it contains liposome, ethosome, pharmacosomes, herbosomes, niosomes, transferosomes, proniosomes, cubosomes, enzymosomes, virosomes etc.

1. A SEMINAR ON
“RECENT ADVANCES IN VESICULR
DRUG DELIVERY
SYSTEM”
Under the Guidance of,
Dr. N. H. ALOORKAR
M. PHARM. Ph. D
Presented by,
Mr. N. G. SHINDE
M. PHARM. (Sem. II)
SATARA COLLEGE OF PHARMACY, SATARA.

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INTRODUCTION
TO
Vesicular Drug Delivery
System

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Advantages-
Prolongation of existence of drug in systemic circulation.
Reduce toxicity.
Improved bioavailability.
Hydrophilic- Lipophilic drugs can be incorporated.
Sustained release system-
 Delay elimination of rapidly metabolizing drugs.
VESICULAR DRUG DELIVERY SYSTEM

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WHY VESICULAR DRUG DELIVERY SYSTEM ?
 Degradation of drug and/or drug loss.
 Harmful side effects.
 Bioavailability at site of disease.
 Intracellular infection-
Conventional therapy is ineffective due to limited
permeation into cell and the problem can be overcome
by VDDS.

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Microscopic spheres - cholesterol, non-toxic
surfactant, glycolipids etc.
Hollow spheres of lipids.
Size- 50 nm-150 nm in diameter.
LIPOSOMES

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• COMPONENTS-
• Phospholipids- Dipalmitoyl phosphatidilcholine
Dipalmitoyl phosphatidil glycerol(DPPG)
• Cholesterol- makes memb. less permeable by filling up holes and disruptions
Lipid conjugated diene
Methacrylate and thiol group
Charge induced lipids

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Cell Membrane

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 Suitable for delivery of
hydrophobic, hydrophilic drugs.
 Biocompatible.
 Suitable for controlled release.
 Localized action in particular
tissues.
 Suitable to administer via various
routes.
 High production cost.
 Leakage/ fusion of encapsulated
drug.
 Phospholipids undergo
hydrolysis/oxidation reaction.
(Ester bonds/Unsat. Acyl gr.)
 Short half-life & low solubility.
ADVANTAGES DISADVANTAGES

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 Immunoliposome
 Stealth liposome- PEG coating
 Improve stability & lengthen circulating half
life.
Inhibit recognition by RES system.
 Phospholipids
 Synthetic Phospholipids
 Glycerolipids
 Sphingolipids
 Glycosphingolipids
 Steroids
 Polymeric material
 Charge-inducing lipids
Advances in liposomesMaterials used in
liposomes preparation

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• The lipid bilayer of the liposome can fuse with other
bilayers (e.g. cell membrane) thus delivering the
liposome contents.
 Endocytosis
 Adsorption to cell surface
 Fusion with plasma cell
membrane
 Transfer of liposomal
content
Drug release from liposomes

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r

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Liposomes as Protein Carriers in Immunology.
Oral Drug Delivery.
Site Specific Delivery.
Sustained or Controlled Delivery.
Gene Therapeutics.
E.g. Liposomal amphotericin B (Enzon)- Fungal infection
Liposomal morphine (Endo, SkyePharma)- Postsurgical
analgesia
Applications

16. Niosomes are non-ionic surfactant vesicles obtained by hydration of
synthetic non-ionic surfactant with or without incarporation of
cholesterol or other lipids.
The vesicle is composed of a bilayer of non-ionic surface active
agents and hence the name niosomes.
Higher chemical stability than liposome.
NIOSOMES

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NIOSOMES

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Hydrophilic, lipophilic as well as amphiphilic moieties can be
incorporated.
Act as a depot to release the drug slowly and offer a controlled
release .
Handling and storage of surfactants do not require any special
conditions.
Enhance the skin penetration of drugs.
WHY NIOSOMES ?

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High patient compliance - oily dosage forms.
Accommodate drug molecules with a wide range of solubilities.
Stable, increase the stability of entrapped drug.
Biodegradable, biocompatible and nonimmunogenic.
Given by oral, parenteral and topical routes.
Improved oral bioavailability of poorly absorbed drugs.
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ADVANTAGES OF NIOSOMES

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Ester bonds of phospholipids are easily hydrolyzed, this can
lead to phosphoryl migration at low PH.
Peroxidation of unsaturated phospholipids.
As liposomes have purified phospholipids they are to be stored
and handled at inert(N2) atmospheres where as Niosomes are
made of non ionic surfactants and are easy to handle and
store.
Phospholipids are naturally occurring substances and as such
require extensive purification thus making them costly.
ADVANTAGES OF NIOSOME OVER LIPOSOME

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NIOSOMES
applications
Transdermal
delivery
Parenteral
delivery
Radio-
pharmaceuticals
Ophthalmic
Drug delivery

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 Transdermal Applications-
An increase in the penetration rate has been achieved by transdermal
delivery of drug incorporated in niosomes.
E.g. erythromycin
 Parenteral Applications-
 Niosomes -sub-micron size
 Vesicles up to 10 μm are administered via i.p. or i.m.
• Delivery of peptide drugs-
 Oral delivery of 9-desglycinamide, 8-arginine vasopressin entrapped in
niosomes increase stability of peptide significantly.
• Ophthalmic Drug Delivery-
Niosomes in less size are suitable for drug administration to eye.

