2. content
2
Introduction
Types of niosomes
Advantages and disadvantages of niosomes
Formulations of niosomes
Structural components of niosomes
Method of preparation
Characterization of niosomes
Applications of niosomes
3. INTRODUCTION
3
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.
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.
4. Types of noisome
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Multi lamellar vesicles (MLV).
Large unilamellar vesicles(LUV)
Small unilamellar vesicles(SUV)
5. Multilamellar vesicles(MLV)
5
It consists of number of bilayer surrounding the
aqueous lipid compatment seperately. The
approximate size of this vesicles is 0.5 to 10 micro
meter diameter. This vesicles are most widely used
niosomes. It is simple to make and are mechanically
stable upon storage for long periods. These vesicles
are highly suited as drug carrier for lipophilic
compounds.
6. Large unilamellar
vesicles(LUV)
6
Niosomes of this type have high aqueous/lipid
compartment ratio , so that larger volume of bio-
active materials can be entrapped with a very
economical use of membrane lipid.
7. Small unilamellar
vesicles(SUV)
7
These small unilamellar vesicles are mostly prepared
from multilamellar vesicles by sonication method ,
french press extrusion electronic stabilization is the
inclusion of dicetyl phosphate in 5(6)–carboxy
fluorescein(CF) loaded span 60 based niosomes.
8. Advantages of niosomes
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High patient compliance in comparision with oily
dosage forms as the vesicle suspension is a water –
based vehicle.
Accomodate drug molecules with wide range of
solubilities.
The characteristics of the vesicle formulation are
variable and controllable. Altering vesicle
composition , size, lamellarity , surface charge and
concentration can control the vesicle
characteristics.
The vesicles may act as a depot, releasing the
9. cont...
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They are osmoticallly active and stable , as well
as they increase the stability of entrappped drug.
Handling and storage of surfactants requires no
special conditions.
They improve oral bioavaibility of poorly absorbed
drugs and enhance skin penetration of drugs.
They can be made to reach the site of action by oral
penetration as well as topical route.
The surfactants are biodegradable , biocompatible
and non- immunogenic.
10. Disadvantage of niosomes
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The aqueous suspension , of niosomes may have
limited shelf life due to fusion , aggregation ,
leaking of entrapped drugs , and hydrolysis of
encapsulated drugs.
The methods of preparation of multilamellar vesicles
such as extrusion , sonication, are time consuming
and may require specliazed equipment for
processing .
11. Formulation of niosomes
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Surfactant; span 60
Cholesterol
Chloroform or methanol
Phosphate buffer
• Drug
14. Non-ionic surfactants
14
Non –ionic surfactants posses hydrophilic head group and
hydrophobic tail .
The hydrophobic moiety may consists of 1/2/3 alkyl chains
or per fluro groups or in some cases a single stearyl groups .
Hydrophilic head groups affect on entrapment efficiency of
drug.
As HLB value increases alkyl chain increases , the size of
niosomes increases . Hence HLB value 14 -17 is not sutaible
for niosomes formulation, HLB value 8.6 have highest
entrapment efficiency , number between 4 and 8 was found to
be compatible with vesicle formation.
15. cholesterol
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• The incorporation of cholesterol into bilayer composition
of niosomes gives membrane stabilizing activity and
decreases the leakiness of membrane.
• Hence incorporation of cholesterol into bilayer increases
the entrapment efficiency .
• Cholesterol is added usually to non-ionic surfactant to
give rigidity and orientation order to the niosomes bilayer
.
• Cholesterol is also known as abolish gel to liquid phase
transition of niosomes system resulting in niosomes that
are less leaky.
16. Other additives
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Other additives include charge inducers which increase
surface charge density and prevent vesicles flocculation
, aggregation and fusion .
Both negatively and positively charged molecules are
used for induction of charge in niosomes.
Dicetyl phosphate and stearyl amine induces negative or
positive charge on membrane and thereby help to
stabilize the form
17. Method of preparation
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1. Ether injection method
2. Thin film hydration technique.
3. Sonication method.
4. Reverse phase evaporation technique (REV)
5. Microfluidization
6. Multiple membrane extrusion method
7. Trans – membrane pH gradient (inside acidic) drug
process (remote loading)
8. Bubble method
9. Formation of niosomes from proniosomes.
18. Ether injection method
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This method provides the means of making
niosomes by slowly introducing a solution of
surfactant dissolved in diethyl ether (volatile
organic solvent) into warm water maintained at
60⁰c .
