors.
 Peptides and Proteases.
 Trippin Aprotinin, Borovaline, Amastatin, Betaststin, and Boroleucin inhibitors.
GURUNANAK COLLEGE OF PHARMACY 12
The Components of the Nasal Formulations:
 Drug component :- Turbutaline sulphate ,Budesonide, ipratropium bromide, Sod. Chromoglycate
 Viscosifying Agents – Hydroxypropyl cellulose.
 Solubilizers – Glycol, Alcohol, Cyclodextrins.
 Surfactants – SLS, Polyacrylic acid.
 Bio-adhesive Polymers – Methylcellulose, Carboxymethylcellulose.
 Preservatives – Parabens, Benzalkonium chloride.
 Antioxidants – Sodium metabisulphite.
GURUNANAK COLLEGE OF PHARMACY 13
GURUNANAK COLLEGE OF PHARMACY 14
GURUNANAK COLLEGE OF PHARMACY 15
Nasal Gels Nasal Drops Nasal Sprays
Nasal Ointments Nasal Powder
GURUNANAK COLLEGE OF PHARMACY 16
RECENT ADVANCES IN INTRANASAL DRUG DELIVERY
Desmopressin Insulin Nasal Spray Antivomiting Nasal Spray
Influenza Vaccine (Nasal use only)
Nasal Vaccine (Covid 19)
GURUNANAK COLLEGE OF PHARMACY 17
IN VITRO NASAL PERMEATION STUDIES (DIFFUSION):
The nasal diffusion cell is fabricated in glass.
The lid has 3 opening, each for
1.Sampling,
2.Thermometer, and
3.Donor tube chamber.
1. The nasal mucosa of sheep was separated & stoned in distilled water containing few drops at gentamycin
injection.
2. Mucosal surface is attached to donor chamber tube.
3. The donor chamber tube is placed such a way that it just touches the diffusion medium in recipient chamber.
4. At predetermined intervals, samples (0.5 ml) from recipient chamber are with draw and transferred to amber
colored ampoules.
5. The samples are estimated for drug content by suitable analytical technique.
GURUNANAK COLLEGE OF PHARMACY 18
1. The rat is anaesthetized.
2. An incision is made in the neck and the trachea is cannulated with a
polyethylene tube.
3. Another tube is inserted through the oesophagus towards the posterior
region of the nasal cavity..
4. The drug solution is delivered to the nasal cavity through the nostril or
through the cannulation tubing.
5. The blood samples are collected from the femoral vein.
The rat Model
GURUNANAK COLLEGE OF PHARMACY 19
1. The rabbit is anaesthetized by an intramuscular injection of
a combination of ketamine and xylazine.
2. The rabbit's head is held in an upright position and the drug
solution is administered by nasal spray into each nostril.
3. During the experiment the body temperature of the rabbit is
maintained at 37°C with the help of a heating pad.
4. The blood samples are collected by an catheter in the
marginal ear vein or artery.
The Rabbit Model
GURUNANAK COLLEGE OF PHARMACY 20
GURUNANAK COLLEGE OF PHARMACY 21
GURUNANAK COLLEGE OF PHARMACY 22

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Inta nasal Drug Delivery System.pptx

  • 1. Guided By :- Dr. Vaishali Kilor Presented By :- Shubham Kamble GURUNANAK COLLEGE OF PHARMACY 1
  • 2. CONTENT ✔ Introduction ✓ Anatomy of Nasal Cavity ✓ Mechanism of Drug Absorption ✓ Advantages & Limitations ✓ Preparation/Formulation Consideration ✓Types/Dosage Forms ✓ Evaluation ✓ Applications GURUNANAK COLLEGE OF PHARMACY 2
  • 3. INTRODUCTION ✓ Nasal Drug Delivery System is administration of drug through Nasal route. ✓ Nasal mucosa has been considered as a potential route of administration to achieve faster & higher level of drug absorption.  Ideal & non-invasive alternative to the parenteral route for systemic drug delivery; since it offers a truly "Needleless" drug delivery.  This route has been a convenient and reliable route.  Several new formulations are used to deliver drugs to the brain by olfactory, neuronal, and trigeminal pathways. GURUNANAK COLLEGE OF PHARMACY 3
  • 4. ANATOMY OF NASAL CAVITY ✓ It is divided into 2 halves big nasal septum.  It contains 3 regions: a) Nasal vestibule b) Olfactory region c) Respiratory region Nasal cavity is covered with mucous membrane which contains goblet cells that secrets mucous. GURUNANAK COLLEGE OF PHARMACY 4
  • 5. NOSE BRAIN PATHWAY The olfactory mucosa (smelling area in nose) is in direct contact with the brain & CSF. ✓ Medications absorbed across the olfactory mucosa directly enter the brain. ✓ This is termed as nose brain pathway which offers a rapid, direct route for drug delivery to the brain. GURUNANAK COLLEGE OF PHARMACY 5
