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Niosome: A future of targeted drug delivery systems

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Over the past several years, treatment of infectious diseases and immunisation has undergone a revolutionary shift. With the advancement of biotechnology and genetic engineering, not only a large number of disease-specific biological have been developed, but also emphasis has been made to effectively deliver these biologicals. Niosomes are vesicles composed of non-ionic surfactants, which are biodegradable, relatively nontoxic, more stable and inexpensive, an alternative to liposomes. This article reviews the current deepening and widening of interest of niosomes in many scientific disciplines and, particularly its application in medicine. This article also presents an overview of the techniques of preparation of niosome, types of niosomes, characterisation and their applications.
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374 Journal of Advanced Pharmaceutical Technology & Research | Oct-Dec 2010 | Vol 1 | Issue 4
Niosome: A future of targeted drug delivery systems
INTRODUCTION
The concept of targeted drug delivery is designed for
aempting to concentrate the drug in the tissues of interest
while reducing the relative concentration of the medication
in the remaining tissues. As a result, drug is localised on the
targeted site. Hence, surrounding tissues are not aected
by the drug. In addition, loss of drug does not happen due
to localisation of drug, leading to get maximum ecacy
of the medication. Dierent carriers have been used for
targeting of drug, such as immunoglobulin, serum proteins,
synthetic polymers, liposome, microspheres, erythrocytes
and niosomes.[1]
Niosomes are one of the best among these carriers. The
self-assembly of non-ionic surfactants into vesicles was
rst reported in the 70s by researchers in the cosmetic
industry. Niosomes (non-ionic surfactant vesicles) obtained
on hydration are microscopic lamellar structures formed
upon combining non-ionic surfactant of the alkyl or dialkyl
polyglycerol ether class with cholesterol.[2] The non-ionic
surfactants form a closed bilayer vesicle in aqueous media
based on its amphiphilic nature using some energy for
instance heat, physical agitation to form this structure.
In the bilayer structure, hydrophobic parts are oriented
away from the aqueous solvent, whereas the hydrophilic
heads remain in contact with the aqueous solvent. The
properties of the vesicles can be changed by varying
the composition of the vesicles, size, lamellarity, tapped
volume, surface charge and concentration. Various forces
act inside the vesicle, eg, van der Waals forces among
surfactant molecules, repulsive forces emerging from
the electrostatic interactions among charged groups of
surfactant molecules, entropic repulsive forces of the head
groups of surfactants, short-acting repulsive forces, etc.
These forces are responsible for maintaining the vesicular
structure of niosomes. But, the stability of niosomes are
affected by type of surfactant, nature of encapsulated
drug, storage temperature, detergents, use of membrane
spanning lipids, the interfacial polymerisation of surfactant
monomers in situ, inclusion of charged molecule. Due to
presence of hydrophilic, amphiphilic and lipophilic moieties
in the structure, these can accommodate drug molecules
with a wide range of solubility.[3] These may act as a depot,
releasing the drug in a controlled manner. The therapeutic
performance of the drug molecules can also be improved
by delayed clearance from the circulation, protecting the
drug from biological environment and restricting eects to
target cells.[4] Noisome made of alpha, omega-hexadecyl-
bis-(1-aza-18-crown-6) (Bola-surfactant)-Span 80-cholesterol
(2:3:1 molar ratio) is named as Bola-Surfactant containing
noisome.[5] The surfactants used in niosome preparation
should be biodegradable, biocompatible and non-
immunogenic. A dry product known as proniosomes may
Abstract
Over the past several years, treatment of infectious diseases and immunisation has
undergone a revolutionary shift. With the advancement of biotechnology and genetic
engineering, not only a large number of disease-specific biological have been developed,
but also emphasis has been made to effectively deliver these biologicals. Niosomes
are vesicles composed of non-ionic surfactants, which are biodegradable, relatively
nontoxic, more stable and inexpensive, an alternative to liposomes. This article reviews
the current deepening and widening of interest of niosomes in many scientific disciplines
and, particularly its application in medicine. This article also presents an overview of
the techniques of preparation of niosome, types of niosomes, characterisation and
their applications.