The surfactant mixture in ether injection through
14 – gauze needle into an aqueous solution of
material .
Vaporization of ether leads to formation of
single layered vesicles.
Depending upon the condition used the
diameter of vesicle range from 50 to 1000 m.
19. Thin film hydration
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All vesicles components i. e surfactant,
cholesterol and charge inducers are disssolved
in volatile organic solvent in a round bottom flask
.
Using rotary evaporator the organic solvent is
evaporated at room temperature forming a thin
dry film of dissolved components.
The dried thin film is hydrated with aqueous
phase with gentle agitation which leads to
formation of niosomes.
The drug can be added to aqueous phase if
hydrophilic and can be dissolved in organic
solvent with other component if hydrophobic.
21. Factor affecting the physicochemical
properties niosomes:
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Nature of surfactants: The surfactants with alkyl chain
length from C12-C18 are suitable for preparation of
noisome.
Membrane additives: Stability of niosomes can be
increased by the number of additives into niosomal
formulation along with surfactant and drugs. The
membrane stability, morphology and permeability of
vesicles are affected by numbers of additive e.g. addition
of cholesterol in niosomal system increases the rigidity
and decreases the drugs permeability through the
membrane. Niosomes prepared by C16G2
/cholesterol/MPEG- Chol show spherical vesicles with
diameters ranging from 20 nm to 200 nms
22. Cont...
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Resistance to osmotic stress: Addition of a
hypertonic salt solution to a suspension of
niosomes brings about reduction in diameter. In
hypotonic salt solution, there is initial slow
release with slight swelling of vesicles probably
due to inhibition of eluting fluid from vesicles,
followed by faster release, which may be due to
mechanical loosening of vesicles .Drug: Entrapment of drug in niosomes
increases vesicle size, probably by interaction of
solute with surfactant head groups, increasing
the charge and mutual repulsion of the
surfactant bilayers, thereby increasing vesicle
size. The hydrophilic lipophilic balance of the
23. Cont...
23
• .
Cholesterol contents: The incorporation of
cholesterol into bilayer composition of niosome
induces membrane stabilizing activity and decreases
the leakiness of membrane. Hence, incorporation of
cholesterol into bilayer increases entrapment
efficiency. The permeability of vesicle bilayer to 5, 6-
carboxy flourescein (CF) is reduced by 10 times due
to incorporation of cholesterol
24. Applications of niosomes
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Niosomes as drug carrrier: Niosomes have also
been used as carrier for iobitridal a diagnostic
agent used for x –ray imagining .
Targeting of bioactive agent : to reticulo –
endothelial system . The cells of RES
preferentially take up the vesicles .
Anti- neoplatic treatment : 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.
25. Cont...
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Localized drug action: drug delivery through
niosomes is one of the approaches to achieve
localized drug action. since their size and low
permeability through epithelium and connective
tissue keeps the drug localized at the site of
administration.
Niosomes formulation as a brain targeted delivery
system for the vasoactive intestinal peptide (VIP):
encapsulated VIP within glucosebearing niosomes
exibitis higher VIP brain uptake as compared to
control .
Niosomes as pulmonary drug delivery system.
26. Cont...
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The vesicle suspension was water–based vehicle.
This will offers high patient compliance in
comparison with oily dosage forms.
They possess an infrastructure consisting of
hydrophilic, amphiphilic and lipophilic moieties
together and as a result could accommodate drug
molecules with a wide range of solubilities.
They improved oral bioavailability of poorly
absorbed drugs and enhanced skin penetration o f
drugs.
They could be made to reach the site of action by
oral, parenteral as well as topical routes.
27. Refrences
27
P Gadhiya, S shukla ,Niosomes in targeted drug
delivery A review, International Journal for
pharmaceutical Research scholars, 2012(1);61-
62.
Gurjar pravina , Naik Nivedita, Niosome: a
promising pharmaceutical drug delivery ,
International journal of pharmaceutics and
analysis ; 2014(2), 425-427.
Gandhi Arijit , suma Oomen sen, Current trend in
niosomes as vesicular drug system , Asian journal
of pharmacy and life sciences ; 2012 2(2), 340-
342
