This document provides an overview of intra nasal drug delivery systems. It discusses the anatomy of the nasal cavity, mechanisms of drug absorption such as paracellular and transcellular transport, and factors that affect drug absorption like biological, physiological and formulation related factors. It also describes the advantages and limitations of the nasal route. Various dosage forms for nasal delivery including drops, sprays, gels and powders are mentioned. Evaluation methods like in-vitro and in-vivo studies are summarized. Finally, applications of the nasal route for delivery of peptides, vaccines and CNS drugs are highlighted.
Computational modelling of drug disposition lalitajoshi9
computational modelling of drug disposition is the integral part of computer aided drug design. different kinds of tools being used in the prediction of drug disposition in human body. This topic in the CADD explains the details about the drug disposition, active transporters and tools.
Biopharmaceutic considerations in drug product design and In Vitro Drug Produ...PRAJAKTASAWANT33
Introduction, biopharmaceutic factors affecting drug bioavailability, rate–limiting steps in drug absorption, physicochemical nature of the drug formulation factors affecting drug product performance
Introduction
Anatomy and physiology of lungs
Advantage and disadvantage of Pulmonary Drug Delivery system.
Aerosols , propellants & container types.
Current technologies for pulmonary drug delivery.
New technologies for pulmonary drug delivery.
Evaluation of Pharmaceutical Aerosols & PDDS.
Pulmonary drug delivery is primarily used to treat conditions of the airways, delivering locally acting drugs directly to their site of action.
Delivery of anti-asthmatic and other locally acting drugs directly to their site of action reduces the dose needed to produce a pharmacological effect, while the low concentrations in the systemic circulation may also reduce side-effects.
The drugs which are administered by pulmonary route are not only for lungs delivery but it goes to systemic circulation and produce the effect where it is desired through out the body. For Eg. A product containing ergotamine tartrate is available as an aerosolized dosage inhaler for the treatment of migraine & Volatile anesthetics, including, halothane, are also given via the pulmonary route.
Used for inhalation and topical aerosols .
Manufactured by impact extrusion process.
Light in weight, less fragile, Less incompatibility due to its seamless nature.
Greater resistance to corrosion .
Pure water and pure ethanol cause corrosion to Al containers.
Added resistance can be obtained by coating inside of the container with organic coating like phenolic , vinyl or epoxy and polyamide resins.
Computational modelling of drug disposition lalitajoshi9
computational modelling of drug disposition is the integral part of computer aided drug design. different kinds of tools being used in the prediction of drug disposition in human body. This topic in the CADD explains the details about the drug disposition, active transporters and tools.
Biopharmaceutic considerations in drug product design and In Vitro Drug Produ...PRAJAKTASAWANT33
Introduction, biopharmaceutic factors affecting drug bioavailability, rate–limiting steps in drug absorption, physicochemical nature of the drug formulation factors affecting drug product performance
Introduction
Anatomy and physiology of lungs
Advantage and disadvantage of Pulmonary Drug Delivery system.
Aerosols , propellants & container types.
Current technologies for pulmonary drug delivery.
New technologies for pulmonary drug delivery.
Evaluation of Pharmaceutical Aerosols & PDDS.
Pulmonary drug delivery is primarily used to treat conditions of the airways, delivering locally acting drugs directly to their site of action.
Delivery of anti-asthmatic and other locally acting drugs directly to their site of action reduces the dose needed to produce a pharmacological effect, while the low concentrations in the systemic circulation may also reduce side-effects.
The drugs which are administered by pulmonary route are not only for lungs delivery but it goes to systemic circulation and produce the effect where it is desired through out the body. For Eg. A product containing ergotamine tartrate is available as an aerosolized dosage inhaler for the treatment of migraine & Volatile anesthetics, including, halothane, are also given via the pulmonary route.
Used for inhalation and topical aerosols .
Manufactured by impact extrusion process.
Light in weight, less fragile, Less incompatibility due to its seamless nature.
Greater resistance to corrosion .
Pure water and pure ethanol cause corrosion to Al containers.
Added resistance can be obtained by coating inside of the container with organic coating like phenolic , vinyl or epoxy and polyamide resins.
Myself Omkar Tipugade , M- Pharm ,Sem - II, Department of pharmaceutics , from Shree Santkrupa College Of Pharmacy , ghogaon . Today I upload presentation on Active Transport like P-gp , BCPR, Nucleoside transporters etc .
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Quality- by- design (QbD) is a concept introduces by the International Conference on Harmonization (ICH) Q8 guidelines.
