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10/11/014 1
ANIRBAN SAHA
AMITY INSTITUTE OF PHARMACY
M.Pharm (Pharmaceutics)
Semester- 2
Enrollment No: A10647014005
 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.
10/11/2014 2
10/11/2014 3
COMPOSITION
10/11/2014 4
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.
ADVANTAGES
10/11/2014 5
 Non-toxic.
 Biodegradable.
 Non-immunogenic.
 Lowers systemic toxicity.
 Targeted delivery.
 Protection of sensitive drug molecules.
 Enhance drug solubilisation ( Amphoterecin, Cyclosporins).
 Improved pharmacokinetic effects.
• 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
10/11/2014 6
COMMONLY USED
PHOSPHOLIPIDS
NATURAL
PHOSPHATIDYL
CHOLINE
PHOSPHATIDYL
ETHANOLAMINE
PHOSPHATIDYL
SERINE
SYNTHETIC
DIOLEOYL
PHOSPHATIDYL
CHOLINE
DISTEAROYL
PHOSPHOTIDYL
CHOLINE
DIOLEOYL
PHOSPHATIDYL
ETHANOLAMINE
COMMONLY USED
PHOSPHOLIPIDS
10/11/2014 8
10/11/2014 8
BASED ON PREPARATION METHOD
10/11/2014 10
10/11/2014 11
General Method Of Liposome Formation
All the methods of preparing liposomes involves 3 to 4 steps.
Analysis of final product
Purification of resultant liposomes
Dispersion of lipids in aqueous media
Drying down lipids from organic solvents
10/11/2014 13
METHODS OF LIPOSOME
PREPARATION
PASSIVE LOADING
Involves loading of the entrapped
agents before or during the
manufacturing procedure
ACTIVE OR REMOTE LOADING
Certain types of compounds with
ionizable groups and those with
both lipid and solubility , can be
introduced into the liposomes after
the formation of the intact vesicles
10/11/2014 14
Classes of Liposomes
CONVENTIONAL LONG CIRCULATING
IMMUNO CATIONIC
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
10/11/2014 16
Lack long term stability (short shelf life)
 Physical and chemical instability
 Freeze dry and pH adjustment
Low “Pay Load” - Poor Encapsulation
 Drugs and drugs without opposite charge
 Modifications
10/11/2014 17
10/11/2014 18
 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/articlesta
ndard/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
10/11/2014 19
10/11/2014 20

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Liposomes- A Novel Drug Delivery System

  • 1. 10/11/014 1 ANIRBAN SAHA AMITY INSTITUTE OF PHARMACY M.Pharm (Pharmaceutics) Semester- 2 Enrollment No: A10647014005
  • 2.  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. 10/11/2014 2
  • 4. COMPOSITION 10/11/2014 4 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.
  • 5. ADVANTAGES 10/11/2014 5  Non-toxic.  Biodegradable.  Non-immunogenic.  Lowers systemic toxicity.  Targeted delivery.  Protection of sensitive drug molecules.  Enhance drug solubilisation ( Amphoterecin, Cyclosporins).  Improved pharmacokinetic effects.
  • 6. • 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 10/11/2014 6
  • 10. BASED ON PREPARATION METHOD 10/11/2014 10
  • 12. General Method Of Liposome Formation All the methods of preparing liposomes involves 3 to 4 steps. Analysis of final product Purification of resultant liposomes Dispersion of lipids in aqueous media Drying down lipids from organic solvents
  • 13. 10/11/2014 13 METHODS OF LIPOSOME PREPARATION PASSIVE LOADING Involves loading of the entrapped agents before or during the manufacturing procedure ACTIVE OR REMOTE LOADING Certain types of compounds with ionizable groups and those with both lipid and solubility , can be introduced into the liposomes after the formation of the intact vesicles
  • 15. Classes of Liposomes CONVENTIONAL LONG CIRCULATING IMMUNO CATIONIC
  • 16. 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 10/11/2014 16
  • 17. Lack long term stability (short shelf life)  Physical and chemical instability  Freeze dry and pH adjustment Low “Pay Load” - Poor Encapsulation  Drugs and drugs without opposite charge  Modifications 10/11/2014 17
  • 19.  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/articlesta ndard/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 10/11/2014 19

Editor's Notes

  1. LIPOSOMES PAGE NO 1