Upload
archibald-bradley
View
225
Download
0
Embed Size (px)
Citation preview
They represents a structure similar to liposome
and hence they can represent alternative vesicular
systems with respect to liposomes.
a) Niosomes are used as an alternative to
liposomes,
which exhibit certain disadvantages such as :
They are expensive
Their ingredients like phospholipids are
chemically unstable because of their
predisposition to oxidative degradation
They require special storage and handling
Purity of natural phospholipids is variable.
b) 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 neutral or charged double-chain
phospholipids
Method of preparation
A. Ether injection method a Mixture of Span 60 , cholesterol and dicetyl
phosphate slowly dissolved in diethyl ether then
injected slowly through a needle in to warm
aqueous phase maintained at 60 °C that
consisting of drug.
Vaporization of ether leads to formation of
unillamellar niosomes
In niosomes, the vesicles forming lipid is a non-ionic
surfactant such as Span 60 which is stabilized by
addition of cholesterol and small amount of anionic
surfactant such as dicetyl phosphate.
B. Thin film hydration technique
Mixture of Span 60 , cholesterol and dicetyl
phosphate are dissolved in a volatile organic
solvent (chloroform) in a round bottom flask.
The organic solvent is removed at room
temperature (20°C) using rotary evaporator
leaving a thin layer of solid mixture deposited on
the wall of the flask.
The dried surfactant film can be rehydrated
with aqueous phase at 60°C with gentle agitation.
This process forms typical multillamellar niosomes.
C. Sonication Drug solution in phosphat buffer is added to the
Mixture of Span 60 , cholesterol and dicetyl
phosphate
The mixture is probe sonicated at 60°C for 3
minutes which lead to formation of unillaminar
niosomes
Separation of Unentrapped Drug
The removal of unentrapped solute from the vesicles
can be accomplished by :
A.Dialysis
B.Gel Filtration
C.Centrifugation.
the properties of niosomes depends on the
composition of the bilayer:
As the concentration of cholesterol increases,
entrapment efficiency decreases.
The entrapment efficiency increases with increase
in the concentration and lipophilicity of
surfactant.
• As HLB value of surfactant decreased give
highest percent entrapment, that Span 60 (HLB
= 4.7) gave highest percent entrapment than
Span 85 (HLB = 9.8)
Targeting
Sustained Release
Localized Drug Action
since their size and low penetrability through
epithelium keeps the drug localized at the site of
administration. results in enhancement of efficacy
and reduces its systemic toxic effects
Pharmaceutical Applications
niosomes can forms from proniosomes by coating a
water-soluble carrier such as sorbitol or maltodextrin
with surfactant.
Where the mixture of maltodextrin and surfactant
is dried to form a free flowing powder, in which each
water-soluble particle is covered with a thin film of
dry surfactant. This preparation is termed
“Proniosomes”.
The niosomes are produced by the rehydration of
Proniosomes by addition of warm water at T > Tc and
brief agitation.
Transfersomes are complex vesicles that have
extremely flexible & self-regulating membranes,
which makes the vesicle very deformable.
Transfersome vesicle can cross microporous
barriers efficiently, even if the porous are much
smaller than the vesicles size.
Transfersome consists of natural phospholipids
suspended in a water-buffered solution containing
drug & biocompatible surfactants (sodium cholate).
Similar to a liposome, a Transfersome has a lipid
bilayer that surrounds an aqueous core.
1. Liposomes are made of phospholipids and to
improve the stability of such vesicles, cholesterol is
included in the bilayer as membrane (stiffening
agent) which lead to more rigid, less flexible and
less permeable lipid bilayers.
2. The liposome that applied locally have crossed the
skin barrier in a low transport rate and distributed
between the cells in building blocks (ceramic
layer).
3. The liposome too large to enter the blood vessels;
locally they are utilized in peripheral tissues below
the application site
Mechanism of Transfersome
penetration: The skin is a nanoporous barrier that only permit the
passage of smaller particles.
Thus the passage of a Transfersome across the skin is
due to vesicle membrane flexibility, hydrophilicity,
and the ability to perforate the skin barrier.
Explanation of High efficiency of Transfersome
transport across the skin compared to liposomes
(rigid vesicles)
• Ultradeformable, lipid vesicle penetrating a
narrow pore, owing to the bilayer components.
•When a suspension of Transfersome
vesicles is placed on the surface of the
skin, the water evaporates from the
skin surface and the vesicles start to
dry out.
• Due to the strong hydrophilicity of Transfersome
ingredients, the vesicles are attracted to the areas
of higher water content in the narrow gaps
between adjoining cells in the skin.
•The phenomenon, together with the vesicle's
extreme ability to deform, enables Transfersomes
to change their shape, fit the channels, move
across the skin barrier and reach regions of high
water content in the deeper skin layers.
• Thus, Transfersomes bypass the cutaneous
capillary and reach the subcutaneous tissue and
the vesicle arrive into the systemic blood
circulation.