Myself Omkar Tipugade , M- Pharm ,Sem - II, Department of pharmaceutics , from Shree Santkrupa College Of Pharmacy , ghogaon . Today I upload presentation on Active Transport like P-gp , BCPR, Nucleoside transporters etc .
REGULATORY AND INDUSTRY VIEWS ON QbD, SCIENTIFICALLY BASED QbD- EXAMPLES OF A...Ardra Krishna
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QbD has been adopted by U.S Food and Drug Administration (FDA) for the discovery, development and manufacture of drugs.
Quality- by- design (QbD) is a concept introduces by the International Conference on Harmonization (ICH) Q8 guidelines.
In ancient time Ayurvedic system of medicine used nasal route for administration of drugs and the process is called as “Nasya”.
Nasal route has been used for local effects of decongestants but, in recent time it is being considered as a preferred route of drug delivery for systemic bioavailability.
Various proteins & peptides have shown a good bioavailability through this route.
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.
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.
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.
Nasopulmonary drug delivery system: Introduction to Nasal and Pulmonary routes of drug delivery, Formulation of Inhalers (dry powder and metered dose), nasal sprays, nebulizers
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New development in herbals,
Bio-prospecting tools for drug discovery,
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1. INTRA NASAL ROUTE
DELIVERY SYSTEMS
Presented by:
Ms. Bhandari Kartiki M.
M. Pharm- Pharmaceutics
(1st year)
1
2. 2
CONTENT
Introduction
Anatomy of Nasal Cavity
Mechanism of Drug Absorption
Factors Affecting Drug Absorption
Advantages & Limitations
Preparation / Formulation Consideration
Types / Dosage Forms
Evaluation
Applications
References
3. 3
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.
INTRODUCTION
4. ANATOMY OF NASAL CAVITY
4
It is divided into 2 halves by 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.
5. NOSE BRAIN PATHWAY
5
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.
7. 7
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.
NOSE BRAIN PATHWAY
8. MECHANISM OF DRUG ABSORPTION
8
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 & passive.
2) Transcellular Transport:
Transport through lipoidal membrane.
Active transport via carrier mediated
means.
9. FACTORS AFFECTING DRUG ABSORPTION
9
i. Biochemical
(Enzymatic inhibition)
ii. Structural features
i. Muco-ciliary clearance (MCC)
ii. Nasal secretion
iii. pH of nasal cavity
iv. Blood flow
v. Pathology
2) Physiological factors:
1) Biological factors:
10. FACTORS AFFECTING DRUG ABSORPTION
10
i. Molecular weight
ii. Particle size
iii. pKa & partition coefficient
iv. Solubility
v. Lipophilicity
i. Dosage form
ii. Contact time & drug concentration
iii. Osmolarity
iv. Viscosity
4) Formulation related factors:
3) Drug related factors:
11. ADVANTAGES & LIMITATIONS
11
ADVANTAGES LIMITATIONS
Non-invasive, Rapid drug
absorption with quick onset of
action.
Risk of local side effects &
irreversible damage of the cilia on
the nasal mucosa.
Hepatic 1st pass metabolism is
absent.
Absorption surface area is less as
compared to GIT.
Better nasal bioavailability for
smaller drug molecules.
Once the drug administered can not
be removed.
Convenient route for long term
Nasal irritation.
12. 12
ADVANTAGES LIMITATIONS
Bioavailability of larger molecules
can be improved by using
absorption enhancer or other
approaches.
The absorption enhancers used to
improve nasal drug delivery may
have histological toxicity which is
not yet clearly established.
Orally non-absorbable drugs may
be delivered to systemic circulation
through nasal route.
ADVANTAGES & LIMITATIONS
13. PREPARATION / FORMULATION CONSIDERATION
13
Drugs:
Commonly used drugs are-
i. β2-adrenergic agonist: terbutaline sulphate.
ii. Corticosteroids : budesonide.
iii. Anti cholinergic: ipratropium bromide.
iv. Mast cell stabilizer : sod. cromoglycate.
Viscosity Modifier:
Increases the viscosity of the solution prolonging the therapeutic
activity of preparation. e.g.: hydroxypropyl cellulose, starch.
14. 14
Solubilizers:
Aqueous solubility of drug always a limitation for nasal drug delivery.
e.g.: glycol, alcohol, labrasol, transcutol.
In such cases surfactants or cyclodextrins (HP-β-cyclodextrin) are
used, these serve as a biocompatible solubilizer & stabilizer in
combination with lipophilic absorption enhancers.
Surfactants:
Modify the permeability of nasal mucosa & facilitate the nasal
absorption of drugs. e.g.: SLS, Poly acrylic acid, sod. glycocholate.
