Liposomes is Greek words means ‘Lipo’ mean ‘Fat’ and ‘Somes’ mean ‘Body’.
Liposomes are concentric bilayered vesicles in which an aqueous core is entirely enclosed by a membranous lipid bilayer mainly composed of natural or synthetic phospholipids.
Liposomes are extensively used as carriers for numerous molecules in cosmetic and pharmaceutical industries.
TỔNG ÔN TẬP THI VÀO LỚP 10 MÔN TIẾNG ANH NĂM HỌC 2023 - 2024 CÓ ĐÁP ÁN (NGỮ Â...
LIPOSOMES INTRODUCTION AND TYPES.pptx
1. SEMINAR
MOLECULAR PHARMACEUTICS
LIPOSOMES- INTRODUCTION AND
TYPES
SUBMITTED BY,
ARDRA KRISHNA P V
MPHARM 2ND SEMESTER
DEPARTMENT OF PHARMACEUTICS
KMCH COLLEGE OF PHARMACY
12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 1
2. CONTENT
12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 2
INTRODUCTION
ADVANTAGES
DISADVANTAGES
TYPES
LIPOSOMES AND CANCER
MARKETED FORMULATIONS
3. TARGETING METHODS
• Rational Research in drug delivery
began in 1950s.
• Need for Targeted/controlled Drug
Delivery:
Delivery of the drug at a rate
and/or a location dictated by the
needs of the body or disease state
over a specified period of time.
12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 3
4. LIPOSOMES
• Liposomes is Greek words means ‘Lipo’
mean ‘Fat’ and ‘Somes’ mean ‘Body’.
• Liposomes are concentric bilayered
vesicles in which an aqueous core is
entirely enclosed by a membranous lipid
bilayer mainly composed of natural or
synthetic phospholipids.
• Liposomes are extensively used as carriers
for numerous molecules in cosmetic and
pharmaceutical industries.
12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 4
5. • Discovered in 1960‟s by Bangham and coworkers.
• The size range of liposome: 20 nm up to several micrometers.
• Due to their size and hydrophobic and hydrophilic character(besides
biocompatibility), liposomes are promising systems for drug delivery.
• The choice of bilayer components determines the ‘rigidity’ or ‘fluidity’
and the charge of the bilayer.
12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 5
8. COMPOSITION OF LIPOSOMES
There are number of components of liposomes however Lecithin
(mixture of phospholipids) and cholesterol being main components.
12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 8
9. PHOSPHOLIPIDS
Phospholipids are fatty substances the major structural components
of cell wall & biological membranes.
Phospholipids are amphipathic moieties with a hydrophilic head
group and two hydrophobic tails.
Two types of phospholipids exist – PHOSPHODIGLYCERIDES
AND SPHINGOLIPIDS, together with their corresponding
hydrolysis products.
• Phospholipids have phosphatidyl moiety (tail) with different head
groups (choline, Ethanolamine, Serine)
• The most common phospholipid is Phosphatidylcholine (PC)
molecule.
12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 9
10. 12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 10
Phosphatidylcholine has
glycerol bridge links a
pair of hydrophobic acyl
hydrocarbon chains
having 10-24 carbon
atoms with a hydrophilic
polar head group.
11. ADVANTAGES
• Provides selective passive targeting to tumor tissues (liposomal
doxorubicin).
• Increased efficacy and therapeutic index.
• Increased stability via encapsulation.
• Reduction in toxicity of the encapsulated agent.
• Improved pharmacokinetic effects (reduced elimination, increased
circulation life times).
• Flexibility to couple with site-specific ligand to achieve active
targeting.
• Site avoidance effect (avoids non-target tissues).
12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 11
12. DISADVANTAGES
• Very high production cost.
• Drug leakage/ entrapment/ drug fusion.
• Sterilization.
• Short biological activity / t ½.
• Oxidation of bilayer phospholipids.
• Repeated iv administration problems.
12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 12
13. STERILIZATION OF LIPOSOMES
• Due to the particular sensitivity of liposomes and their tendency to
physicochemical alterations, their sterilization remains a real challenge.
Conventional sterilization methods such as heat, ethylene oxide, ultraviolet
and gamma irradiations are considered as unsuitable for liposome
sterilization.
• The search for an alternative method being therefore necessary, the
applicability of SUPERCRITICAL CARBON DIOXIDE (ScCO2)
TECHNOLOGY, which is nowadays a promising strategy for the
sterilization of sensitive products such as liposomes. ScCO2 could
effectively be an interesting alternative to achieve sterility of liposomes.
