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NANO52
Foothill College
Introduction
• Liposome was found by Alec Bangham of Babraham
Institute in Cambridge, England in 1965.
• In 1990, drugs with liposome and Amphotericin B
were approved by Ireland.
• In 1995 America F.D.A approved liposor doxodubicin.
• Liposome is a lipid vesicle suspending in the hydro-
phase with a diameter around 0.0025~3.5um. The
membrane of liposome is made of phospholipids,
which have phosphoric acid sides to form the
liposome bilayers.
Definition
An artificial microscopic vesicle consisting
of an aqueous core enclosed in one or
more phospholipid layers, used to convey
vaccines, drugs, enzymes, or other
substances to target cells or organs.
• Presentation by:
• Shilpi Bhatnagar
• M.Pharm (Q.A.) 1st semester
Liposome Structure
PHOSPHOLIPID
BILAYER
AQUEOUS
CAVITY
Composition of liposomes:
A. Phospholipids
The most common natural phospholipid is the phospatidylcholine
(PC) is the amphipathic molecule and also known as lecithin.
A liposome is an artificially-prepared
vesicle composed of a lipid bilayer.
The liposome can be used as a vehicle
for administration of nutrients and
pharmaceutical drugs.[2] Liposomes
can be prepared by disrupting
biological membranes (such as by
sonication).
Liposomes are composed of natural
phospholipids, and may also contain
mixed lipid chains with surfactant
properties (e.g., egg
phosphatidylethanolamine). A
liposome design may employ surface
ligands for attaching to unhealthy
tissue.[3]
The major types of liposomes are the
multilamellar vesicle (MLV), the
small unilamellar vesicle (SUV), and
the large unilamellar vesicle (LUV).
Advantages of Liposomes
• Biocompatible, completely biodegradable, non-toxic, flexible,
nonimmunogenic.
• Liposomes supply both a lipophilic environment and
aqueous “milieu interne” in one system. Can protect
encapsulated drug.
• Reduce exposure of sensitive tissues to toxic drugs.
• Alter the pharmacokinetic and pharmacodynamic property of
drugs (reduced elimination, increased circulation life time).
• Flexibility to couple with site-specific ligands to achieve
active targeting (Anticancer and Antimicrobial drugs).
• Liposomes can encapsulate micro and macromolecules
such as haemoglobin, erythropoeitin, interferon g etc.
• Can be formulated into multiple dosage forms.
Disadvantages
UV – Unilamellar MVV/MV –
MLV – Multilamellar OLV – Oligolamellar
Vesicles (all size Multivesicular
Vesicles (>0.5µm) Vesicles (0.1-1µm)
ranges) vesicle(>1µm)
SUV – Small
Unilamellar vesicles
(20-100 nm)
MUV – Medium
Unilamellar vesicles
GUV – Giant
Unilamellar vesicles
LUV – Large
Unilamellar vesicles
(>100 nm)
Classification
• Based on Structural Parameters:
a. Multi-laminar vesicles (MLV): made up of series of
concentric bi-layer of lipid enclosing a small internal
volume with size range > 0.5um.
b. Oligolamelar vesicles (OLV): constitutes 2 to 10 bi layer
of lipids surrounding a large internal volume with size
range of 0.1 – 1um.
c. Unilamellar vesicle (ULV): single layer of lipids. Based
on the size of the single layer they are further divide
into the following types with in ULV as
• Small unilaminar vesicle: size of 20 to 40 nm
• Medium unilaminar vesicle: size of 40 to 80 nm
• Large unilaminar vesicle: size of 100 to 1000 nm
• Gaint unilaminar vesicle: size of more than 1000 nm
d. Multivesicular Vesicle(MV): constitutes for multiple
vesicles and size range >1um.
Types of Preparation
REV SUVs/OLV
made by
reverse-phase
evaporation MLV-REV
method MLVs made by
DRV Dehydrated reverse phase
– rehydration evaporation
method method
Based on
Method of
Preparation
SPLV
VET
Stable
Vesicles prepared
plurilamellar
by extrusion
vesicles
technique
FATMLV
Frozen and
Thawed MLVs
Composition - Applications
Neutral/negatively
CL (Convention
charged phospholipids
Liposomes
& cholesterol
RSVE – Reconstituted
Fusogenic Liposomes
Sendai Virus envelopes
Using phospholipids
pH sensitive liposomes such as PE or DOPE with
OA
Based on composition
and applications
Cationic lipids with
Cationic Liposomes
DOPE
With attached
Immuno-liposomes
monoclonal antibody
General Structure of various
types of liposomes
General Method of Liposome Preparation
Method of Preparation
1. Encapsulation
2. Partitioning
3. Reverse
loading
http://en.wikipedia.org/wiki/Liposome
1. Physical Characterization:
Characterization parameters Analytical method/Instrument
4. Electrical surface potential and surface pH Zetapotential measurements & pH sensitive probes
Phospholipid hydrolysis,
4. HPLC and TLC
Cholesterol auto-oxidation.
5. Osmolarity Osmometer
3. Biological Characterization
Characterization parameters Analytical method/Instrument
Avian retrovirus vaccine Killed avian retrovirus Chicken pox Vineland lab, USA
The flexibility in their behaviour can be exploited for the drug delivery through any
route of administration and for any drug or material irrespective of its
physicochemical properties.
The uses of liposomes in the delivery of drugs and genes to tumour sites are
promising and may serve as a handle for focus of future research.
References
Target and Controlled Drug delivery – Novel Carrier Systems by S.P.Vyas and R.K.Khar.
Controlled and Novel Drug Delivery Systems by Sanjay K. Jain and N.K.Jain. 2.
http://noopurmandrek.files.wordpress.com/2010/09/lipo1.jpg (accessed on 15-04-2011)
3. www.nanobiotec.iqm.unicamp.br/download/liposomas-3.ppt accessed on 15-04-2011)
4. http://www.uni-magdeburg.de/imos/mea_sen/img/pictures/Lipo.jpg (accessed on 15-04-2011)
5. http://www.nanolifenutra.com/images/image_liposome_01.jpg (accessed on 15-04-2011)
6. http://www.azonano.com/work/bFgW9FjRw248U2PRC2In_files/image002.gif (accessed on 15-
04-2011)
7. http://upload.wikimedia.org/wikipedia/en/2/28/Liposome.jpg (accessed on 15-04-2011)
Biopharmaceutics and pharmacokinetics a treatise by D.M.Bramhankar and sunil B. jaiswal (first
edition reprint 2005) pg.no- 360-361.
9. “Liposomes preparation methods” a review by Mohammad riaz in Pakistan journal of
pharmaceutical sciences vol.19(1), January 1996, pp.65-77.