Key words: Bilayer, drug entrapment, lamellar, niosomes, surfactants
Kazi Masud Karim, Asim Sattwa
Mandal, Nikhil Biswas, Arijit Guha,
Sugata Chatterjee, Mamata Behera,
Ketousetuo Kuotsu
Department of Pharmaceutical
Technology, Jadavpur University,
Kolkata – 700 032, West Bengal, India
J. Adv. Pharm. Tech. Res.
Address for correspondence
Dr. Ketousetuo Kuotsu, Department of Pharmaceutical
Technology, Jadavpur University, Kolkata - 700 032,
West Bengal, Kolkata, India. E-mail: ketousetuoju@yahoo.in
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375
Journal of Advanced Pharmaceutical Technology & Research | Oct-Dec 2010 | Vol 1 | Issue 4
Karim, et al.: Niosome – A future of targeted drug delivery systems
be hydrated immediately before use to yield aqueous
niosome dispersions. The problems of niosomes such as
aggregation, fusion and leaking, and provide additional
convenience in transportation, distribution, storage, and
dosing.[6]
Niosomes behave in vivo like liposomes, prolonging
the circulation of entrapped drug and altering its organ
distribution and metabolic stability.[7] As with liposomes,
the properties of niosomes depend on the composition
of the bilayer as well as method of their production. It is
reported that the intercalation of cholesterol in the bilayers
decreases the entrapment volume during formulation, and
thus entrapment eciency.[8]
However, differences in characteristics exist between
liposomes and niosomes, especially since niosomes
are prepared from uncharged single-chain surfactant
and cholesterol, whereas liposomes are prepared from
double-chain phospholipids (neutral or charged). The
concentration of cholesterol in liposomes is much more than
that in niosomes. As a result, drug entrapment eciency of
liposomes becomes lesser than niosomes. Besides, liposomes
are expensive, and its ingredients, such as phospholipids,
are chemically unstable because of their predisposition
to oxidative degradation; moreover, these require special
storage and handling and purity of natural phospholipids
is variable.
Niosomal drug delivery is potentially applicable to many
pharmacological agents for their action against various
diseases. It can also be used as vehicle for poorly absorbable
drugs to design the novel drug delivery system. It enhances
the bioavailability by crossing the anatomical barrier of
gastrointestinal tract via transcytosis of M cells of Peyer’s
patches in the intestinal lymphatic tissues.[9] The niosomal
vesicles are taken up by reticulo-endothelial system. Such
localised drug accumulation is used in treatment of diseases,
such as leishmaniasis, in which parasites invade cells of
liver and spleen.[10,11] Some non-reticulo-endothelial systems
like immunoglobulins also recognise lipid surface of this
delivery system.[2-8,10-12] Encapsulation of various anti-
neoplastic agents in this carrier vesicle has minimised drug-
induced toxic side eects while maintaining, or in some
instances, increasing the anti-tumour ecacy.[13] Doxorubicin,
the anthracycline antibiotic with broad-spectrum anti-
tumour activity, shows a dose-dependent irreversible
cardio-toxic eect.[14,15] Niosomal delivery of this drug to
mice bearing S-180 tumour increased their life span and
decreased the rate of proliferation of sarcoma. Intravenous
administration of methotrexate entrapped in niosomes to
S-180 tumour bearing mice resulted in total regression of
tumour and also higher plasma level and slower elimination.
It has good control over the release rate of drug, particularly
for treating brain malignant cancer.[16] Niosomes have been
used for studying the nature of the immune response
provoked by antigens.[17] Niosomes can be used as a carrier
for haemoglobin.[18,19] Vesicles are permeable to oxygen and
haemoglobin dissociation curve can be modied similarly
to non-encapsulated haemoglobin. Slow penetration of drug
through skin is the major drawback of transdermal route
of delivery.[20] Certain anti-inflammatory drugs like
urbiprofen and piroxicam and sex hormones like estradiol
and levonorgestrel are frequently administered through
niosome via transdermal route to improve the therapeutic
ecacy of these drugs. This vesicular system also provides
beer drug concentration at the site of action administered
by oral, parenteral and topical routes. Sustained release
action of niosomes can be applied to drugs with low
therapeutic index and low water solubility. Drug delivery
through niosomes is one of the approaches to achieve
localised drug action in regard to their size and low
penetrability through epithelium and connective tissue,
which keeps the drug localised at the site of administration.
Localised drug action enhances ecacy of potency of the
drug and, at the same time, reduces its systemic toxic eects,
eg, antimonials encapsulated within niosomes are taken up
by mononuclear cells, resulting in localisation of drug,
increase in potency, and hence decrease in dose as well as
toxicity.[13] The evolution of niosomal drug delivery
technology is still at the stage of infancy, but this type of
drug delivery system has shown promise in cancer
chemotherapy and anti-leishmanial therapy.
VARIOUS TYPES OF NIOSOME
Based on the vesicle size, niosomes can be divided into
three groups. These are small unilamellar vesicles (SUV,
size=0.025-0.05 μm), multilamellar vesicles (MLV, size=>0.05
μm), and large unilamellar vesicles (LUV, size=>0.10 μm).
