Method For Drug Loaded Niosomes Development
Niosomes were prepared by a modified ethanol injection method. The required amounts of
phospholipids and cholesterol were dissolved in ethanol and the lipophilic drug was added to
the organic phase. The resulting organic phase was injected by means of a syringe pump to
the 45 ± 2 °C aqueous phase (The hydrophilic drug was added to the aqueous phase) under
magnetic stirring. Spontaneous niosomes formation occurred as soon as ethanolic solution
was in contact with the aqueous phase. The niosomes suspension was then kept under stirring
for 1h room temperature to remove the traces of solvent unloaded drug was removed by
ultracentrifugation of niosomes suspension at 60,000 rpm for 1 hour. The obtained niosomes
were dispersed in phosphate buffer saline (PBS) and stored at + 4°C.
CHARACTERIZATION OF NIOSOMES SYSTEMS
Drug-Excipient Compatibility Studies
In drug-excipients compatibility studies, the samples which were kept at various accelerated
conditions, were withdrawn and carried out physical characteristics evaluation like color
change at different intervals. From the results of compatibility studies, we observed that
there was no incompatibility in drugs alone or with excipients.
FT-IR Spectrophotometeric Study
The FT-IR spectroscopy study was carried out to check the compatibility between the drug
and the polymers used for the preparation of gel. The FT-IR was performed for drug, polymer
and physical mixtures of drug and polymer. The spectra obtained from FT-IR spectroscopy
studies at wavelength ranging from 4000 cm-1 to 400 cm-1. There was no appearance and
disappearance of any characteristic peaks and this showed that there was no interaction
between the drug and polymers.
Morphological Study By Scanning Electron Microscopy
Niosomes morphology was studied by SEM. Negative-stain SEM images showed that
niosomes obtained were spherical shaped and composed of several phospholipid bilayers
(i.e., MLVs), which could have an impact on drug-release. According to SEM, niosomes
ranged in size from 200 to 400 nm. No drug crystals were visible in SEM, regardless of the
preparation technique or the loaded drug and clearly showed an interaction between drug and
polymer.
Percentage Drug Entrapment
The average percent drug entrapment efficiency of optimized formulation showed a
maximum drug entrapment of 72% and 69% for 5FU and TTN respectively.
In Vitro Release Study of Niosomes
An In Vitro release study was performed on nine different formulas of drug-loaded niosomes.
The studied formulas were selected in order to investigate the phospholipid concentration and
cholesterol content impact on drug-release profile, these being the main parameters that
influenced size and encapsulation efficiencies.
In Vitro drug release studies of drug-loaded niosomes were conducted for a period of 8 h
using dialysis method, entire formulations were performed in skin pH to evaluate the release.
From the release profile, it was observed that the phospholipid-concentration impact on drug
release profile, these being the main parameters that influenced size and encapsulation
efficiencies. Influenced the drug release from the niosomes. Release of optimized niosomes
was better than other formulations. It was probably due to the presence of phospholipid
concentration and optimum size of niosomes.
Influence of Phospholipid Concentration on the Vesicle
Size and encapsulation efficiency Phospholipid concentration showed a positive effect on
niosomes encapsulation efficiencies. The influence of the phospholipid concentration on
encapsulation efficiency and vesicle size has been studied. It was found that when
phospholipid concentration was increased from 20 to 60 mg/ml, 5-FU encapsulation
efficiencies were nearly doubled (from 34 to 72 %). Similar encapsulation results have been
obtained for TTN efficiency of niosomes was found to be in the range of 42 to 69%. It has
been reported that the thickness of the lipid surface of niosomes increases with the increasing
amount of phospholipid used in formulation
Selection of Niosomes
FT-IR graphs of the pure drug, soya lecithin, cholesterol and their physical mixtures was
performed and the FT-IR graphs it is noted that there is no possible interactions between
drugs and the other. The average percent drug entrapment efficiency of optimized showed a
maximum drug entrapment of 72.86% and 69.70% for 5FU and TTN respectively.
Dissolution data shows that F6 displayed higher drug release of 72 and 77% for for 5FU and
TTN respectively for 8 hours and phospholipid concentration showed a positive effect on
niosomes encapsulation efficiencies. On the basis of above mentioned data F6 were selected
as optimized formulation

We Claim(10):
1. A niosomes comprising: Vesicles encapsulated water-soluble drug (5FU) in the aqueous
spaces and lipid-soluble drug (TTN) incorporated into the lipid membranes.
2. The niosomes according to claim 1 prepared by modified ethanol injection method.
3. The niosomes according to claim 2 wherein the formulation F1, drug(s) 5FU (500mg) &
TTN (0.100mg), cholesterol: phospholipid ratio 1:5, by modified ethanol injection
method.
4. The niosomes according to claim 2 wherein the formulation F2, drug(s) 5FU (500mg) &
TTN (0.100mg), cholesterol: phospholipid ratio 1:10, by modified ethanol injection
method.
5. The niosomes according to claim 2 wherein the formulation F3, drug(s) 5FU (500mg) &
TTN (0.100mg), cholesterol: phospholipid ratio 1:15, by modified ethanol injection
method.
6. The niosomes according to claim 2, drug(s)-excipients compatibility studies reveal that
there was no incompatibility in drug(s)s alone or with excipients.
7. The niosomes according to claim 2 FT-IR study showed that there was no interaction
between the drug(s)s and polymers.
8. The niosomes according to claim 2, The SEM reveal that no interaction between drug(s)
and polymer.
9. The niosomes according to claim 2, selected niosomes were subjected for further
formulation development.
10. The niosomes according to claim 2, % drug(s) content of 5FU and TTN loaded niosomes
were found in formulation (F3) having, drug(s) 5FU (500mg) & TTN (0.100mg),
cholesterol: phospholipid ratio 1:15, can be preferred because of maximum drug(s)
release and highest % drug(s) content.