3. Introduction
Factors Affecting Niosomes Preparation
Methods of Preparation
Characterization of Niosomes
Stability of Niosomes
Applications of Niosomes
Toxicity of Niosomes
4. Niosomes are non-ionic surfactant based unilamellar or
multilamellar bilayer vesicles up on hydration of non ionic
surfactants with or without incorporation 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 ,entrap either in the
aqueous layer or in vesicular membrane
made of lipid materials.
3
5. Structure of niosomes:
Head part
(hydrophilli
c)Tail part
(hydrophobic)
Drug
molecules
Phospholipi
ds
Polar heads
facing
hydrophilic
region
Hydrophobic
drugs
localized in
the
hydrophobic
lamellae
Hydrophilic
drugs
located in
aqueous
regions
encapsulate
d
These vesicular systems are similar to liposomes that
can be
used as carriers of amphiphilic and lipophilic drugs.
It is less toxic and improves the therapeutic index of5
6. They are osmotically active and stable.
They increase the stability of the entrapped drug.
The vesicle suspension being water based offers greater
patient compliance over oil based systems
Since the structure of the niosome offers place to
accommodate hydrophilic, lipophilic as well as ampiphilic
drug moieties, they can be used for a variety of drugs.
The vesicles can act as a depot to release the drug slowly and
of controlled release.
Biodegradable, non-immunogenic and biocompatible.
Advantages of niosomes:
6
8. According to the nature of lamellarity
1. Multilamellar vesicles (MLV) 1-5 μm in size.
2. Large Unilamellar vesicles (LUV) 0.1 – 1μm in size
3. Small Unilamellar vesicles (SUV) 25 – 500 nm in
size.
According to the size
1. Small Niosomes (100 nm – 200 nm)
2. Large Niosomes (800 nm – 900 nm)
3. Big Niosomes (2 μm – 4 μm)
10. Cholesterol and Non ionic surfactants are the two major
components used for the preparation of niosomes.
Cholesterol provides rigidity and proper shape. The
surfactants play a major role in the formation of niosomes.
non-ionic surfactants like spans(span 20,40,60,85,80), tweens
(tween 20,40,60,80) are generally used for the preparation of
Niosomes.
Few other surfactants that are reported to form niosomes are
as follows :
Ether linked surfactant
Di-alkyl chain surfactant
Ester linked
Sorbitan Esters
Poly-sorbates
Components of niosomes:
10
12. Sl.
No.
Liposomes Niosomes
1. Vesicles made up of concentric
bilayer of phospholipids
Vesicles made up of
surfactants with or without
incorporation of cholesterol.
2. Size ranges from 10-3000nm Size ranges from 10-100nm
3. Comparatively expensive Inexpensive
4. Special storage condition are
required
No such special requirement
5. Phospholipids used are unstable Non-ionic surfactants are
stable
6. Comparatively more toxic Less toxic
Comparisition between liposomes & niosomes:
12
16. The mixture is
probe sonicated
at 60°C for 3
minutes using a
sonicator with a
titanium probe to
yield Niosomes.
Added to the
surfactant/
cholesterol
mixture in a
10 ml glass
vial
Aliquot of
drug
solution in
buffer
Sonication method
17. Creation of a solution
of cholesterol and
surfactant (1:1 ratio)
in a mixture of ether
and chloroform
An aqueous phase
containing the drug
to be loaded is
added to this
Resulting two
phases are
sonicated at 4-
5°C
A clear gel is
formed which is
further sonicated
after the addition
of phosphate
buffered saline
(PBS)
Temperature is
raised to 40°C and
pressure is reduced
to remove the
organic phase
Viscous Niosome
suspension is formed
which can be diluted
with PBS and heated
on a water bath at
60°C for 10 minutes
to yield Niosomes
18. A solution of the surfactant is
made by dissolving it in diethyl
ether.
This solution is then introduced using an
injection (14 gauge needle) into warm water
or aqueous media containing the drug
maintained at 60°C.
Vaporization of the ether
leads to the formation of
single layered vesicles.
• The particle size of the Niosomes formed depend on the
conditions used, and can range anywhere between 50-1000
μm.