Methods of Preparation
Niosomes are prepared by dierent methods based on
the sizes of the vesicles and their distribution, number of
double layers, entrapment eciency of the aqueous phase
and permeability of vesicle membrane.
Preparation of small unilamellar vesicles
Sonication
The aqueous phase containing drug is added to the mixture
of surfactant and cholesterol in a scintillation vial.[11] The
mixture is homogenised using a sonic probe at 60°C for 3
minutes. The vesicles are small and uniform in size.
Micro uidisation
Two uidised streams move forward through precisely
dened micro channel and interact at ultra-high velocities
within the interaction chamber.[21] Here, a common
gateway is arranged such that the energy supplied to the
system remains within the area of niosomes formation.
The result is a greater uniformity, smaller size and beer
reproducibility.
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376 Journal of Advanced Pharmaceutical Technology & Research | Oct-Dec 2010 | Vol 1 | Issue 4
Karim, et al.: Niosome – A future of targeted drug delivery systems
Preparation of multilamellar vesicles
Hand shaking method (Thin lm hydration technique)
In the hand shaking method, surfactant and cholesterol
are dissolved in a volatile organic solvent such as diethyl
ether, chloroform or methanol in a rotary evaporator,
leaving a thin layer of solid mixture deposited on the wall
of the ask.[11] The dried layer is hydrated with aqueous
phase containing drug at normal temperature with gentle
agitation.
Trans-membrane pH gradient (inside acidic) drug uptake process
(remote Loading)
Surfactant and cholesterol are dissolved in chloroform.[22]
The solvent is then evaporated under reduced pressure to
obtain a thin lm on the wall of the round-boom ask.
The lm is hydrated with 300 mM citric acid (pH 4.0) by
vortex mixing. The multilamellar vesicles are frozen and
thawed three times and later sonicated. To this niosomal
suspension, aqueous solution containing 10 mg/ml of drug
is added and vortexed. The pH of the sample is then raised
to 7.0-7.2 with 1M disodium phosphate. This mixture is
later heated at 60°C for 10 minutes to produce the desired
multilamellar vesicles.
Preparation of large unilamellar vesicles
Reverse phase evaporation technique (REV)
In this method, cholesterol and surfactant are dissolved in
a mixture of ether and chloroform.[23] An aqueous phase
containing drug is added to this and the resulting two
phases are sonicated at 4-5°C. The clear gel formed is further
sonicated aer the addition of a small amount of phosphate
buered saline. The organic phase is removed at 40°C under
low pressure. The resulting viscous niosome suspension
is diluted with phosphate-buered saline and heated in a
water bath at 60°C for 10 min to yield niosomes.
Ether injection method
The ether injection method is essentially based on slow
injection of niosomal ingredients in ether through a
14-gauge needle at the rate of approximately 0.25 ml/min
into a preheated aqueous phase maintained at 60°C.[11,24] The
probable reason behind the formation of larger unilamellar
vesicles is that the slow vapourisation of solvent results in an
ether gradient extending towards the interface of aqueous-
nonaqueous interface. The former may be responsible for
the formation of the bilayer structure. The disadvantages of
this method are that a small amount of ether is frequently
present in the vesicles suspension and is dicult to remove.
Miscellaneous
Multiple membrane extrusion method
A mixture of surfactant, cholesterol, and diacetyl phosphate
in chloroform is made into thin lm by evaporation.[20]
The lm is hydrated with aqueous drug solution and the
resultant suspension extruded through polycarbonate
membranes, which are placed in a series for up to eight
passages. This is a good method for controlling niosome
size.
Niosome preparation using polyoxyethylene alkyl ether
The size and number of bilayer of vesicles consisting
of polyoxyethylene alkyl ether and cholesterol can be
changed using an alternative method.[25] Temperature
rise above 60°C transforms small unilamellar vesicles
to large multilamellar vesicles (>1 μm), while vigorous
shaking at room temperature shows the opposite eect, ie,
transformation of multilamellar vesicles into unilamellar
ones. The transformation from unilamellar to multilamellar
vesicles at higher temperature might be the characteristic
for polyoxyethylene alkyl ether (ester) surfactant, since it is
known that polyethylene glycol (PEG) and water remix at
higher temperature due to breakdown of hydrogen bonds
between water and PEG moieties. Generally, free drug is
removed from the encapsulated drug by gel permeation
chromatography dialysis method or centrifugation method.
Often, density differences between niosomes and the
external phase are smaller than that of liposomes, which
make separation by centrifugation very dicult. Addition
of protamine to the vesicle suspension facilitates separation
during centrifugation.
