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1
NIOSOMES
Presented by:
Chinchole Pravin Sonu
(M.PHARM 2nd
SEM)
DEPARTMENT OF PHARMACEUTICS & QUALITY
ASSURANCE
R. C. Patel Institute of Pharmaceutical
Education and Research, shirpur.
2
CONTENT
Introduction
Advantages
Components
Methods of preparation
Characterization
Stability
Applications
References
3
Introduction
Non-ionic surfactant vesicles.
A novel drug delivery system, in which the
medication is encapsulated in a vesicle.
Unilamellar or Multilamellar vesicles which
are very similar to liposomes in structure.
Formed from the self assembly of non-ionic
amphiphiles by hydration in aqueous media
resulting in closed bilayer structures.
4
 Non-ionic surfactants orient in an aqueous medium as
planner bilayer lattices wherein polar or hydrophilic heads
align facing aqueous media while hydrocarbon segments are
so aligned that their interaction with aqueous media is
minimized.
 Every bilayer forms a vesicle so that hydrocarbon/water
interface remains no more exposed.
5
Advantages
 Low cost of production.
 Can act as a depot to release the drug slowly and
offer a controlled release and reduce toxicity.
 Osmotically active and stable.
 Increase the stability of the entrapped drug.
 Can be used for oral, parenteral as well topical use.
 Improve the therapeutic performance of the drug by
protecting it from the biological environment.
6
Components
 Non-ionic surfactants
Polyglycerol alkylethers
Glucosyl dialkylethers
Crown ethers
Polyoxyethylene alkyl
ethers
Esters
 Ionic surfactants
Dicetylphosphate
Stearylamine
 Cholesterol
7
 Basic structural unit – alkyl ether lipids
 Divided in to 2 classes based on hydrophilic head group,
• (A) Alkyl ethers in which hydrophilic head group
consists of repeat glycerol subunits, related isomers.
• (B) Larger sugar molecules, and those in which
hydrophilic head group consists of repeat ethylene
oxide subunits.
 Alkyl esters, amides, fatty acid,
amino acid also form vesicles.
8
 Self-assembly of surfactants in to vesicles can be
determined by critical packing parameter (CPP),
CPP=V/Ic a
where, V=hydrocarbon chain volume
a=area of hydrophilic head group
Ic=hydrocarbon chain length
– CPP between 0.5 to 1 surfactant form vesicles
– CPP<0.5 spherical micelles
– CPP>1 inverted micelles
9
Methods of Preparation
 Ether injection:-
– Surfactant:
cholesterol
solution in
ether
– 14 gauge
needle
– Size: 50 – 1000
μm
10
 Hand shaking method : -(Thin film hydration technique)
11
 Sonication:-
12
 Extrusion:-
13
Trans membrane pH gradient (inside acidic) drug Uptake Process
(Remote Loading):-
Surfactant: cholesterol in chloroform
Solvent is evaporated under reduced
pressure
Thin film hydrated with 300mM citric acid ( pH 4)
MLVs frozen & thawed 3 times, sonicated
10mg/ml Aqueous solution of drug added & vortexed
pH is raised to 7-7.2 with 1M disodium phosphate
Heated at 60°C for 10 minutes
Niosomes
14
Reverse phase evaporation:-
Surfactant:cholesterol(1:1) in ether or
chloroform
Drug in aqueous phase
Sonicated at 4-5˚C
Add PBS & sonicated
Organic phase removed at 40˚C under reduced pressure
Viscous niosome suspension diluted with PBS
Heated on a water bath at 60˚C for 10 min
Niosomes
15
 Bubble method:-
 Niosomes from proniosomes:-
C:S in buffer (pH 7.4) at 70ºC
Mixed for15 sec with high shear homogenizer
Bubbled at 70°C using the nitrogen gas
Niosomes
16
Separation of unentrapped drug:-
(1)Dialysis
(2)Gel filtration
(3)Centrifugation
17
Characterization
 A) Size, Shape and Morphology:-
 B) Entrapment efficiency:-
 C)Vesicle surface charge:-
18
Stability
 Stability in buffer : -
 Stability in hypertonic media : -
Osmotic shrinkage.
 Stability in hypotonic media : -
Slow release of drug for 1 hr followed by faster drug release.
 Stability in Vivo :-
19
Applications
 1)Drug targeting
 2)Anti-neoplastic treatment
 3)Leishmaniasis
 4)Delivery of Peptide Drugs
 5)Use in Studying Immune Response
 6)Niosomes as Carriers for Haemoglobin
 7)Transdermal Drug Delivery Systems Utilizing Niosomes
20
References
• Vyas S. P. And Khar R. K.,Targeted And Controlled Drug
Delivery System, 1st
Edition, 2002, CBS Publication; 249 - 277.
• Jain N. K., Controlled and novel Drug Delivery, 1st
edition 2001,
CBS Publication; 292 - 301.
• Arora Rajnish and Jain C.P., Advances in niosomes as a drug
carrier: A review, Asian journal of pharmaceutics, Vol-1,Issue-
1,April-june 2007,29-39.
