LIPOSOMES - A Novel

Drug Delivery System

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INTRODUCTION
Liposomes are the simple microscopic vesicles in which
aqueous layer is enclosed by phospho lipid bilayers that
are used to transfer vaccines ,drugs ,enzymes and other
substances to targetcells or organs

Structually ,liposomes are concentric bilayerd vesicles in

which an aqueous volume is entirely enclosed by a
membraneous lipid bilayer mainly composed of natural or
synthetic phospholipids.

Can be produced from cholesterols, non toxic surfactants,

sphingolipids, glycolipids, long chain fatty acids and even
membrane proteins.

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Structure Of Liposome

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COMPOSITION

Phospholipids:
Dilauryl phosphotidyl choline (DLPC), Dimyristoyl phosphotidyl choline
(DMPC), Dipalmitoy phosphotidyl choline (DPPC), Distearoyl
phosphotidyl choline (DSPC), Dioleolyl phosphotidyl choline (DOPC),
Dilauryl phosphotidyl glycerol (DLPG), Distearoyl phosphotidyl serine
(DSPS).

Cholesterol:
Act as intercalator with phospholipids molecules.
Restrict the confirmational changes of lipids.
Membrane stabilizer.

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 ADVANTAGES

Non-toxic.
Biodegradable.
Non-immunogenic.
Lowers systemic toxicity.
Targeted delivery.
Protection of sensitive drug molecules.
Enhance drug solubilisation ( Amphoterecin,
Cyclosporins).
Improved pharmacokinetic effects.

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 DISADVANTAGES
Leakage of encapsulated drug during storage.

Short half-life.

Batch to batch variation.

Difficult in large scale manufacturing and sterilization.

Production cost is high.

Once administered, liposomes can not be removed.

Some times phospholipids undergoes hydrolysis and

oxidation reactions
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COMMONLY USED
PHOSPHOLIPIDS PHOSPHATIDYL
CHOLINE

PHOSPHATIDYL
NATURAL
ETHANOLAMINE

PHOSPHATIDYL
SERINE
COMMONLY USED
PHOSPHOLIPIDS
DIOLEOYL
PHOSPHATIDYL
CHOLINE

DISTEAROYL
SYNTHETIC PHOSPHOTIDYL
CHOLINE

DIOLEOYL
PHOSPHATIDYL
ETHANOLAMINE
TYPES

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BASED ON STRUCTURE

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BASED ON PREPARATION
METHOD

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General Method Of Liposome Formation

All the methods of preparing liposomes involves 3 to 4 steps.

Drying down lipids from organic solvents

Dispersion of lipids in aqueous media

Purification of resultant liposomes

Analysis of final product

PREPARATION METHODS

METHODS OF LIPOSOME
PREPARATION

ACTIVE OR REMOTE LOADING

PASSIVE LOADING
Involves loading of the entrapped
agents before or during the
manufacturing procedure
Certain types of compounds with
ionizable groups and those with
both lipid and aqueous solubility ,
can be introduced into the
liposomes after the formation of
the intact vesicles

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PREPARATION PROCESS

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Classes of Liposomes

CONVENTIONAL LONG CIRCULATING

IMMUNO CATIONIC
USES OF LIPOSOMES
PHARMACOKINETICS - Efficacy And Toxicity

Changes the absorbance and bio distribution

Deliver drug in desired form

Multidrug resistance

PROTECTION

Decrease harmful side effects

Change where drug accumulates in the body

Protects drug

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Problems With Liposomal Preparation Of Drugs

Lacklongtermstability(shortshelflife)

Physicalandchemicalinstability

FreezedryandpHadjustment

LowPayLoadPoorEncapsulation

Drugsanddrugswithoutoppositecharge

Modifications

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EXAMPLES

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References:

Y. Sultana., Liposomal Drug Delivery Systems: An Update Review. ,

Current Drug Delivery 2007, 4, 297-305.
Sharma Shailesh, Sharma Neelam, Kumar Sandeep, Gupta GD.,
Liposomes: Areview., Journal of Pharmacy Research 2009, 2(7),1163-
1167.
Mohammad Riaz., Liposomes Preparation Methods., Pakistan Journal
of Pharmaceutical Sciences Vol.19(1), January 1996, 65-77.
MU Uhumwangho and RS Okor., Current trends in the production and
biomedical applications of liposomes: a review ., JMBR June 2005 Vol.
4(1) 9-21.
http://www.biopharminternational.com/biopharm/data/articlestandar
d/biopharm/032002/7278/article.pdf., web, 28.01.2012
http://www.ias.ac.in/jarch/currsci/68/00000742.pdf.,web, 28.01.2012
D.D. Lasic., Applications of Liposomes., Handbook of Biological
Physics., Elsevier Science B.V.., 1995., Vol.1., 1-29

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