Steps of Ether injection method
19. Good method for controlling Niosomes size.
Mixture of surfactant, cholesterol and
dicetyl phosphate in chloroform is made
into thin film by evaporation
The film is hydrated with aqueous drug
solution
Resultant suspension is extruded through
polycarbonate membranes which are
placed in series for upto 8 passages Multiple membrane extrusion method
20. A recently developed technique which allows the preparation of
Niosomes without the use of organic solvents.
The bubbling unit consists of a round bottom flask with three
necks, and this is positioned in a water bath to control the
temperature.
Water-cooled reflux and thermometer is positioned in the
first and second neck, while the third neck is used to supply
nitrogen.
Cholesterol and surfactant are dispersed together in a buffer
(pH 7.4) at 70°C.
This dispersion is mixed for a period of 15 seconds with
high shear homogenizer and immediately afterwards, it is
bubbled at 70°C using the nitrogen gas to yield Niosomes.
21. Water soluble
carrier such as
sorbitol is
coated with
surfactant.
The result of the
coating process is a
dry formulation in
which each water-
soluble particle is
covered with a thin
film of dry
surfactant.
This preparation
is termed
“Proniosomes”.
The Niosomes
are recognized by
the addition of
aqueous phase at
T > Tm and brief
agitation.
T=Temperature.
Tm = mean phase transition temperature
22. Separation of
unentrapped
drug
Dialysis
Centrifugation
Gel filtration
Separation of unentrapped drug:
Dialyzed in a dialysis
tubing against
phosphate buffer or
normal saline
The unentrapped drug is
removed by gel filtration
of niosomal dispersion
through a Sephadex-G-50
column and elution with
phosphate buffered saline
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.
CentrifuserGel Filtration 73
24. a) Size, Shape and Morphology
Freeze Fracture Electron Microscopy:- Visualize the vesicular
structure of surfactant based vesicles.
Photon Correlation spectroscopy :- Determine mean diameter
of the vesicles.
Electron Microscopy :- Morphological studies of vesicles.
b) Entrapment efficiency
After preparing niosomal dispersion, unentrapped drug is
separated by dialysis and the drug remained entrapped in
niosomes is determined by complete vesicle disruption using
50% n-propanol or 0.1% Triton X-100 and analysing the
resultant solution by appropriate assay method for the drug.
c) Vesicle Suface Charge
Determined by measurement of electrophoretic mobility and
expressed in expressed in terms of zeta potentia
74
25. At various time intervals, the buffer is analysed for the drug content by an
appropriate assay method.
The bag containing the vesicles is placed in 200 ml of buffer solution in a 250
ml beaker with constant shaking at 25°C or 37°C.
The vesicle suspension is pipetted into a bag made up of the tubing and
sealed.
A dialysis sac is washed and soaked in distilled water.
A method of in-vitro release rate study includes the use of dialysis tubing.
26. The vesicle surface charge can play an important role in
the behaviour of Niosomes in vitro and in vivo.
Charged Niosomes are more stable against aggregation
and fusion than uncharged vesicles.
In order to obtain an estimate of the surface potential, the
zeta potential of individual Niosomes can be measured by
Microelectrophoresis, Fluorophores, and Dynamic light
scattering.
Zeta potential is calculated by using Henry equation (S P
Vyas, 2011)
ζ =
µ𝐸4πη
Σ
Where ζ is Zeta potential, µ𝐸 is electrophoretic mobility, η
is viscosity of the medium and Σ is dielectric constant
28. Lancôme has come out with a variety of anti-
ageing products which are based on noisome
formulations. L’Oreal is also conducting research
on anti-ageing cosmetic products.
76
29. Summary :
Niosomes provide incorporating the drug into for
a better targeting of the drug at appropriate tissue
destination .
They presents a structure similar to liposome and
hence they can represent alternative vesicular
systems with respect to liposomes
Niosomes are thoughts to be better candidates
drug delivery as compared to liposomes due to
various factors like cost, stability etc. Various type of
drug deliveries can be possible using niosomes like
targeting, ophthalmic, topical, parenteral etc.
77
30. 1. Madhav Nvs* And Saini A, Niosomes: A Novel
Drug Delivery System, International Journal Of
Research In Pharmacy And Chemistry, 2011,
1(3),498-511.
2. Lohumi Ashutosh, Rawat Suman, A Novel Drug
Delivery System: Niosomes Review, Journal Of
Drug
Delivery & Therapeutics; 2012, 2(5), 129-135.
