Liposomes are defined as phospholipid vesicles consisting of one or more concentric lipid bilayers enclosing discrete aqueous spaces. The unique ability of liposomal systems to entrap both lipophilic and hydrophilic compounds enables a diverse range of drugs to be encapsulated by these vesicles.
4. INTRODUCTION
LIPOSOME
Liposome’s are concentric bilayered vesicles
in which an aqueous core is entirely
enclosed by a membranous lipid bilayer
mainly composed of natural of synthetic
phospholipids.
Liposome’s were first produced in England
in 1961 by Alec D. Bangham, who was
studying phospholipids and blood clotting.
In which polar head groups face outwards
into the aqueous medium and the lipid
chains turns inwards to avoid the water
phase.
5. Figure 1: Scheme of a liposome
formed by phospholipids in an
aqueous solution.
8. Purpose of Liposome doses
form
Liposome's have been widely used to
enhance the efficiency of drug
delivery though various routes of
administration.
Liposome's can be utilized as carriers
to deliver drugs and thereby improve
the therapeutic effect of different types
of drugs.
9. 1. Liposome's increases efficacy and
therapeutic index of drug .
2. It increases stability via encapsulation.
3. It reduces the toxicity of encapsulating
agent.
4. They helps to reduce the exposure of
sensitive tissue to toxic drugs.
5. They have flexibility to couple with site
specific ligands to achieve active
targeting.
1. Liposome's having low solubility.
2. Short half life.
3. Sometimes phospholipids undergoes
oxidation and hydrolysis like reaction.
4. Leakage and fusion of encapsulated
drugs/molecules.
DISADVANTAGES
ADVANTAGES
10. Chemical Names: Miconazole nitrate
IUPAC Name: 1-[2-(2,4-dichlorophenyl)-2-[(2,4-dichlorophenyl)
methoxy]ethyl] imidazole
Molecular Formula: C18H15Cl4N3O4
Molecular Weight : 479.135 g/mol
Structure: miconazole nitrate
Melting point 170-185 C
Solubility in Water 0.000763 mg/ml
Color: white to off white.
Drug Profile
12. Ether injection method
Thin film hydration technique
Sonication Method
Reverse Phase Evaporation Technique (REV)
Methods of Formulation
13. Remove organic solvent at Room temperature
Thin layer formed on the Walls of flask
Film is rehydrated to form multilamellar
Liposome
Thin film hydration
technique
Dru
g
Lecithin Cholester
ol
Solvent+ + +
16. y = 0.0031x + 1E-04
R² = 0.966
0
0.005
0.01
0.015
0.02
0.025
0.03
0.035
0 2 4 6 8 10 12
Series1 Linear (Series1)
Standard of
Calibration curve
17. Entrapment
Efficiency
After the removal of
unentrapped drug by
dialysis, the entrapment
efficiency of all the
formulations was studied.
The various factors like
lipid concentration, drug
to lipid ratio, cholesterol
and lecithin content will
change the entrapment
efficiency.
Formulation No Drug : Lecithin :
Cholesterol
Ratio
Percentage
Entrapped Drug
F3 1:7:2 89.74%
F4 1:7.6:1.4 94.41%
F5 1:8.1:0.85 92.92%
Table:06 Entrapment efficiency Of Miconazole Nitrate
of Liposome Formulation
21. Stability
Analysis
Properties 1st month 3rd month 6th month
F3 F4 F5 F3 F4 F5
Entrapment
Efficiency
89.74% 94.41% 92.92% 79.55% 93.23% 90.50% Under observation
Grittiness No No No No No No Under observation
Visual aspect Moderate Good Good Under observation
22. Due to their unique properties, including low
cytotoxicity, good biocompatibility and
biodegradability, liposomes possess wide
applications in different fields including gene and
drug delivery, food and nutrition industries and
cosmetics.
For active targeting of liposome's, thermo-labile,
pH-sensitive, photo-sensitive and antibody coated
vesicles, have been designed. By passive targeting.
From the present study, it can be concluded that
Drug release rate and extent were increased.To be
used efficiently for enhancing absorption
Conclution
23. References
1. Kimball's Biology Pages, "Cell Membranes." StryerS. Biochemistry, 1981, 213.
2. Vyas S.P. & Khar R.K. “Targeted & controlled drug delivery: Novel carrier
system”. CBS publishers and distributors, 2007.
3. Gomez-Hens, A., Fernandez-Romero, J.M. “Analytical methods for the control of
liposomal
delivery systems”, Trends Anal Chem, 2006, 25,167–178.
4. Riaz M.; “review : liposomes preparation methods,” Pak. J. Pharm. Sci.; 1996, 19,
65-77.
5. Deamer D. and Bangham A.D. Biochim. Biophys. Acta.; 1976; 443: 629.
6. Frank Szoka, Jr. & Demetrios Papahadjopoulos, “Comparative properties and
methods of preparation of lipid vesicles (Liposomes),” Ann. Rev. Biophys. Bioeng.,
1980, 9, 467-508.
7. Augustin, M.A.; Hemar, Y. Nano- and micro-structured assemblies for
encapsulation of food ingredients. Chem. Soc. Rev., 2009, 38(4), 902-912.
8. Mozafari, M.R, Johnson, C., Hatziantoniou, S., Demetzos, C. Nanoliposomes
and their applications in food nanotechnology. J. Liposome Res., 2008, 18(4),
309-327.
9 Bangham, A.D. A correlation between surface charge and coagulant action
of phospholipids. Nature, 1961, 192(4808), 1197-1198.