12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 13
14. TYPES
12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 14
BASED ON
METHOD OF
PREPARATION
BASED ON
STRUCTURAL
PARAMETERS
BASED ON
COMPOSITION
AND
APPLICATION
CLASSIFICATION
LIPOSOMES CAN BE CLASSIFIED BASED ON THREE DIFFERENT CRITERIA:
15. CLASSIFICATION OF LIPOSOMES
12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 15
BASED ON
STRUCTURAL
PARAMETERS
MLV
Multilamellar
Vesicles (>0.5
μm)
OLV
Oligolamellar
Vesicles (0.1 – 1
μm)
UV Unilamellar
Vesicles (Full
size range)
SUV Small
Unilamellar
Vesicles (20 –
100 nm)
GUV Giant
Unilamellar
Vesicles ( >1
μm)
MUV Medium
Unilamellar
Vesicles
LUV Large
Unilamellar
Vesicles (>100
nm)
MVV / MV
Multivesicular
Vesicles (>1
μm)
17. BASED ON
COMPOSITION AND
APPLICATION
CL (
Conventional
liposomes)
Neutral/ Negatively charged
phospholipids and cholesterol
Fusogenic
Liposomes
RSVE – Reconstituted Sendai
Virus Envelop
pH sensitive
Liposomes
Using phospholipids such as PE or
DOPE with OA
Cationic
Liposomes
Cationic Lipids with DOPE
Long Circulatory (
stealth) Liposomes
( LCL)
High Tc made using cholesterol
and 5 – 10% PEG – DSPE or GM1
Immuno –
liposomes
With attached monoclonal
antibody
12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 17
18. BASED ON
METHOD OF
PREPARATION
DRV
dehydrated
–
Rehydration
method
VET Vesicle
prepared by
extrusion
technology
REV SUVs/
OLVs made
by reverse –
phase
evaporation
method
FAT MLV
Frozen
and
Thawed
MLVs
MLV- REV
MLVs made
by reverse
phase
evaporation
method
SPLV
stable
plurilamell
ar Vesicles
12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 18
20. 12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 20
TRANSFEROSOMES ARCHEOSOMES
VIROSOMES ETHOSOMES
21. MARKETED FORMULATIONS
CARRIER
SYSTEM
TARGETED SITE CARRIER FORMULATION MARKETED
EXAMPLES
IV TUMOR CELL LIPOSOMES POWDER , DISPERSION AND
SOLVENT FOR CONCENTRATE
FOR DISPERSION FOR INFUSION
myocet
IV FUNGAL CELL WALL LIPOSOMES POWDER FOR DISPERSION FOR
INFUSION AmBisome®
12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 21
22. LIPOSOMES AND CANCER
• Liposomes have revolutionized
cancer therapy by their broad
clinical applications.
• Liposomes overcome the
limitations of conventional
chemotherapy by improving the
bioavailability and stability of the
drug molecules and minimizing
side effects by site-specific
targeted delivery of the drugs.
12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 22
23. Biological Challenges Facing Liposomal
Drug Delivery Systems
As with any foreign particle that enters the body, liposomes
encounter multiple defense systems aimed at recognition, neutralization,
and elimination of invading substances. These defenses include the RES
(Reticuloendothelial system), opsonization, and immunogenicity. While
these obstacles must be circumvented for optimal liposome function,
other factors such as the enhanced permeability and retention (EPR)
effect can be exploited to enhance drug delivery.
12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 23
24. REFERENCES
• Akbarzadeh, A., Rezaei-Sadabady, R., Davaran, S. et al. Liposome: classification,
preparation, and applications. Nanoscale Res Lett 8, 102 (2013).
https://doi.org/10.1186/1556-276X-8-102
• Sriram Vemuri, C.T Rhodes, Preparation and characterization of liposomes as
therapeutic delivery systems: a review, Pharmaceutica Acta Helvetiae, Volume 70,
Issue 2, 1995, https://doi.org/10.1016/0031-6865(95)00010-7
• Nina Filipczak, Jiayi Pan, Satya Siva Kishan Yalamarty, Vladimir P. Torchilin,
Recent advancements in liposome technology, Advanced Drug Delivery Reviews,
Volume 156, 2020, 4-22, https://doi.org/10.1016/j.addr.2020.06.022
12-07-2022 Department of Pharmaceutics, KMCH College OF Pharmacy 24