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 PEG -glucose conjugates on the surface of niosomes
significantly improved tumor targeting of an encapsulated
paramagnetic agent.
 Phase I and phase II studies-
 Methotrexate gel- localized psoriasis.
 Niosomal methotrexate gel is more efficacious than
placebo and marketed methotrexate gel.
RECENT ADVANCES IN NIOSOMES

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A research article was published claiming that acyclovir
entrapped niosomes were prepared by Hand shaking and Ether
injection methods . The results indicated an increase in the oral
bioavailability of acyclovir.
Lancome has come out with a variety of anti-ageing products
which are based on niosome formulations
RECENT ADVANCES IN NIOSOMES

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Lipid based elastic vesicles-
Phospholipids, alcohol (In high concentration) and water.
Size : nanometer- microns
High conc. Ethanol- (20-50%)
Lipid memb. Packed less tightly than conventional vesicles hence
improved drug distribution through stratum corneum.
↑ Fluidity of cell membrane → ↑skin permeability
Ulter solubility properties of stratum corneum
↑Solubility of drug,
e.g. Levonorgesterol, hydrocortisone, 5-flurouracil (TDDS).
ETHOSOMES

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MECHANISM OF
ETHOSOMES

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Delivery of large molecules. e.g. peptides, proteins.
High patient compliance- (semisolid gel/ cream)
Passive, non-invasive and immediate commercialization.
Enhanced drug permeation through skin (TDDS).
Applied widely in Pharmaceutical, Veterinary, and
Cosmetic fields.
e.g. Antiviral drugs- Zidovudine (orally- side effects)
Ethosomal preperation- prolong release
TDD of harmones- 30 times more permeation of drug.
TESTOSOME Patch (Testosterone ethosome) (rabbit pinna skin)
Advantages of ethosomal drug delivery

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TRANSFEROSOMES
Transferosomes are specially optimized ultra-deformable lipid
supramolecular aggregates which are able to penetrate the skin.
 It consists of inner aqueous compartment surrounded by lipid
bilayer (semidilute suspension).
 Deformability property- Rapid shape transformation
Non-invasive delivery of small, medium and large sized
drugs.

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COMPONENTS
Phospholipids-
Soya phosphatidyl choline
Egg phosphatidyl choline
Surfactants- (flexibility)
Tween 80
Sodium cholate
Alcohol- (solvent)
Methanol
Ethanol
Buffering agent-
(hydrating agent)
Saline phosphate buffer pH
7.4

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High deformability gives better penetration of drug.
Acts as carrier for LMW & HMW drugs.
e.g. analgesics, sex hormones, anticancer etc.
Biocompatible and biodegradable.
High entrapment efficiency
Used for topical, systemic delivery.
Easy to scale up.
Advantages of Transferosomes

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VESICULAR
SYSTEM
PROBLEMS
Liposomes
&
Transferosomes
• Degradation by oxidation, sedimentation, leaching of
drug
• Lack of purity of the natural phospholipids
• Expensive to prepare
Niosomes
Aqueous suspension –
aggregation, fusion, leaching or hydrolysis of
entrapped drugs, thus limiting the shelf life
• Time consuming preparation
• Requires specialized equipment.

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(Pharmacon- drug, soma- carrier)
System formed by linking the drug to a carrier.
Colloidal dispersion of drugs covalently bound to lipids.
Self Assembled Nanoparticles (SAN).
Composed of amphiphilic prodrugs, so high drug loading
amount & very low drug leakage can be achieved easily.
↓interfacial tension-↑ contact area- ↑ bioavailability.
PHARMACOSOMES

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ADVANTAGES-
Drug targeting
Controlled release
High entrapment efficiency
No need of removal of unentrapped drug from
formulation as required in liposome.
Improves bioavailability of poorly soluble drugs.
Suitable for hydrophilic-lipophilic drugs.
Reduce cost of therapy.
PHARMACOSOMES

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“Hollow shell microcapsules consist of coagulated or fused
particles at interface of emulsion droplets”.
Control of size allows flexibility in application.
Colloidosome membrane offers great potential in controlling
the permeability of entrapped species.
Allows selective and timed release.
COLLOIDOSOMES