Emulsion method
The oil in water (o/w) emulsion is prepared from an organic
solution of surfactant, cholesterol, and an aqueous solution
of the drug.[26,27] The organic solvent is then evaporated,
leaving niosomes dispersed in the aqueous phase.
Lipid injection method
This method does not require expensive organic phase.
Here, the mixture of lipids and surfactant is rst melted
and then injected into a highly agitated heated aqueous
phase containing dissolved drug. Here, the drug can be
dissolved in molten lipid and the mixture will be injected
into agitated, heated aqueous phase containing surfactant.
Niosome preparation using Micelle
Niosomes may also be formed from a mixed micellar
solution by the use of enzymes. A mixed micellar solution
of C16 G2, dicalcium hydrogen phosphate, polyoxyethylene
cholesteryl sebacetate diester (PCSD) converts to a niosome
dispersion when incubated with esterases. PCSD is cleaved
by the esterases to yield polyoxyethylene, sebacic acid and
cholesterol. Cholesterol in combination with C16 G2 and
DCP then yields C16 G2 niosomes.
Characterisation of niosomes
Size
Shape of niosomal vesicles is assumed to be spherical, and
their mean diameter can be determined by using laser light
scaering method.[28] Also, diameter of these vesicles can be
determined by using electron microscopy, molecular sieve
chromatography, ultracentrifugation, photon correlation
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Journal of Advanced Pharmaceutical Technology & Research | Oct-Dec 2010 | Vol 1 | Issue 4
Karim, et al.: Niosome – A future of targeted drug delivery systems
microscopy and optical microscopy[29,30] and freeze fracture
electron microscopy. Freeze thawing of niosomes increases
the vesicle diameter, which might be aributed to a fusion
of vesicles during the cycle.
Bilayer formation
Assembly of non-ionic surfactants to form a bilayer vesicle
is characterised by an X-cross formation under light
polarisation microscopy.[31]
Number of lamellae
This is determined by using nuclear magnetic resonance
(NMR) spectroscopy, small angle X-ray scattering and
electron microscopy.[29]
Membrane rigidity
Membrane rigidity can be measured by means of mobility
of uorescence probe as a function of temperature.[31]
Entrapment eciency
Aer preparing niosomal dispersion, unentrapped drug is
separated 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.[32] It can
be represented as:
Entrapment eciency (EF) = (Amount entrapped / total
amount) × 100
In vitro Release Study
A method of in vitro release rate study was reported with
the help of dialysis tubing.[33] A dialysis sac was washed
and soaked in distilled water. The vesicle suspension was
pipeed into a bag made up of the tubing and sealed. The
bag containing the vesicles was then placed in 200 ml buer
solution in a 250 ml beaker with constant shaking at 25°C
or 37°C. At various time intervals, the buer was analysed
for the drug content by an appropriate assay method. In
another method, isoniazid-encapsulated niosomes were
separated by gel ltration on Sephadex G- 50 powder kept
in double distilled water for 48 h for swelling.[34] At rst, 1
ml of prepared niosome suspension was placed on the top
of the column and elution was carried out using normal
saline. Niosomes encapsulated isoniazid elutes out rst
as a slightly dense, white opalescent suspension followed
by free drug. Separated niosomes were lled in a dialysis
tube to which a sigma dialysis sac was aached to one end.
The dialysis tube was suspended in phosphate buer of
pH (7.4), stirred with a magnetic stirrer, and samples were
withdrawn at specic time intervals and analysed using
high-performance liquid chromatography (HPLC) method.
In vivo Release Study
Albino rats were used for this study. These rats were
subdivided with groups. Niosomal suspension used for
in vivo study was injected intravenously (through tail vein)
using appropriate disposal syringe.
Factors Affecting Physico-Chemical Properties of
Niosomes
Various factors that aect the physico-chemical properties
of niosomes are discussed further.
Choice of surfactants and main additives
A surfactant used for preparation of niosomes must have a
hydrophilic head and a hydrophobic tail. The hydrophobic
tail may consist of one or two alkyl or peruoroalkyl groups
or, in some cases, a single steroidal group.[35] The ether-type
surfactants with single-chain alkyl tail is more toxic than
corresponding dialkyl ether chain. The ester-type surfactants
are chemically less stable than ether-type surfactants and
the former is less toxic than the laer due to ester-linked
surfactant degraded by esterases to triglycerides and fay
acid in vivo.[36] The surfactants with alkyl chain length from
C12 to C18 are suitable for preparation of noisome. Span
series surfactants having HLB number between 4 and 8 can
form vesicles.[37] Dierent types of non-ionic surfactants
with examples are given in Table 1.[38]
The stable niosomes can be prepared with addition of
different additives along with surfactants and drugs.