  • 6. GURUNANAK COLLEGE OF PHARMACY 6
  • 7. NOSE BRAIN PATHWAY.  Another way of drug absorption is through Trigeminal Nerve Pathway with the help of Pons. ✓ Besides the direct nose-to-brain pathways, there are other routes for the drugs to penetrate the brain. ✓ Such as from the respiratory route, drug can be transported partially to the circulation & reach the brain by the "nose-to-blood-to- brain" pathway. GURUNANAK COLLEGE OF PHARMACY 7
  • 8. GURUNANAK COLLEGE OF PHARMACY 8
  • 9. MECHANISM OF DRUG ABSORPTION  The 1st step in absorption is passage of absorbed drug through the mucus layer.  2 mechanisms have been primarily used- 1) PARACELLULAR TRANSPORT  Aqueous Route of Transport  Slow and Passive 2) TRANSCELLULAR TRANSPORT  Transport through lipoidal membrane  Active transport via carrier mediated means GURUNANAK COLLEGE OF PHARMACY 9
  • 10. GURUNANAK COLLEGE OF PHARMACY 10
  • 11. GURUNANAK COLLEGE OF PHARMACY 11
  • 12. VARIOUS APPROACHES: 1. Prodrug Approach: The absorption of peptides like angiotensin II, Bradykinin, Vasopressin, and Calcitonin is improved when prepared into enamine derivatives. 2. Structural Modification: Chemical modification of Salmon Calcitonin to elcatonin (C-N bond replaces the S-S bond) showed better bioavailability. 3. Particulate drug Delivery: 1. Microspheres, Nanoparticles, and Liposomes. 2. Nasal Enzyme Inhibitors.  Peptides and Proteases.  Trippin Aprotinin, Borovaline, Amastatin, Betaststin, and Boroleucin inhibitors. GURUNANAK COLLEGE OF PHARMACY 12
  • 13. The Components of the Nasal Formulations:  Drug component :- Turbutaline sulphate ,Budesonide, ipratropium bromide, Sod. Chromoglycate  Viscosifying Agents – Hydroxypropyl cellulose.  Solubilizers – Glycol, Alcohol, Cyclodextrins.  Surfactants – SLS, Polyacrylic acid.  Bio-adhesive Polymers – Methylcellulose, Carboxymethylcellulose.  Preservatives – Parabens, Benzalkonium chloride.  Antioxidants – Sodium metabisulphite. GURUNANAK COLLEGE OF PHARMACY 13
  • 14. GURUNANAK COLLEGE OF PHARMACY 14
  • 15. GURUNANAK COLLEGE OF PHARMACY 15
  • 16. Nasal Gels Nasal Drops Nasal Sprays Nasal Ointments Nasal Powder GURUNANAK COLLEGE OF PHARMACY 16
  • 17. RECENT ADVANCES IN INTRANASAL DRUG DELIVERY Desmopressin Insulin Nasal Spray Antivomiting Nasal Spray Influenza Vaccine (Nasal use only) Nasal Vaccine (Covid 19) GURUNANAK COLLEGE OF PHARMACY 17
  • 18. IN VITRO NASAL PERMEATION STUDIES (DIFFUSION): The nasal diffusion cell is fabricated in glass. The lid has 3 opening, each for 1.Sampling, 2.Thermometer, and 3.Donor tube chamber. 1. The nasal mucosa of sheep was separated & stoned in distilled water containing few drops at gentamycin injection. 2. Mucosal surface is attached to donor chamber tube. 3. The donor chamber tube is placed such a way that it just touches the diffusion medium in recipient chamber. 4. At predetermined intervals, samples (0.5 ml) from recipient chamber are with draw and transferred to amber colored ampoules. 5. The samples are estimated for drug content by suitable analytical technique. GURUNANAK COLLEGE OF PHARMACY 18
  • 19. 1. The rat is anaesthetized. 2. An incision is made in the neck and the trachea is cannulated with a polyethylene tube. 3. Another tube is inserted through the oesophagus towards the posterior region of the nasal cavity.. 4. The drug solution is delivered to the nasal cavity through the nostril or through the cannulation tubing. 5. The blood samples are collected from the femoral vein. The rat Model GURUNANAK COLLEGE OF PHARMACY 19
  • 20. 1. The rabbit is anaesthetized by an intramuscular injection of a combination of ketamine and xylazine. 2. The rabbit's head is held in an upright position and the drug solution is administered by nasal spray into each nostril. 3. During the experiment the body temperature of the rabbit is maintained at 37°C with the help of a heating pad. 4. The blood samples are collected by an catheter in the marginal ear vein or artery. The Rabbit Model GURUNANAK COLLEGE OF PHARMACY 20
  • 21. GURUNANAK COLLEGE OF PHARMACY 21
  • 22. GURUNANAK COLLEGE OF PHARMACY 22