MOLECULAR PHARMACEUTICS, NOVEL DRUG DELIVERY SYSTEM, NIOSOMES

1. NIOSOMES
Presented by:
NAVEEN BALAJI
2nd Semester M.Pharm
Department of Pharmaceutics
SSCP
Tumkur.

2. • Niosomes are novel drug delivery system in which both hydrophilic
and hydrophobic drug is encapsulated in a vesicle. This are non-ionic
surfactant vesicles, which are biodegradable , relatively non-toxic ,
more stable, inexpensive and alternative to liposome.
• They present a structure similar to liposomes they can represent
alternative to vesicular system with respect to liposomes.

3. • Niosomes basically made of non – ionic surfactant which provide
advantages over the phospholipids because they are more
economical and are chemically more stable as they are not easily
hydrolysed or oxidized during storage.
• The vesicles forming amphiphile is a non-ionic surfactant stabilized by
addition of cholesterol and small amount of anionic surfactant such
as dicetyl phosphate

4. • Similar to liposomes, in that they are also made up of a bilayer.
• However, the bilayer in the case of Niosomes is made up of non-ionic
• Surface active agents rather than phospholipids.
• Vesicle holds hydrophilic drugs within the space enclosed in the
vesicle, while hydrophobic drugs are embedded within the bilayer
itself.
• Niosomes vesicle would consist of a vesicle forming amphiphile
• i.e.a non-ionic surfactant such as Span- 60, which is usually stabilized
by the addition of cholesterol.

5. made of uncharged single chain
made of neutral or charged double
 In both basic unit of assembly is Amphiphiles, but they
phospholipids in liposomes and nonionic surfactants in
niosomes.
 Both can entrap hydrophilic and lipophilic drugs.
 Both have same physical properties but differ in their chemical
composition.
 Niosomes has higher chemical stability than liposomes.
 Niosomes
surfactant molecules
 Liposomes
chain phospholipids.

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.
Advantagesofniosomes:
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7.  Improve the therapeutic performance of the drug molecules by
 Delayed clearance from the circulation
 Protecting the drug from biological environment
 Restricting effects to target cells
 Niosomal dispersion in an aqueous phase can be emulsified in a nonaqueous
phase to
 Regulate the delivery rate of drug
 Administer normal vesicle in external non-aqueous phase.
 Handling and storage of surfactants requires no special conditions.
 Bioavailability of poorly absorbed drugs is increased.
 Targeted to the site of action by oral, parenteralas well as topical
routes.
ADVANTAGES OF NIOSOMES
DELIVERY SYSTEM

8. Aggregation (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. These charged
molecule sare used mainly to prevent aggregation of
niosomes) Fusion(due to repulsive force it can
avoided)

9. Leaking of entrappeddrug
Hydrolysis of encapsulated drugs
which limiting the shelf life of the
dispersion.
Leaking of entrappeddrug
Hydrolysis of encapsulated drugs
which limiting the shelf life of the
dispersion.

10. Disadvantage of niosomes
 The aqueous suspension , of niosomes may have
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to fusion , aggregation ,limited shelf life due
leaking of entrapped drugs , and hydrolysis of
encapsulated drugs.
 The methods of preparation of multilamellar vesicles
such as extrusion , sonication, are time consuming
specliazed equipment forand may require
processing .

11.  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)
TYPES OF NIOSOMES

12. 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.
Components of niosomes:
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13. • Cholesterol provides rigidity and proper shape.
• Reduces leakage of drug from the Niosome
• Strengthen the non-polar tail of the non-ionic surfactant
• Increase in the entrapment efficiency

14. 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:

15. METHODS OF PREPARATION
(Madhav NVS, 2011)
 Film Method
 Ether Injection Method
 Sonication
 Reverse Phase Evaporation
 Heating Method
 Microfluidization
 Multiple Membrane Extrusion Method
 Transmembrane pH gradient (inside acidic) Drug
Uptake Process (remote Loading)
 The “Bubble” Method
 Formation of Niosomes from Proniosomes