The niosomes formed have a number of morphologies
and their permeability and stability properties can be
altered by manipulating membrane characteristics by
dierent additives. In case of polyhedral niosomes formed
from C16G2, the shape of these polyhedral niosomes
remains unaected by adding low amount of solulan C24
(cholesteryl poly-24-oxyethylene ether), which prevents
aggregation due to development of steric hindrance. In
contrast, addition of C16G2:cholesterol:solulan (49:49:2)
results in formation of spherical niosomes.[39] The mean
size of niosomes is inuenced by membrane composition.
Addition of cholesterol molecule to niosomal system makes
the membrane rigid and reduces leakage of drug from the
noisome.[40]
Temperature of hydration
Hydration temperature influences the shape and size
of the niosome. For ideal condition, it should be above
the gel to liquid phase transition temperature of system.
Table 1: Different types of non-ionic surfactants
Type of non-ionic
surfactant
Examples
Fatty alcohol Cetyl alcohol, stearyl alcohol, cetostearyl
alcohol, oleyl alcohol
Ethers Brij, Decyl glucoside, Lauryl glucoside,
Octyl glucoside, Triton X-100,
Nonoxynol-9
Esters Glyceryl laurate, Polysorbates, Spans
Block copolymers Poloxamers
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378 Journal of Advanced Pharmaceutical Technology & Research | Oct-Dec 2010 | Vol 1 | Issue 4
Karim, et al.: Niosome – A future of targeted drug delivery systems
Temperature change in the niosomal system affects
assembly of surfactants into vesicles and also induces vesicle
shape transformation.[35,39] A polyhedral vesicle formed by
C16G2:solulan C24 (91:9) at 25°C, on heating, transforms
into spherical vesicle at 48°C, but on cooling from 55°C, the
vesicle produces a cluster of smaller spherical niosomes at
49°C before changing into polyhedral structures at 35°C. In
contrast, the vesicle formed by C16G2:cholesterol:solulan
C24 (49:49:2) shows no shape transformation on heating
or cooling.[27] Along with the above-mentioned factors,
the volume of hydration medium and time of hydration
of niosomes are also critical factors. Improper selection of
these factors may result in the formation of fragile niosomes
or creation of drug leakage problems.
Nature of encapsulated drug
The physico-chemical properties of encapsulated drug
inuence charge and rigidity of the niosome bilayer. The
drug interacts with surfactant head groups and develops
the charge that creates mutual repulsion between surfactant
bilayers, and hence increases vesicle size.[29] The aggregation
of vesicles is prevented due to the charge development on
bilayer. The eect of the nature of drug on formation vesicle
is given in Table 2.
Factors affecting vesicles size, entrapment efficiency, and
release characteristics
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. In
polyoxyethylene glycol (PEG)-coated vesicles, some drug
is entrapped in the long PEG chains, thus reducing the
tendency to increase the size. The hydrophilic lipophilic
balance of the drug aects the degree of entrapment.
Amount and type of surfactant
The mean size of niosomes increases proportionally with
increase in the hydrophilic-lipophilic balance (HLB) of
surfactants such as Span 85 (HLB 1.8) to Span 20 (HLB 8.6)
because the surface free energy decreases with an increase
in hydrophobicity of surfactants.[41] The bilayers of the
vesicles are either in the so-called liquid state or in gel
state, depending on the temperature, the type of lipid or
surfactant and the presence of other components such as
cholesterol. In the gel state, alkyl chains are present in a well
ordered structure, and in the liquid state, the structure of the
bilayers is more disordered. The surfactants and lipids are
characterised by the gel-liquid phase transition temperature
(TC). Phase transition temperature (TC) of surfactants also
aects entrapment eciency, ie, Span 60 having higher TC
provides beer entrapment.
Cholesterol content and charge
Inclusion of cholesterol in niosomes increases its
hydrodynamic diameter and entrapment efficiency. In
general, the action of cholesterol is twofold. On one hand,
cholesterol increases the chain order of liquid state bilayers,
and, on the other, it decreases the chain order of gel state
bilayers. At a high cholesterol concentration, the gel state
is transformed to a liquid-ordered phase. An increase in
cholesterol content of the bilayers resulted in a decrease in
the release rate of encapsulated material, and therefore an
increase in the rigidity of the resulting bilayers. The presence
of charge tends to increase the interlamellar distance
between successive bilayers in multilamellar vesicle
structure and leads to greater overall entrapped volume.[41]
Methods of Preparation
Hand shaking method forms vesicles with greater diameter
(0.35-13 nm) compared to the ether injection method
(50-1,000 nm). Small-sized niosomes can be produced by
Reverse Phase Evaporation (REV) method. Microuidisation
method gives greater uniformity and small-sized vesicles.
