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niosome anshul vishwakarma .pptx
1. Department of pharmaceutical sciences
Dr. Hari Singh Gour Vishwavidyalaya
Sagar, (M.P.)
(A CENTRAL UNIVERSITY)
PRESENTED BY:-
Anshul Vishwakarma
Y21254007
NIOSoMOES
3. DEFINITION
Niosomes are non - ionic surfactant based unilamellar or multilamellar bilayer vesicles .
These are formed upon hydration of non ionic surfactants with or without incorporation of
cholesterol.
The niosomes are very small , and microscopic in size . Their size lies in the nanometric
scale.
Niosomes are a novel drug delivery system , in which the medication is encapsulated in a
vesicle .
Both hydrophilic & lipophilic drugs , can be entrapped either in the aqueous layer or in lipid
layer.
4. CLASSIFICATION OF NIOSOMES
• The niosomes are classified as a function of the number of bilayer (e.g. MLV, SUV) or as a function of size. (e.g.
LUV, SUV) or as a function of the method of preparation
• The various types of niosomes are described below:
A. Multi lamellar vesicles (MLV, size ≥ 0.05 µm)
B. Large unilamellar vesicles (LUV, size ≥ 0.10 µm)
C. Small unilamellar vesicles (SUV, size = 0.025-0.05 µm)
5. STRUCTURE OF NIOSOMES
• Niosomes are microscopic lamellar structures
Basic structural components are
I. Non ionic surfactant
II. cholesterol
III. Charge inducing molecule
6. NON-IONIC SURFACTANTS
• Selection of surfactant should be done on the basis of HLB value.
• As hydrophilic lipophilic balance (HLB) is a good indicator of the vesicle forming ability of any surfactant,
HLB number in between 4 and 8 is found to be compatible with vesicle formation.
• Alkyl ethers: some surfactants for the preparation of niosomes containing drugs/chemicals as:
1) surfactant-i (mol.Wt.473) is C16 mono alkyl glycerol ether with average of three glycerol units.
2) surfactant-ii (mol.Wt.972) is diglycerol ether with average of the seven glycerol units.
3) surfactant iii (mol.Wt.393) is ester linked surfactant.
• Alkyl esters
• Alkyl amides
• Fatty acid and amino acid compounds
7. CHOLESTEROL
• Steroids are important components of the cell membrane and their presence in membrane affect the bilayer
fluidity and permeability. Cholesterol is a steroid derivative, which is mainly used for the formulation of
niosomes.
• Although it may not show any role in the formation of bilayer, its importance in formation of niosomes and
manipulation of layer characteristics can not be discarded. In general, incorporation of cholesterol affect
properties of niosomes like membrane permeability, rigidity, encapsulation efficiency, ease of rehydration of
freeze dried niosomes and their toxicity.
• As a result of this, the niosome become less leaky in nature.
8. CHARGEDMOLECULE:
• Some charged molecules are added to niosomes to increase stability of niosomes by
electrostatic repulsion which prevents coalescence.
• The negatively charged molecules used are diacetyl phosphate (dcp) and phosphotidic acid.
Similarly, stearyl amine (STR) and stearyl pyridinium chloride are the well known
positively charged molecules used in niosomal preparations.
• These charged molecules are used mainly to prevent aggregation of niosomes.
10. METHODOF PREPARATION
1.Ether injection (LUV) based on the vesicle size, niosomes can be divided into three groups.
2. Hand shaking method (MLV) these are small unilamellar vesicles (SUV, size=0.025-0.05 μm),
3. The “bubble” method multilamellar vesicles (MLV, size=>0.05 μm), and large
4. Reverse phase evaporation (LUV) unilamellar vesicles (LUV, size=>0.10 μm).
5. Sonication (SUV)
6. Multiple membrane extrusion method
7. Trans membrane ph gradient drug uptake process (remote loading) (MLV)
8. Microfluidization method (SUV)
9. Formation of niosomes from proniosomes
11. COMMONSTAGESOF ALL METHODSOF PREPARATIONOF NIOSOMES
Cholesterol + non ionic surfactant
Dissolve in organic solvent
Solution in organic solvent
Drying
Thin film
Dispersion (hydration)
Niosome suspension
12. • ETHER INJECTIONMETHOD
Niosomes by slowly introduce in a solution of
surfactant dissolve in diethyl ether into warm water
maintain at 60 C
Mixture in ether is injected through 14-gauge needle
into an aqueous solution of material
Vaporization of ether leads to the formation of the
single layer vesicles
Diameter of the vesicle range from 50 to 1000 nm
depends upon the conditions use
13. HANDSHAKINGMETHOD
The mixing ingredients - surfactant and cholesterol and charge
induce
Dissolves in a volatile organic solvent (chloroform, diethyl ether
or methanol) in a round bottom flask
By using a rotary evaporator organic solvent is evaporated at
room temperature 20°C
Forming a thin layer of solid mixture
The dry surfactant film can be re-hydrated with an aqueous phase
at 0-60°C with gentle agitation
Formation of niosomes
14. • THE “BUBBLE” METHOD
Bubbling unit involves round-bottomed flask with three
neck position in water bath to control the temperature
Water-cool reflux is positioned in the first neck and
thermometer is positioned in the second neck and nitrogen
supply through the third neck
Cholesterol and surfactant are dispersed in the buffer (ph
7.4) at 70°C dispersion mixing for 15 seconds with high
shear homogenizer
“Bubbled” at 70°c using nitrogen gas
15. • REVERSEPHASEEVAPORATION
Surfactant:cholesterol(1:1) in ether or chloroform
Drug in aqueous phase
Sonicated at 4-5˚c
Add pHs & sonicated
organic phase removed at 40˚c under reduced pressure
Viscous niosome suspension diluted with pHs
Heated on a water bath at 60˚c for 10 min
Niosomes
16. • SONICATION
Mixture of drug solution in the buffer, surfactant and cholesterol
Sonicated with a titanium probe sonicator at 60°c for 3 minutes to yield niosomes
17. • MULTIPLEMEMBRANEEXTRUSIONMETHOD
• Mixture of surfactant, cholesterol and dicetyl
phosphate in chloroform forms thin film by
rotary evaporator.