16. •Mixture of
Surfactant and
Cholesterol
Dissolved in an
organic solvent
in a round-
bottomed flask.
(e.g. diethyl
ether,
chloroform, etc.)
solvent is•organic
removed by low
pressure/vacuum at
room temperature
example
using a
rotary
evaporator.
• The resultant
dry surfactant
film is hydrated
by agitation at
50–60°C
Multilamellar
vesicles
(MLV) are
formed
FILM METHOD
• Also known as hand shaking method

17. FILM METHOD
Figure 6: Steps of Film method (Madhav NVS, 2011)

18. • The drug can be added to aqueous phase if hydrophilic and can be
dissolved in organic solvent with other component if hydrophobic.

19. 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.
ETHER INJECTION METHOD
Figure 7: Steps of Ether injection method (Madhav NVS, 2011)

20. Ether injection Method: 14 guage
needle
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21. 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
Figure 8: Sonication method

22. 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
phosphate
saline
of
buffered
(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
REVERSE PHASE EVAPORATION

23.  Non-toxic, Scalable and one-step method.
HEATING METHOD
Mixtures of non-ionic
surfactant, cholesterol
and/or charge inducing
molecules are added to an
aqueous medium e.g.
buffer, distilled H2O, etc
• In the presence of a
Polyol such as glycerol.
The mixture is
heated while
stirring at low
shear forces
• Until vesicles are
formed

24. • Charge inducing molecule Some charged molecules are added to
niosomes to increase stability . Charge-inducing components like
charged phospholipids, and non-ionic surfactant .

25.  Good method for controlling Niosomes size.
MULTIPLE MEMBRANE EXTRUSION
METHOD
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
Figure 10: Multiple membrane
extrusion method (Madhav NVS, 2011)

26. • Extruded:
• Force or press out; expel:

27. NIOSOME DELIVERYAPPLICATIONS
 Niosomes as Drug Carriers
 Diagnostic imaging with Niosomes:
 Niosomes can act as carriers for radiopharmaceuticals
 and site specific vehicles for spleen and liver imaging.

28. NIOSOME DELIVERYAPPLICATIONS
 Drug Targeting
 Delivery to the brain
 Anti cancer drugs
 Anti infectives

29. • In Oncology:
• Most–anti neoplastic drug cause severe side effects. Niosomes can
alter the metabolism , prolong circulation and half life of drug , thus
decreasing the side effects of drug.
• Various anticancer drugs like MTX(methotrexate),can be encapsulated
inside the niosomes and they can be easily delivered to the tumor
cells due to small size.

30. • Targeting of bioactive agents:
• To Reticulo-endothelial system (RES)
• The cells of RES preferentially take up the vesicles .
• To organs other than RES

31.  Ophthalmic drug delivery
 Delivery of peptide drugs
 Immunological application of Niosomes
 Delivery system for the vasoactive intestinalpeptide
(VIP)
 Niosomes as carriers for Hemoglobin
 Niosomal vaccines
NIOSOME DELIVERYAPPLICATIONS

32. • Transdermal delivery of drugs by Niosomes:
• They have application in topical and transdermal products both
containing hydrophobic and hydrophilic drugs. An increase in the
penetration rate is achieved by transdermal delivery incorporated in
niosomes. The intracellular route is the main route of vesicle
penetration across the skin. Ex: erythromycin

33. • In the treatment of Lieshmaniasis:
• Niosomes are used for drug targeting in treatment of diseases in
which the organism resides in the RES. Lieshmaniasis is a disease in
which parasite invades the cells of liver and spleen. Niosomes are
used for the delivery of stilbogluconate, an anti-leishmaniasis agent
to visceral organs.

34. • In the delivery of peptide drugs
• As immunological adjuvants:
• The ability of niosomes to enhance antibody production.
• Niosomes as pulmonary drug delivery system.
• They improved oral bioavailability of poorly absorbed drugs

35.  Sustained Release
 Localized Drug Action
OTHER APPLICATIONS