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 uid from
vesicles, followed by faster release, which may be due to
mechanical loosening of vesicles structure under osmotic
stress.[2,42]
Table 3 lists drugs that have been used in animal study
through dierent routes.
CONCLUSION
Recent advancements in the eld of scientic research have
resulted in the endorsement of small molecules such as
proteins and vaccines as a major class of therapeutic agents.
These, however, pose numerous drug-associated challenges
such as poor bioavailability, suitable route of drug delivery,
physical and chemical instability and potentially serious
side eects. Opinions of the usefulness of niosomes in the
Table 2: Effect of the nature of drug on the
formation of niosomes
Nature of
the drug
Leakage
from the
vesicle
Stability Other
properties
Hydrophobic
drug
Decreased Increased Improved trans-
dermal delivery
Hydrophilic
drug
Increased Decreased –
Amphiphilic
drug
Decreased Increased
encapsulation, altered
electrophoretic
mobility
Macromolecule Decreased Increased
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Journal of Advanced Pharmaceutical Technology & Research | Oct-Dec 2010 | Vol 1 | Issue 4
Karim, et al.: Niosome – A future of targeted drug delivery systems
withaferin A, with beer tumor eciency. Indian J Pharm Sci
1998;60:45-8.
11. Baillie AJ, Coombs GH, Dolan TF, Laurie J. Non-ionic surfactant
vesicles, niosomes, as delivery system for the anti-leishmanial drug,
sodium stibogluconate. J Pharm Pharmacol 1986;38:502-5.
12. Gregoriadis G. Targeting of drugs: Implications in medicine. Lancet
1981;2:241-6.
13. Hunter CA, Dolan TF, Coombs GH, Baillie AJ. Vesicular systems
(Niosome and Liposomes) for delivery of sodium stibogluconate
in experimental murine visceral leishmaniasis. J Pharm Pharmacol
1988;40:161-5.
14. Cummings J, Stuart JF, Calman KC. Determination of adriamycin,
adriamycinol and their 7-deoxyaglycones in human serum by high-
performance liquid chromatography. J Chromatogr 1984;311:125-
33.
15. Suzuki K, Sokan K. The Application of Liposomes to Cosmetics.
Cosmetic and Toiletries 1990;105:65-78.
16. Alcantar N, Dearborn K, VanAuker M, Toomey R, Hood E.
Niosome-hydrogel drug delivery. US 2008/0050445A1. 2008.
17. Brewer JM, Alexander J. The adjuvant activity of non-ionic sur-
factant vesicles (niosomes) on the BALB/c humoral response to
bovine serum albumin. Immunology 1992;75:570-5.
18. Moser P, Marchand-Arvier M, Labrude P, Handjani -Vila RM,
Vignerson C. Hemoglobin niosomes. I. Preparation, functional
and physico-chemical properties, and stability. Pharma Acta Helv
1989;64:192-202.
19. Moser P, Arvier MM, Labrude P, Vignerson C. Niosomes of hemo-
globine. II. Vitro interactions with plasma proteins and phagocytes.
Pharm Acta Helv 1990;65:82-92.
20. Jayaraman SC, Ramachandran C, Weiner N. Topical delivery of
erythromycin from various formulations: An in vivo hairless mouse
study. J Pharm Sci 1996;85:1082-4.
21. Khandare JN, Madhavi G, Tamhankar BM. Niosomes novel drug
delivery system. East Pharmacist 1994;37:61-4.
22. Mayer LD, Bally MB, Hope MJ, Cullis PR. Uptake of antineoplastic
agents into large unilamellar vesicles in response to a membrane
potential. Biochem Biophys Acta 1985;816:294-302.
23. Naresh RA, Chandrashekhar G, Pillai GK, Udupa N. Antiinam-
matory activity of Niosome encapsulated diclofenac sodium with
Tween-85 in Arthitic rats. Ind J Pharmacol 1994;26:46-8.
24. Rogerson A, Cummings J, Willmo N, Florence AT. The distribu-
tion of doxorubicin in mice following administration in niosomes.
J Pharm Pharmacol 1988;40:337-42.
25. Pardakhty A, Varshosaz J, Rouholamini A. In vitro study of polyoxy-
ethylene alkyl ether niosomes for delivery of insulin. Int J Pharm
2007;328:130-41.