• The film hydrates with aqueous drug
polycarbonate membranes.
• Solution and resultant suspension extrude
through polycarbonate membrane and placed in
series for up to 8 passages. It is a good method
for niosome size control
18. • TRANSMEMBRANEPHGRADIENTDRUGUPTAKEPROCESS
In remote loading process surfactants and cholesterol are dissolved in organic solvent
(chloroform)
solvent evaporates under reduced pressure to get a thin film on the wall of the round
bottom flask
film hydrates with 300 mm citric acid (pH4.0) by vortex mixing
multilamellar vesicles are frozen and thawed 3 times and later sonication
for niosomal suspension, aqueous solution containing 10 mg/ml of drug is added and
vortex
sample pH is raises to 7.0-7.2 with 1M disodium phosphate
the mixture is later heated at 60°C for 10 minutes to yield niosomes
19. • FORMATIONOFNIOSOMESFROMPRONIOSOMES:
• Proniosome is a dry formulation in which each water soluble particle are covered with a thin film of dry
surfactant.
• The niosomes are recognizing by the adding aqueous phase at T > tm with brief agitation.
T is the temperature and tm is the mean phase transition temperature
Carrier + Surfactant = proniosomes,
Proniosomes + Water = Niosomes
20. • SEPARATIONOF UNENTRAPPEDDRUG
The removal of unentrapped solute from the vesicles can be accomplished
by various techniques, which include: -
1) Dialysis: the aqueous niosomal dispersion is dialyzed in dialysis tubing
against phosphate buffer or normal saline or glucose solution.
2) Gel filtration: the unentrapped drug is removed by gel filtration of
niosomal dispersion through a sephadexg-50 column and elution with
phosphate buffered saline or normal saline.
3) Centrifugation: the niosomal suspension is centrifuged and the
supernatant is separated. The pellet is washed and then resuspended to
obtain a niosomal suspension free from unentrapped drug.
21. • EVALUATIONPARAMETERS
Entrapment efficiency (%EE)
Size, shape and morphology
In vitro release study
Tissue distribution/in vivo study
Stability study
Number of lamellae
Membrane rigidity
Vesicular surface charge
22. • APPLICATIONOF NIOSOME
• Ophthalmic drug delivery
• Localized drug action
• Diagnostic imaging with noisome
• Transdermal delivery of drugs by niosomes
• Niosome as a carrier for hemoglobin
• Targeting of bioactive agent
23. ADVANTAGESOF NIOSOMES
Targeted drug delivery can be achieved using niosomes the drug is delivered directly to the body
part where the therapeutic effect is required
Reduced dose is required to achieve the desired effect
Subsequent decrease in the side effects
The therapeutic efficacy of the drugs is improved by reducing the clearance rate, targeting to the
specific site and by protecting the encapsulated drug
Niosomes are amphiphillic i.E. Both hydrophilic and lipophillic in nature and can accommodate a
large number of drugs with a wide range of solubilities
Improve the oral bioavailability of poorly soluble drugs
Enhance the skin permeability of drugs when applied topically
24. DISADVANTAGESOF NIOSOME
• Aqueous suspension of niosome may exhibit fusion, aggregation leaching or hydrolysis of
entrapped drug, thus limiting the shelf life of niosome dispersion.
• Time consuming
• Requires specialized equipment
• Inefficient drug loading
25. REFERENCES
• Jain N.K.’’Advances controlled and novel drug delivery system’’ Ed.1 CBS Publishers and distributors ,New
Delhi 2000, pg.300-320
• Mithal B. M., A text book of pharmaceutical formulation, ed 6 , Vallabh prakashan , 306-307
• Kaur D , Kumar S , Niosomes: present scenario and future aspects Journal of drug delivery & therapeutics.
2018; 8(5):35-43