Nasal drug delivery
Upcoming SlideShare
Loading in...5
×
 

Like this? Share it with your network

Share

Nasal drug delivery

on

  • 4,709 views

 

Statistics

Views

Total Views
4,709
Views on SlideShare
4,701
Embed Views
8

Actions

Likes
4
Downloads
230
Comments
0

3 Embeds 8

http://makepharmacyyourlife.blogspot.in 5
http://makepharmacyyourlife.blogspot.com 2
http://www.makepharmacyyourlife.blogspot.in 1

Accessibility

Categories

Upload Details

Uploaded via as Microsoft PowerPoint

Usage Rights

© All Rights Reserved

Report content

Flagged as inappropriate Flag as inappropriate
Flag as inappropriate

Select your reason for flagging this presentation as inappropriate.

Cancel
  • Full Name Full Name Comment goes here.
    Are you sure you want to
    Your message goes here
    Processing…
Post Comment
Edit your comment

Nasal drug delivery Presentation Transcript

  • 1. NASAL DRUG DELIVERY SYSTEM
  • 2. Inhalation/pulmonary drug delivery system includes Metered dose inhalers Dry powder inhalers Inhalation solutions & suspensions (for nebulizers) Inhalation nasal sprays2 3/23/2011
  • 3. Historically, nasal drug delivery system has received interest since ancient times Therapy through intranasal administration has been an accepted form of treatment in the Ayurvedic system of Indian medicine.3 3/23/2011
  • 4. Merits Avoidance of hepatic first-pass metabolism. Rate of absorption comparable to IV medication. Rapid onset of pharmacological action. User-friendly, painless, non-invasive, needle- free administration mode.4 3/23/2011
  • 5. Merits...  Lower dose & hence lower side effects  Useful for both local & systemic drug delivery  For CNS drugs, better site for rapid onset of action E.g.. Inhalation anesthesia, Morphine etc.5 3/23/2011
  • 6. Limitations Once administered, rapid removal of the therapeutic agent from the site of absorption is difficult Pathologic conditions such as cold or allergies may alter significantly the nasal bioavailability6 3/23/2011
  • 7. NASAL ROUTE - medical aspects7 3/23/2011
  • 8.  The respiratory tract, which includes the  nasal mucosa  hypo pharynx  large airways &  small airways  provides a relatively large mucosal surface area of approx. 100 m2 (in normal adult) for drug absorption8 3/23/2011
  • 9. Cross-sectional view Nasal site of drug spray & absorption Pathways for nasal absorption9 3/23/2011
  • 10. Cross-sectional view a – nasal vestibule d – middle turbinate b – palate e – superior turbinate (olfactory mucosa) c – inferior turbinate f – nasopharynx10 3/23/2011
  • 11. Site of drug spray & absorption11 3/23/2011
  • 12. Pathways for nasal absorption  Absorption through the olfactory neurons - transneuronal absorption. Olfactory epithelium is considered as a portal for substances to enter CNS  Absorption through the supporting cells & the surrounding capillary bed - venous drainage  Absorption into the cerebrospinal fluid12 3/23/2011
  • 13. Transneuronal absorption Olfactory nerve – 1st cranial sensory nerve13 3/23/2011
  • 14. Nasal enzymes • Cytochrome P 450 dependent onooxygenases, Lactate dehydrogenase, Oxidoreductase, Hydrolases, Esterase, lactic dehydogenase, malic enzymes, lysosomal proteinases, steroid hydroxylases., etc. • Cytochrome P450 dependent mono oxygenases has been reported to catalyse the metabolism of xenobiotics, nasal decongestants, nocotine, cocaine, phenacetin, nitrosamine progesterone etc. • Insulin zinc free was hydrolysed slowly by leusine aminopeptidase, • PG of E series was inactivated 15 hydroxyprostaglandin dehydrogenase14 3/23/2011
  • 15. Nasal enzymes – contd., Progesterone and testosterone were metabolized by several steroid hydroxylases in the nasal mucosa of rats.15 3/23/2011