26. Hao Y, Zhao F, Li N, Yang Y, Li K. Studies on a high encapsulation
of colchicines by a noisome system. Int J Pharm 2002;244:73-80.
27. Uchegbu IF, Vyas SP. Non-ionic surfactant based vesicles (nio-
somes) in drug delivery. Int J Pharm 1998;172:33-70.
28. Almira I, Blazek-welsh IA, Rhodes GD. Maltodextrin – Based
proniosomes. AAPS PharmSciTech 2001;3:1-8.
29. Biswal S, Murthy PN, Sahu J, Sahoo P, Amir F. Vesicles of Non-ionic
Surfactants (Niosomes) and Drug Delivery Potential. Int J Pharm
Sci Nanotech 2008;1:1-8.
30. Azmin MN, Florence AT, Handjani-Vila RM, Stuart JF, Vanlerberghe
G, Whiaker JS. The eect of non-ionic surfactant vesicle (niosome)
entrapment on the absorption and distribution of methotrexate in
mice. J Pharm Pharmacol 1985;37:237-42.
31. Manosroi A, Wongtrakul P, Manosroi J, Sakai H, Sugawara F,
Yuasa M, et al. Characterization of vesicles prepared with vari-
ous non-ionic surfactants mixed with cholesterol. Colloids Surf B
2003;30:129-38.
Table 3: Drugs used in niosomal delivery
Routes of drug
administration
Examples of Drugs
Intravenous route Doxorubicin, methotrexate, sodium
stibogluconate, iopromide, vincristine,
diclofenac sodium, flurbiprofen,
centchroman, indomethacin, colchicine,
rifampicin, tretinoin, transferrin and
glucose ligands, zidovudine, insulin,
cisplatin, amarogentin, daunorubicin,
amphotericin B, 5-fluorouracil,
camptothecin, adriamycin, cytarabine
hydrochloride
Peroral route DNA vaccines, proteins, peptides, ergot
alkaloids, ciprofloxacin, norfloxacin,
insulin
Transdermal route Flurbiprofen, piroxicam, estradiol,
levonorgestrol, nimesulide, dithranol,
ketoconazole, enoxacin, ketorolac
Ocular route Timolol maleate, cyclopentolate
Nasal route Sumatriptan, influenza viral vaccine
Inhalation All-trans retinoic acids
delivery of proteins and biologicals can be unsubstantiated
with a wide scope in encapsulating toxic drugs such as
anti-AIDS drugs, anti-cancer drugs, and anti-viral drugs.
It provides a promising carrier system in comparison with
ionic drug carriers, which are relatively toxic and unsuitable.
However, the technology utilised in niosomes is still in its
infancy. Hence, researches are going on to develop a suitable
technology for large production because it is a promising
targeted drug delivery system.
REFERENCES
1. Allen TM. Liposomal drug formulations: Rationale for develop-
ment and what we can expect for the future. Drugs 1998;56:747-56.
2. Malhotra M, Jain NK. Niosomes as drug carriers. Indian Drugs
1994;31:81-6.
3. Udupa N. Niosomes as drug carriers. In: Jain NK, editor. Controlled
and novel drug delivery. 1st edition. New Delhi: CBS Publishers
and Distributors; 2002.
4. Baillie AJ, Florence AT, Hume LR, Muirhead GT, Rogerson A. The
Preparation and propereties of Niosomes-Non ionic surfactant
vesicles. J Pharm Pharmacol 1985;37:863-8.
5. Kaur IP, Garg A, Singla AK, Aggarwal D. Vesicular systems in
ocular drug delivery: An overview. Int J Pharm 2004;269:1-14.
6. Hu C, Rhodes DG. Proniosomes: A Novel Drug Carrier Prepara-
tion. Int J Pharm 1999;185:23-35.
7. Azmin MN, Florence AT, Handjani-Vila RM, Stuart JF, Vanlerberghe
G, Whiaker JS. The eect of non-ionic surfactant vesicle (noisome)
entrapment on the absorption and distribution of methoterxate in
mice. J Pharm Pharmacol 1985;37:237-42.
8. Szoka Jr F, Papahadjopoulos D. Comparative properties and
methods of preparation of lipid vesicles (liposomes). Annu Rev
Biophys Bioeng 1980;9:467-508.
9. Jadon PS, Gajbhiye V, Jadon RS, Gajbhiye KR, Ganesh N. Enhanced
oral bioavailability of griseofulvin via niosomes. AAPS PharmSci-
Tech 2009;10:1186-92.