PREPARATION / FORMULATION CONSIDERATION
15. 15
Buffers:
To maintain pH of the formulation between 4.5-7. e.g.: acetate buffer,
citrate buffer, pot. phosphate buffer.
Tonicity modifier:
Hypertonic solution causes shrinkage of the cell & inhibit loss of drug via
muco ciliary clearance (MCC). E.g.: NaCl, sod. sulfite, sod. acid phosphate.
Humectant:
To prevent drying of nasal cavity & irritation by antioxidants or
permeation enhancers. e.g.: glycerin, sorbitol, mannitol.
PREPARATION / FORMULATION CONSIDERATION
17. 17
TYPES / DOSAGE FORMS
Nasal Drops:
Simplest & convenient
systems.
Disadvantage- lack of
dose precision.
Nasal Spray:
Solution / suspension
forms.
Deliver an exact dose
from 25 - 200 μm.
Nasal Gel:
High viscosity solution
/ suspension.
Reduce post-nasal drip,
irritation, taste impact.
18. 18
TYPES / DOSAGE FORMS
Mucosal Atomization
Device (MAD):
Emergency nasal delivery
as an atomized spray.
Broad 30μm spray ensure
great mucosal coverage.
Nasal Powder:
Drugs unstable in solution
/ suspension form.
Local application, absence
of preservatives, stable.
Nasal Strips:
For breathing problems &
snoring.
It pulls out the nostrils &
increases air flow to nasal
cavity.
19. TYPES / DOSAGE FORMS (RECENT ADVANCES)
19
Desmopressin
Nasal Insulin
Spray (Sun
Pharma)
Anti-
vomiting
Nasal Spray
(Lincoln
Pharma)
Nasal Spray Flu Vaccines for
Influenza
Another recent e.g.: SaNOtize’s
Nasal Spray for Covid-19.
20. EVALUTION
20
Glass
fabricate
d nasal
diffusion
cell with
3
openings:
sampling,
thermom
eter, & a
donor
tube
chamber
Nasal
mucosa
of sheep:
stoned in
distilled
water +
sample
drug
Mucosal
surface
attached
to donor
chamber
tube that
touches
the
diffusion
medium
in
recipient
chamber
At
specific
intervals,
samples
withdraw
n from
recipient
chamber
&
transferr
ed to
amber
colored
ampoules
Drug
content is
estimate
d by
suitable
analytical
techniqu
e.
In-Vitro Nasal Permeation Studies (Diffusion):
21. 21
In-Vivo Nasal Absorption Studies (Animal model):
Rat Model:
Anaesthetized rat & Incision made at
neck
Tube inserted through esophagus
towards posterior of nasal cavity
Drug solution delivered to nasal cavity
through nostril / cannulation tubing
Blood samples collected from femoral
vein.
Rabbit Model:
Rabbit anaesthetized by ketamine +
xylazine IM inj.
Head held upright & drug administered
by nasal spray into each nostril
Rabbit’s body temp. maintained at 37°C
with heating pad
Blood samples collected by catheter
from marginal ear vein / artery.
22. APPLICATIONS
22
Delivery of peptide-based & non-peptide pharmaceuticals:
Peptide-based pharmaceuticals E.g.: Insulin, Calcitonin, Pituitary hormones.
Non-peptide pharmaceuticals E.g.: Adrenal corticosteroids, Sex hormone, Vit B.
Delivery of diagnostic drugs:
E.g.: Secretin, Pentagastrin.
CNS delivery through nasal route: (Nose-Brain Pathway)
E.g.: Parkinson’s disease, Alzheimer's disease or Pain associated to brain injury.
Nasal vaccination:
E.g.: FluMist (LAIV) Influenza vaccine.
23. 23
REFERENCES
1. Vyas TK, Shahiwala A, Marathe S, Misra A. Intranasal drug delivery for brain
targeting. Current drug delivery. 2005 Apr 1;2(2):165-75.
2. Appasaheb PS, Manohar SD, Bhanudas SR, Anjaneri N. A review on intranasal
drug delivery system. Journal of Advanced Pharmacy Education & Research
Oct-Dec. 2013 Oct;3(4).
3. Chien Y W. Nasal Drug Delivery & Delivery System. In James Swarbrick. Novel
Drug Delivery System. 2nd ed. New York, Informa Healthcare, 2009; 229-266.
4. Baviskar DT, Jain D. Nasal Drug Delivery System. In Novel drug delivery
systems, Niraliprakashan. 2018; 4th ed: pp. 8.1-8.20.
5. MAD NasalTM - YouTube. Available from:
https://www.youtube.com/watch?v=7sJMaSOoH88