  • 16. Nasal pH • Nasal secretion of adult : 5.5-6.5 • Infants and children: 5-6.7 • It becomes alkaline in conditions such as acute rhinitis, acute sinusitis. • Lysozyme in the nasal secretion helps as antibacterial and its activity is diminished in alkaline pH16 3/23/2011
  • 17. Therapeutic class of drugs for nasal route17 3/23/2011
  • 18. Therapeutic class of drugs 1. β2 adrenergic agonists 2. Corticosteroids 3. Antiviral 4. Antibiotics 5. Antifungal 6. More recently, vaccines18 3/23/2011
  • 19. Drugs commonly administered through pulmonary route include 1. Terbutaline Sulphate - β2 adrenergic agonist 2. Salbutamol - β2 adrenergic agonist 3. Budesonide - corticosteroid 4. Ipratropium Bromide - anticholinergic 5. Sodium Chromoglycate – mast cell stabilizer19 3/23/2011
  • 20. Formulation Development20 3/23/2011
  • 21. Formulation Development Dosage form Dosage form Factors affecting drug absorption Factors affecting drug absorption Formulation considerations Formulation considerations Physiological Pharmaceutical21 3/23/2011
  • 22. Dosage forms Liquid drop Liquid spray/nebulizers Aerosol Suspension spray/nebulizers Gel Sustained release22 3/23/2011
  • 23. Drug concentration Factors affecting Vehicle of drug delivery drug absorption Mucosal contact time Degree of drug’s ionization pH of the absorption site Size of the drug molecule Relative lipid solubility23 3/23/2011
  • 24. Physiological effects - Drug metabolism in the respiratory tract & reduction of systemic effect - Protein binding - Mucociliary transport causing increased or decreased drug residence time24 3/23/2011
  • 25. Physiological effects.... - Local toxic effects of the drug E.g., edema, cell injury, or altered tissue defenses - Local or systemic effects of propellants, preservatives, or carriers25 3/23/2011
  • 26. Pharmaceutical effects - Physico-chemical properties of a drug candidate - Spray pump devices - Methods to enhance drug absorption26 3/23/2011
  • 27. 1. Effect of particle size 2. Effect of molecular size 3. Effect of solution pH 4. Effect of drug lipophilicity 5. Effect of drug concentration27 3/23/2011
  • 28. Methods to enhance nasal absorption of drugs  Structural modification  Salt or ester formation  Formulation design28 3/23/2011
  • 29. SPRAY PUMP DEVICES Unidose Bidose Multidose29 3/23/2011
  • 30. Applications Delivery of non-peptide pharmaceuticals Delivery of peptide-based pharmaceuticals Delivery of diagnostic drugs30 3/23/2011
  • 31. 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%31 3/23/2011
  • 32. Delivery of peptide-based pharmaceuticals  Peptides & proteins have a generally low oral bioavailability because of their physico- chemical instability and susceptibility to hepato- gastrointestinal first-pass elimination E.g. Insulin, Calcitonin, Pituitary hormones etc.  Nasal route is proving to be the best route for such biotechnological products32 3/23/2011
  • 33. Delivery of diagnostic drugs Diagnostic agents such as • Phenolsulfonphthalein – kidney function • Secretin – pancreatic disorders • Pentagastrin – secretory function of gastric acid33 3/23/2011
  • 34. CONCLUSION  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 drugs34 3/23/2011
  • 35.  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 effects35 3/23/2011
  • 36. Attractive for delicate molecules allowing systemic administration without significant degradation Nasal drug delivery system offers flexibility for multiple formulations ranging from nasal drop to suspension spray36 3/23/2011
  • 37. Recent activities indicate a bright prospect for site-specific delivery of biotechnological products such as Insulin & other hormones37 3/23/2011
  • 38. THANK YOU38 3/23/2011