3. Pawar Sd *, Pawar Rg, Niosome: An Unique Drug
Delivery System, International journal Of
Pharmacy,
Biology and Allied Sciences, April, 2012, 1(3): 406-
416.
4. Rajesh Z. Mujoriya, Niosomal Drug Delivery
System –
A Review, International Journal Of Applied
Pharmaceutics, Vol 3, Issue 3, 2011,7-10.
79
1. Vyas SP, K. R. (2011). Targeted and Controlled Drug
Delivery Novel carrier systems. New delhi: CBS
Publisher and Distributors.
31. Success in life mostly depends on the power of
‘CONCENTRATION’
--- Swami
Vivekananda
Editor's Notes
polysorbate 20 ,should be above the gel to liquid phase
transition temperature of system.leads to gel to liq transition in niosomes,
Niosomes for the treatment of Leishmaniasis-Niosomes are being used for the delivery of stilbogluconate an antileishmaniasis agent for its delivery to visceral organs. It may be related to passive delivery of the vesicles and the contents through RES recognition and uptake by the Kupffer cells.
Niosomes in Oncology:-
Various anticancer drugs like MTX, DOX, can be encapsulated inside the niosomes and bac easily be delivered to the tumor cells due to small size.
Niosomes as immunological adjuvants:-
The ability of niosomes to enhance antibody production in response to Bovine Seum Albumin was compared with Freud’s adjuvant in the Balb/c mice which revealed niosomes as potent stimulator of cellular immunity.
4. Niosomes and Oral drug delivery:-
Niosomes can be used for oral delivery of drug thus protecting it from the hostile environment of the GIT and targeting to RE.
5. Niosomes for Transdermal drug delivery:-
They are being used in topical and transdermal products both contaning hydrophobic and hydrophillic drugs. The intracellular route is the main route of vesicle penetration across the skin.
6. Niosomes in Diagnostic imaging:-
Niosomes can act as carriers for radiopharmaceuticals and site specific vehicle for spleen and liver imaging.
Niosomes for the treatment of Leishmaniasis-Niosomes are being used for the delivery of stilbogluconate an antileishmaniasis agent for its delivery to visceral organs. It may be related to passive delivery of the vesicles and the contents through RES recognition and uptake by the Kupffer cells.
Niosomes in Oncology:-
Various anticancer drugs like MTX, DOX, can be encapsulated inside the niosomes and bac easily be delivered to the tumor cells due to small size.
Niosomes as immunological adjuvants:-
The ability of niosomes to enhance antibody production in response to Bovine Seum Albumin was compared with Freud’s adjuvant in the Balb/c mice which revealed niosomes as potent stimulator of cellular immunity.
4. Niosomes and Oral drug delivery:-
Niosomes can be used for oral delivery of drug thus protecting it from the hostile environment of the GIT and targeting to RE.
5. Niosomes for Transdermal drug delivery:-
They are being used in topical and transdermal products both contaning hydrophobic and hydrophillic drugs. The intracellular route is the main route of vesicle penetration across the skin.
6. Niosomes in Diagnostic imaging:-
Niosomes can act as carriers for radiopharmaceuticals and site specific vehicle for spleen and liver imaging.
Niosomes for the treatment of Leishmaniasis-Niosomes are being used for the delivery of stilbogluconate an antileishmaniasis agent for its delivery to visceral organs. It may be related to passive delivery of the vesicles and the contents through RES recognition and uptake by the Kupffer cells.
Niosomes in Oncology:-
Various anticancer drugs like MTX, DOX, can be encapsulated inside the niosomes and bac easily be delivered to the tumor cells due to small size.
Niosomes as immunological adjuvants:-
The ability of niosomes to enhance antibody production in response to Bovine Seum Albumin was compared with Freud’s adjuvant in the Balb/c mice which revealed niosomes as potent stimulator of cellular immunity.
4. Niosomes and Oral drug delivery:-
Niosomes can be used for oral delivery of drug thus protecting it from the hostile environment of the GIT and targeting to RE.
5. Niosomes for Transdermal drug delivery:-
They are being used in topical and transdermal products both contaning hydrophobic and hydrophillic drugs. The intracellular route is the main route of vesicle penetration across the skin.
6. Niosomes in Diagnostic imaging:-
Niosomes can act as carriers for radiopharmaceuticals and site specific vehicle for spleen and liver imaging.
