Liposome Drug Delivery System

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
Phospholipids
Classification of liposomes
Structural parameters:
Multi lamellar vesicles.
Oligo lamellar vesicles.
Unilamellar vesicles.
Small unilamellar vesicles.
Large uni lamellar vesicles.
Multi vesicular vesicles.
METHOD OF PREPARATION:
Single or oligo lamellar vesicles by REV.

Multi lamellar vesicles by REV.
Vesicles prepared by extrusion method.
Dehydration method.
BASED ON COMPOSITION AND APPLICATION:
Conventional liposomes
Fusogenic liposomes.
Long circulatory liposomes
Ph sensitive liposomes.
Cationic liposomes.
Immuno liposome .
CLASSIFICATION
METHOD OF LIPOSOMS PREPARATION
Passive loading active loading
 mechanical dispersion method

 solvent dispersion method
 detergent removal method
Mechanical dispersion methods
 lipid film hydration by hand shaking,

non handshaking method.
 micro emulsification.
 french pressure.
 membrane extrusion.
 dried reconstituted.
 freeze-thawed.
DETERGENT REMOVAL METHOD:
Detergent removal from mixed micelles.

Dialysis.
Column chromatography.
Dilution.
Solvent dispersion methods:
 Ethanol injection.
 Ether injection.
 Double emulsion.
 Reverse phase evaporation.
MATERIALS USED FOR
PREPARATION OF LIPOSOME
1.Natural phospholipids
2.Synthetic phospholipids
3. Sphingolipids
4. Glycosphingolipids
5.Steroid
6. Polymeric material
Thin film hydration using hand
shaking &non shaking method
French pressure cell
Sonication method
Membrane extrusion method
Freeze taw liposomes & dried
reconstituted vesicles
Ethanol &ether injection method
Reverse phase evaporation
vesicles
ACTIVE LOADING TECHNIQUE
DETERGENT REMOVAL MEHODS
STAGE:1
At low concentrations Detergent
Lipid vesicular Lipid Water
Size of vesicles
STAGE:2
Critical detergent concentrations Membrane structure is unstable
Transforms gradually into micelles
STAGE:3
All Lipids exists in mixed micelle Form
DIALYSIS
Detergents High CMC
Removal is facilitated
Egg Pc + Sodium cholate dialysis Formation of vesicles
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.
CHACTERIZATION OF
LIPOSOMES
Internal volume.
Encapsulation efficiency.
Lamellarisity.
Size & size distribution..
Phase behaviour of liposomes
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.
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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LIPOSOMAL DRUG DELIVERY

1) Effective encapsulation of both small and large

2) Prolonging and targeting release of therapeutic agents

3) Minimizing clinical drug dose and reducing toxicity

4 Increased stability via encapsulation

Single or oligo lamellar vesicles by REV.

Long circulatory liposomes

Passive loading active loading

 mechanical dispersion method

 lipid film hydration by hand shaking,

Detergent removal from mixed micelles.

Transforms gradually into micelles

Egg Pc + Sodium cholate dialysis Formation of vesicles

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