10. Sheena IP, Singh UV, Kamath R, Uma Devi P, Udupa N. Niosomal
[Downloaded free from http://www.japtr.org on Wednesday, September 28, 2016, IP: 83.84.166.247]
380 Journal of Advanced Pharmaceutical Technology & Research | Oct-Dec 2010 | Vol 1 | Issue 4
Karim, et al.: Niosome – A future of targeted drug delivery systems
32. Balasubramaniam A, Kumar VA, Pillai KS. Formulation and in-vivo
evaluation of niosome encapsulated daunorubicin hydrochloride.
Drug Dev Ind Pharm 2002;28:1181-93.
33. Yoshioka T, Stermberg B, Florence AT. Preparation and properties
of vesicles (niosomes) of sobitan monoesters (Span 20, 40, 60, and
80) and a sorbitan triester (Span 85). Int J Pharm 1994;105:1-6.
34. Karki R, Mamatha GC, Subramanya G, Udupa N. Preparation,
characterization and tissue disposition of niosomes containing
isoniazid. Rasayan J Chem 2008;1:224-7.
35. Uchegbu FI, Vyas PS. Non-ionic surfactant based vesicles (nio-
somes) in drug delivery. Int J Pharm 1998;172:33-70.
36. Hunter CA, Dolan TF, Coombs GH, Baillie AJ. Vesicular system
(niosomes and liposomes) for delivery of sodium stibogluconate
in experimental murine visceral leishmaniasis. J Pharm Pharmacol
1988;40:161-5.
37. Yoshioka T, Florence AT. Vesicle (niosome)-in-water-in-oil (v/w/o)
emulsion an in-vitro study. Int J Pharm 1994;108:117-23.
38. Cooper and Gunn. Emulsions and cream. In: Carter SJ, editor.
Dispensing for Pharmaceutical Students. 12th edition. New York:
CBS Publishers and Distributors; 2000. P. 128.
39. Arunothayanun P, Bernard MS, Craig DQ, Uchegbu IF, Florence
AT. The eect of processing variables on the physical characteristics
of nonionic surfactant vesicles (niosomes) formed from hexadecyl
diglycerol ether. Int J Pharm 2000;201:7-14.
40. Rogerson A. Adriamycin-loaded niosomes–drug entrapment,
stability and release. J Microencap 1987;4:321-8.
41. Yoshioka T, Stermberg B, Florence AT. Preparation and properties
of vesicles (niosomes) of sobitan monoesters (Span 20, 40, 60, and
80) and a sorbitan triester (Span 85). Int J Pharm 1994;105:1-6.
42. Rogerson A, Cummings J, Willmo N, Florence AT. The distribu-
tion of doxorubicin in mice following administration in niosomes.
J Pharm Pharmacol 1988;40:337-42.
Source of Support: Nil, Conict of Interest: Nil.
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Vesicles prepared from self-assembly of hydrated non-ionic surfactants molecules are called niosomes. These types of vesicles were first reported in the cosmetic industries. Niosomes exhibit more chemical stability than liposomes (a phospholipids vesicle) as non-ionic surfactants are more stable than phospholipids. Non-ionic surfactants used in formation of niosomes are polyglyceryl alkyl ether, glucosyl dialkyl ether, crown ether, polyoxyethylenealkyl ether, ester-linked surfactants, and steroid-linked surfactants and a spans, and tweens series. Niosomes preparation is affected by processes variables, nature of surfactants, and presence of membrane additives and nature of drug to be encapsulated. This review article presents an overview of theoretical concept of factors affecting niosome formation, techniques of noisome preparation, characterization of niosome, applications, limitations and market status of such delivery system.
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The self assembly of non-ionic surfactants into vesicles was first reported in the seventies by researchers in the cosmetic industry. Since then a number of groups world wide have studied non-ionic surfactant vesicles (niosomes) with a view to evaluating their potential as drug carriers. This article presents a summary of the achievements in the field to date. Niosomes may be formed form a diverse array of amphiphiles bearing sugar, polyoxyethylene, polyglycerol, crown ether and amino acid hydrophilic head groups and these amphiphiles typically possess one to two hydrophobic alkyl, perfluoroalkyl or steroidal groups. The self assembly of surfactants into niosomes is governed not only by the nature of the surfactant but by the presence of membrane additives, the nature of the drug encapsulated and the actual method of preparation. Methods of niosome preparation and the number of different morphologies that have been identified are detailed. The influence of formulation factors on niosome stability is also examined as are methods to optimise drug loading. In vivo these systems have been evaluated as immunological adjuvants, anti-cancer/anti-infective drug targeting agents and carriers of anti-inflammatory drugs. Niosomes have also been used in diagnostic imaging. Efforts to achieve transdermal and ophthalmic drug delivery with some formulations are also discussed.