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“LIPOSOMES- A NOVEL VESSICULAR CARRIER”
Presented By
Mr. Bhosale Pramod
Motiram
M. Pharm (SEM- I)
Pharmaceutics
Roll No-02
Guided By-
Prof. A. W. Ambekar
M. Pharm.
Pharmaceutics
.
A Seminar on
DR.VITHALRAO VIKHE PATIL FOUNDATION’S
COLLEGE OF PHARMACY, AHMEDNAGAR.
1
 Introduction
 Advantages & Disadvantages
 Mechanism of liposomes action
 Classification
 Types Of Liposomes
 Method of Liposome Preparation
 Evalution of Liposomes
 Applications
 Recent Advances
 Some marketed Preparation
2
 Liposomes are simple microscopic , concentric bi-layered vesicles in which an
aqueous volume is entirely enclosed by a membranous lipid bi-layer mainly
composed of phospholipids and cholesterol.
 Liposomes were discovered by Bhangam and co-workers in 1960’s in England.
 The size of a liposome is upto 20 nm
 Liposomes are the drug carrier loaded with great variety of molecules such as small
drug molecules, proteins, nucleotides & even plasmids.
 Liposomes can be produced from cholesterols, non toxic
surfactants,sphingolipids,glycolipids,long chain fatty acids & even membrane
proteins.
3
4
 ADVANTAGES:
 Biocompatibility and Biodegradability.
 Easy to manufacture.
 Targeted drug delivery
 Prolonged circulation in stealth mode
 Able to protect encapsulated drug from degradation.
 DISADVANTAGES:
 Poor stability
 High manufacturing cost
 Poor loading capacity
 Challenging sterilization
 Poor reproducibility
5
6
Outside
of the
cell.
Liposome
Inside
of
cell.
Inside
of
cell.
Drug
releasing
into cell
Cell
membrane
Cell
membrane
Phospholipids of liposome
are incorporated into cell
membrane
Classification
BASED ON STRUCTURE :
 Multi-lamellar large vesicles (>0.5 µm) MLV
 Oligo-lamellar vesicles (0.1 – 1µm) OLV
 Uni-lamellar vesicles ( All size ranges) UV
 Small uni-lamellar vesicles (20 – 100 nm) SUV
 Medium size uni-lamellar vesicles (>100 nm) MUV
 Large uni-lamellar vesicles (>100 nm) LUV
 Giant uni-lamellar vesicles (>1 µm) GUV
 Multi-vesicular vesicles (>1 µm) MV
BAESD ON LIPOSOMAL FORMATION:
 Reverse phase evaporation REV
 Multi-lamellar vesicle by REV MLV-REV
 Stable plurilamellar vesicle SPLV
 Frozen and thawed MLV FATLV
 Vesicles prepared by extrusion techniques VET
 Dried reconstituted vesicles DRV
7
 There are two type of liposomes based on their structure.
a) Unilamellar liposomes: Unilamellar vesicles has a single phospho-lipid bilayer
sphere enclosing aqueous solution.
b) Multilamellar Liposomes: Multilamellar vesicles have onion structure. Typically,
several Unilamellar vesicles will form one inside the other in diminishing size,
creating a multilamellar structure of concentric phospholipid spheres separated by
layers of water.
8
a) Handshaking Method-
b) Sonication Method-
9
There are two sonication techniques:
i) Probe Sonication
ii) Bath Sonicator
c) Reverse Phase Evaporation Method:-
Lipid organic solvent aqueous solution
mix
sonicate
formation of w/o emulsion
evaporate to remove the organic solvent
Lipids form a phospholipid bilayer
vigorous shaking
water droplets collapse
formation of LUV’s.
10
d) Freeze Dried Rehydration Method:-
 It is obtained from Pre-formed liposomes.
 Small macromolecule can be achieved in this.
 During dehydration, lipid bilayer & material are
encapsulated in liposomes.
 They are braught in closed contact.
 Aqueous phase should be added in small portion to
get Rehydration Method.
11
 Evaluation could be classified into three broad
Categories,
1. Physical
2. Chemical
3. Biological parameters.
Techniques:-
 Microscopic Techniques
1. Optical Microscopy
2. Cryo-Transmission Electron Microscopy Techniques (cryo-
TEM)
 Diffraction and Scattering Techniques
 Hydrodynamic Techniques
12
 Formulation of antineoplastic drugs into liposomes will significantly enhances
systemic circulation time.
 Decreased toxicity by reducing free drug levels in plasma.
 Increased EPR (Enhanced permeability &retention effect).
 Decreased cardio-toxicity of Doxorubicin by liposomal encapsulation.
