LIPOSOMAL DRUG DELIVERY

SYSTEM
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LIPOSOMES
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ADVANTAGES
1) Effective encapsulation of both small and large
molecules with a wide range of hydrophobicity levels and
Pk.

2) Prolonging and targeting release of therapeutic agents
by modification of liposome surface


3) Minimizing clinical drug dose and reducing toxicity
effects

4 Increased stability via encapsulation


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Phospholipids
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Classification of liposomes


Structural parameters:
Multi lamellar vesicles.
Oligo lamellar vesicles.
Unilamellar vesicles.
Small unilamellar vesicles.
Large uni lamellar vesicles.
Multi vesicular vesicles.




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METHOD OF PREPARATION:

Single or oligo lamellar vesicles by REV.
Multi lamellar vesicles by REV.
Vesicles prepared by extrusion method.
Dehydration method.


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BASED ON COMPOSITION AND APPLICATION:


Conventional liposomes

Fusogenic liposomes.

Long circulatory liposomes

Ph sensitive liposomes.

Cationic liposomes.

Immuno liposome .
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CLASSIFICATION
METHOD OF LIPOSOMS PREPARATION

Passive loading active loading

mechanical dispersion method
solvent dispersion method
detergent removal method
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Mechanical dispersion methods

lipid film hydration by hand shaking,
non handshaking method.
micro emulsification.
french pressure.
membrane extrusion.
dried reconstituted.
freeze-thawed.


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DETERGENT REMOVAL METHOD:

Detergent removal from mixed micelles.
Dialysis.
Column chromatography.
Dilution.
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Solvent dispersion methods:

Ethanol injection.
Ether injection.
Double emulsion.
Reverse phase evaporation.

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MATERIALS USED FOR
PREPARATION OF LIPOSOME
1.Natural phospholipids
2.Synthetic phospholipids
3. Sphingolipids
4. Glycosphingolipids
5.Steroid
6. Polymeric material


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Thin film hydration using hand
shaking &non shaking method

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French pressure cell
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Sonication method
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Membrane extrusion method
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Freeze taw liposomes & dried
reconstituted vesicles
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Ethanol &ether injection method
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Reverse phase evaporation
vesicles
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ACTIVE LOADING TECHNIQUE
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DETERGENT REMOVAL MEHODS
STAGE:1
At low concentrations Detergent
Lipid vesicular Lipid Water

STAGE:2
Size of vesicles
Critical detergent concentrations Membrane structure is unstable
Transforms gradually into micelles
STAGE:3
All Lipids exists in mixed micelle Form
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DIALYSIS
Detergents
High CMC
Removal is facilitated
Egg Pc + Sodium cholate
dialysis
Formation of vesicles
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Stealth Liposomes
Major problem in use of liposomes for
delivery of drug by injection in to blood
stream is the specific uptake of the
liposome by reticuloendothelial system .
avoid the uptake by the RES are called
stealth liposomes.
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CHACTERIZATION OF
LIPOSOMES
Internal volume.
Encapsulation efficiency.
Lamellarisity.
Size & size distribution..
Phase behaviour of liposomes

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Therapeutic application
Liposome as drug/protein delivery vehicles.
Liposomes in anti microbial ,anti fungal
anti viral therapy.
Liposome in tumour therapy.
Liposomes in gene delivery.
Liposomes in immunology.
Liposomes as radiopharmaceutical and
radiodiagnostic carriers.
Liposoms in cosmetics and dermatology.
Liposomes in bioreactor technology.

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REFERENSES
REFERNCES:
Alpes H., Allmann K., Plattner H., Reichert J., Rick R. and Schulz S. (1986). Biochim.
Biophys. Acta. 862: 294.
Bangham A.D., Standish M.M. and Watlins J.C. (1965). J. Mol. Biol. 13: 238.
Bangham A.D., Hill M.W. and Miller N.G.A. (1974). In: Methods in Membrane Biology
(Koln N.D., ed.) Plenum. N.Y., Vol.1, p.l.
Batzri S. and Korn E.D. (1973). Biochim. Biophy. Acta. 298: 1015.
Cestaro B., Pistolesi E., Hershkowitz N. and Galt S. (1982). Biochim. Biophys. Acta.
685:
Cullis R.P., Hope M.J., Bally M.B., Madden T.D. and Janoff AS. (1987). In:
Liposomes from Biophysics to Therapeutics (Ostro M. J., Ed.) Marcel Dekker, N.Y.,
Chapter
Deamer D. and Bangham A.D. (1976). Biochim. Biophys. Acta. 443: 629.
Enoch H.G. and Strittmatter P. (1979). Proc. Natl. Acad. Sci. USA. 76: 145.
Fiona J., James A., Hayward A. and Chapman D. (1987). Biochim. Biophys.
Acta.341.
Friese J. (1984). In: Liposome Technology (Gregoriadis G., ed.) CRC Press, Florida,

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