• PharmaXChange.info
• Www.wikipedia.org
21

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Niosomes

  • 1. 1 NIOSOMES Presented by: Chinchole Pravin Sonu (M.PHARM 2nd SEM) DEPARTMENT OF PHARMACEUTICS & QUALITY ASSURANCE R. C. Patel Institute of Pharmaceutical Education and Research, shirpur.
  • 3. 3 Introduction Non-ionic surfactant vesicles. A novel drug delivery system, in which the medication is encapsulated in a vesicle. Unilamellar or Multilamellar vesicles which are very similar to liposomes in structure. Formed from the self assembly of non-ionic amphiphiles by hydration in aqueous media resulting in closed bilayer structures.
  • 4. 4  Non-ionic surfactants orient in an aqueous medium as planner bilayer lattices wherein polar or hydrophilic heads align facing aqueous media while hydrocarbon segments are so aligned that their interaction with aqueous media is minimized.  Every bilayer forms a vesicle so that hydrocarbon/water interface remains no more exposed.
  • 5. 5 Advantages  Low cost of production.  Can act as a depot to release the drug slowly and offer a controlled release and reduce toxicity.  Osmotically active and stable.  Increase the stability of the entrapped drug.  Can be used for oral, parenteral as well topical use.  Improve the therapeutic performance of the drug by protecting it from the biological environment.
  • 6. 6 Components  Non-ionic surfactants Polyglycerol alkylethers Glucosyl dialkylethers Crown ethers Polyoxyethylene alkyl ethers Esters  Ionic surfactants Dicetylphosphate Stearylamine  Cholesterol
  • 7. 7  Basic structural unit – alkyl ether lipids  Divided in to 2 classes based on hydrophilic head group, • (A) Alkyl ethers in which hydrophilic head group consists of repeat glycerol subunits, related isomers. • (B) Larger sugar molecules, and those in which hydrophilic head group consists of repeat ethylene oxide subunits.  Alkyl esters, amides, fatty acid, amino acid also form vesicles.
  • 8. 8  Self-assembly of surfactants in to vesicles can be determined by critical packing parameter (CPP), CPP=V/Ic a where, V=hydrocarbon chain volume a=area of hydrophilic head group Ic=hydrocarbon chain length – CPP between 0.5 to 1 surfactant form vesicles – CPP<0.5 spherical micelles – CPP>1 inverted micelles
  • 9. 9 Methods of Preparation  Ether injection:- – Surfactant: cholesterol solution in ether – 14 gauge needle – Size: 50 – 1000 μm
  • 10. 10  Hand shaking method : -(Thin film hydration technique)
  • 13. 13 Trans membrane pH gradient (inside acidic) drug Uptake Process (Remote Loading):- Surfactant: cholesterol in chloroform Solvent is evaporated under reduced pressure Thin film hydrated with 300mM citric acid ( pH 4) MLVs frozen & thawed 3 times, sonicated 10mg/ml Aqueous solution of drug added & vortexed pH is raised to 7-7.2 with 1M disodium phosphate Heated at 60°C for 10 minutes Niosomes
  • 14. 14 Reverse phase evaporation:- Surfactant:cholesterol(1:1) in ether or chloroform Drug in aqueous phase Sonicated at 4-5˚C Add PBS & sonicated Organic phase removed at 40˚C under reduced pressure Viscous niosome suspension diluted with PBS Heated on a water bath at 60˚C for 10 min Niosomes
  • 15. 15  Bubble method:-  Niosomes from proniosomes:- C:S in buffer (pH 7.4) at 70ºC Mixed for15 sec with high shear homogenizer Bubbled at 70°C using the nitrogen gas Niosomes
  • 16. 16 Separation of unentrapped drug:- (1)Dialysis (2)Gel filtration (3)Centrifugation
  • 17. 17 Characterization  A) Size, Shape and Morphology:-  B) Entrapment efficiency:-  C)Vesicle surface charge:-
  • 18. 18 Stability  Stability in buffer : -  Stability in hypertonic media : - Osmotic shrinkage.  Stability in hypotonic media : - Slow release of drug for 1 hr followed by faster drug release.  Stability in Vivo :-
  • 19. 19 Applications  1)Drug targeting  2)Anti-neoplastic treatment  3)Leishmaniasis  4)Delivery of Peptide Drugs  5)Use in Studying Immune Response  6)Niosomes as Carriers for Haemoglobin  7)Transdermal Drug Delivery Systems Utilizing Niosomes
  • 20. 20 References • Vyas S. P. And Khar R. K.,Targeted And Controlled Drug Delivery System, 1st Edition, 2002, CBS Publication; 249 - 277. • Jain N. K., Controlled and novel Drug Delivery, 1st edition 2001, CBS Publication; 292 - 301. • Arora Rajnish and Jain C.P., Advances in niosomes as a drug carrier: A review, Asian journal of pharmaceutics, Vol-1,Issue- 1,April-june 2007,29-39. • PharmaXChange.info • Www.wikipedia.org
  • 21. 21