 Positively charged liposomes have enhanced immunogenic properties for vaccines
and hypersensitivity responses.
 PEGylated liposomes are recent advancement in brain targeted drug delivery
systems.
 Liposomes used as drug carriers for efficient treatment of neuronal inflammation
(Methyl prednisolone) & others exhibited superior anti inflammatory activity than
Other activity. 13
1) Liposomes in Cancer
2) Sustain release Liposomes
3) Liposomes in Gene Delivery
4) Lipsomes for Protein & Peptide Delivery
5) Liposome for Oral administration
6) PH Sensitive Liposomes
7) Antibody Mediated targeting liposomes
14
Brand Name Drug Category Route
Doxil Doxorubicin Anticancer Intravenous
Daunoxome Daunorubicin Anticancer Intravenous
Epaxel Hepatitis A
vaccine
Protection
against Hepatitis
Subcutaneous
Elamax Lidocaine Local anesthetic Topical
Mikasome Amikacine Antibacterial Intravenous
15
 Vyas S.P., Khar K.R. Trageted and Controlled drug delivery. CBS Publisher and distributors, New Delhi. 2002; 1;181,187.
 Riaz.M. Liposomes preparation method pakisthan journal of pharmaceutical sciences. 1996; 19(1); 65-77.
 Lipowsky R. Nature 1992; 349: 475–481. Lasic DD. Elsevier Amsterdam 1993;231.
 Svetina S and B Zeks. Biophys Acta 1982; 44: 979–986.
 Alving C. R. et al., Therapy of Leishmaniasis: Superior Efficacies of Liposome‐Encapsulated Drugs, Proc. Natl. Acad. Sci.
(USA),1978, 75, 2959–2963.
 Lopez‐Berestein G. et al., Liposomal Amphotericin B for the treatment of Systemic Fungal Infections in Patients with
Cancer: A Preliminary Study, J. Infect. Dis., 1985, 151, 704–710.
 Gregoriadis G. Genetic Vaccines: Strategies for Optimization, Pharm. Res., 1998, 15, 661–670.
 Spanjer H. H., Scherphof G., Targetting of lactosylceramidecontaining liposomes to hepatocytes in vivo. Biochim
Biophys.Acta, 1983, 174, 40‐47.
 Nicolau C., Legrand A., Grosse E., Liposomes as carriers for in vivo gene transfer and expression, Methods in
enzymology,1987, 149, 157‐176.
 www.slideshare.com
 www.authorstream.com 16
THANK YOU…
17

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Bhosale seminar

  • 1. “LIPOSOMES- A NOVEL VESSICULAR CARRIER” Presented By Mr. Bhosale Pramod Motiram M. Pharm (SEM- I) Pharmaceutics Roll No-02 Guided By- Prof. A. W. Ambekar M. Pharm. Pharmaceutics . A Seminar on DR.VITHALRAO VIKHE PATIL FOUNDATION’S COLLEGE OF PHARMACY, AHMEDNAGAR. 1
  • 2.  Introduction  Advantages & Disadvantages  Mechanism of liposomes action  Classification  Types Of Liposomes  Method of Liposome Preparation  Evalution of Liposomes  Applications  Recent Advances  Some marketed Preparation 2
  • 3.  Liposomes are simple microscopic , concentric bi-layered vesicles in which an aqueous volume is entirely enclosed by a membranous lipid bi-layer mainly composed of phospholipids and cholesterol.  Liposomes were discovered by Bhangam and co-workers in 1960’s in England.  The size of a liposome is upto 20 nm  Liposomes are the drug carrier loaded with great variety of molecules such as small drug molecules, proteins, nucleotides & even plasmids.  Liposomes can be produced from cholesterols, non toxic surfactants,sphingolipids,glycolipids,long chain fatty acids & even membrane proteins. 3
  • 4. 4
  • 5.  ADVANTAGES:  Biocompatibility and Biodegradability.  Easy to manufacture.  Targeted drug delivery  Prolonged circulation in stealth mode  Able to protect encapsulated drug from degradation.  DISADVANTAGES:  Poor stability  High manufacturing cost  Poor loading capacity  Challenging sterilization  Poor reproducibility 5
  • 7. Classification BASED ON STRUCTURE :  Multi-lamellar large vesicles (>0.5 µm) MLV  Oligo-lamellar vesicles (0.1 – 1µm) OLV  Uni-lamellar vesicles ( All size ranges) UV  Small uni-lamellar vesicles (20 – 100 nm) SUV  Medium size uni-lamellar vesicles (>100 nm) MUV  Large uni-lamellar vesicles (>100 nm) LUV  Giant uni-lamellar vesicles (>1 µm) GUV  Multi-vesicular vesicles (>1 µm) MV BAESD ON LIPOSOMAL FORMATION:  Reverse phase evaporation REV  Multi-lamellar vesicle by REV MLV-REV  Stable plurilamellar vesicle SPLV  Frozen and thawed MLV FATLV  Vesicles prepared by extrusion techniques VET  Dried reconstituted vesicles DRV 7
  • 8.  There are two type of liposomes based on their structure. a) Unilamellar liposomes: Unilamellar vesicles has a single phospho-lipid bilayer sphere enclosing aqueous solution. b) Multilamellar Liposomes: Multilamellar vesicles have onion structure. Typically, several Unilamellar vesicles will form one inside the other in diminishing size, creating a multilamellar structure of concentric phospholipid spheres separated by layers of water. 8
  • 9. a) Handshaking Method- b) Sonication Method- 9
  • 10. There are two sonication techniques: i) Probe Sonication ii) Bath Sonicator c) Reverse Phase Evaporation Method:- Lipid organic solvent aqueous solution mix sonicate formation of w/o emulsion evaporate to remove the organic solvent Lipids form a phospholipid bilayer vigorous shaking water droplets collapse formation of LUV’s. 10
  • 11. d) Freeze Dried Rehydration Method:-  It is obtained from Pre-formed liposomes.  Small macromolecule can be achieved in this.  During dehydration, lipid bilayer & material are encapsulated in liposomes.  They are braught in closed contact.  Aqueous phase should be added in small portion to get Rehydration Method. 11
  • 12.  Evaluation could be classified into three broad Categories, 1. Physical 2. Chemical 3. Biological parameters. Techniques:-  Microscopic Techniques 1. Optical Microscopy 2. Cryo-Transmission Electron Microscopy Techniques (cryo- TEM)  Diffraction and Scattering Techniques  Hydrodynamic Techniques 12
  • 13.  Formulation of antineoplastic drugs into liposomes will significantly enhances systemic circulation time.  Decreased toxicity by reducing free drug levels in plasma.  Increased EPR (Enhanced permeability &retention effect).  Decreased cardio-toxicity of Doxorubicin by liposomal encapsulation.  Positively charged liposomes have enhanced immunogenic properties for vaccines and hypersensitivity responses.  PEGylated liposomes are recent advancement in brain targeted drug delivery systems.  Liposomes used as drug carriers for efficient treatment of neuronal inflammation (Methyl prednisolone) & others exhibited superior anti inflammatory activity than Other activity. 13
  • 14. 1) Liposomes in Cancer 2) Sustain release Liposomes 3) Liposomes in Gene Delivery 4) Lipsomes for Protein & Peptide Delivery 5) Liposome for Oral administration 6) PH Sensitive Liposomes 7) Antibody Mediated targeting liposomes 14
  • 15. Brand Name Drug Category Route Doxil Doxorubicin Anticancer Intravenous Daunoxome Daunorubicin Anticancer Intravenous Epaxel Hepatitis A vaccine Protection against Hepatitis Subcutaneous Elamax Lidocaine Local anesthetic Topical Mikasome Amikacine Antibacterial Intravenous 15
  • 16.  Vyas S.P., Khar K.R. Trageted and Controlled drug delivery. CBS Publisher and distributors, New Delhi. 2002; 1;181,187.  Riaz.M. Liposomes preparation method pakisthan journal of pharmaceutical sciences. 1996; 19(1); 65-77.  Lipowsky R. Nature 1992; 349: 475–481. Lasic DD. Elsevier Amsterdam 1993;231.  Svetina S and B Zeks. Biophys Acta 1982; 44: 979–986.  Alving C. R. et al., Therapy of Leishmaniasis: Superior Efficacies of Liposome‐Encapsulated Drugs, Proc. Natl. Acad. Sci. (USA),1978, 75, 2959–2963.  Lopez‐Berestein G. et al., Liposomal Amphotericin B for the treatment of Systemic Fungal Infections in Patients with Cancer: A Preliminary Study, J. Infect. Dis., 1985, 151, 704–710.  Gregoriadis G. Genetic Vaccines: Strategies for Optimization, Pharm. Res., 1998, 15, 661–670.  Spanjer H. H., Scherphof G., Targetting of lactosylceramidecontaining liposomes to hepatocytes in vivo. Biochim Biophys.Acta, 1983, 174, 40‐47.  Nicolau C., Legrand A., Grosse E., Liposomes as carriers for in vivo gene transfer and expression, Methods in enzymology,1987, 149, 157‐176.  www.slideshare.com  www.authorstream.com 16