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Water soluble phytoconstituents-
e.g. flavonoids, tannins, glycosidic aglycons poorly absorbed
due to large mol. Size /poor lipid solubility- poor
bioavailability.
 Better pharmacokinetic and pharmacodynamic profile than
herbal extracts.
Advantages-
Enhance absorption of lipid insoluble phytoconstituents.
Phosphatidylcholine- Acts as carrier and hepatoprotective.
Better stability profile (PTC=PC).
HERBOSOME

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“Concentric bilayered vesicle in which aqueous volume is entirely
enclosed with phospholipid bilayer membrane”.
“Sphingolipids used in preparation of stable liposome”
ADVANTAGES-
 Provide selective passive targeting to
tumor tissue.
-Flexibility to couple with site specific
ligands.
 Increase stability via encapsulation.
SPHINGOSOMES
Hydrolysis-
√ Ester linkage- Phospholipids
Ether amide linkage- Sphingolipids

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“Layerosomes are conventional liposomes coated with one or more
multiple layers of biocompatible polyelectrolytes in order to
stabilize their structure”.
Layer by layer coating concept – stabilization of nanosystem.
LAYEROSOMES

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Unsaturated fatty acid liposomes are colloidal suspensions
composed of fatty acid and their ionizable species (soap).
Fatty acid vesicles are mixed “fatty acid/ soap vesicle”
More stable than liposomes.
UFOSOMES

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PROLIPOSOME-
Lipid and drug are coated
on a soluble carrier to form
free flowing granulating
material.
Controlled release
Better stability
Increased solubility
Ease of handling
PRONIOSOMES-
Water soluble carrier particles
that are coated with surfactant.
Dry & free flowing product.
More stable during sterilization
and storage.
Minimizes problems of niosomes
such as fusion, aggregation,
sedimentation, leakage on storage.
STRATEGIES TO IMPROVE INTRAVESICLE DRUG DELIVERY
PROVESICULAR DRUG DELIVERY

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Physical means-
IONTOPHORESIS-
effective method of drug transport in deeper layer of bladder.
e.g. Mitomycin C , Bethanechol
Electroporation (high voltage than Iontophoresis)
↑ Permeability of tissue due to electric field.
Helpful for delivery of drug in bladder carcinoma treatment.
Electroporation- Sonophoresis (low intensity ultrasound waves)-
↓ tissue damage.
STRATEGIES TO IMPROVE INTRAVESICLE DRUG DELIVERY
IMPROVING PERMEABILITY

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Chemical means-
Prior instillation of DMSO enhance absorption of
chemotherapeutic drugs.
e.g. Paclitaxel, Pirarubicin
Intravesicle instillation of saponin before administration of
anticancer drug.
e.g. 4-0-tetrahydropyranyldoxorubicin (THP)
↑ Conc. of THP in bladder tissue.
Topical application of Chitosan and Cyclodextrins- disrupts
intercellular tight junction- ↑paracellular transport.
STRATEGIES TO IMPROVE INTRAVESICLE DRUG DELIVERY

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AQUASOME
CRYPTOSOMES
EMULSOMES
DISCOMES
GENOSOMES
VESOSOMES
PROTEOSOMES
ARCHAEOSOMES
HEMOSOMES
ERYTHROSOMES
ENZYMOSOMES
PHOTOSOMES
VIROSOMES
FUTURE PERSPECTIVES

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AQUASOMES
“Three layered self assembly - ceramics carbon nanocrystalline
particulate core coated with glassy cellobiose -specific targeting &
molecular shielding”.
CRYPTOSOMES
“Lipid vesicles with surface coat composed of pc and of suitable
polyoxyethylene derivative of phosphatidyl ethanolamine”.
Capable of ligand mediated drug targeting.
DISCOMES
“Niosome solubilized with non-ionic surfactant solution”.
(polyoxyethylene cetyl ether class)

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EMULSOMES
“Nanosize lipid particles (bioadhesive nanoemulsion) consist of
microscopic lipid assembly with polar core used for parenteral
delivery of poorly water soluble drugs”.
GENOSOMES
“Artificial macromolecular complexes for functional gene
transfer.”
Cationic lipids-↑biodegradability & stability in blood stream.
PHOTOSOMES
“Photolyses encapsulated in liposome, which release the content
photo-triggered charges in membrane permeability
characteristics”

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VIROSOME
“Liposome spiked with virus glycoprotein, incorporated into
the liposomal bilayers based on retro virus derived lipids”.
VESOSOMES
“Nested bilayer compartment of saturated phospholipids”.
Multiple compartments- better protection to the interior
contents .
PROTEOSOMES
“High molecular weight multi-submit enzyme complexes with
catalytic activity, specifically due to the assembly pattern of
enzymes”.

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HEMOSOMES
“Hb containing liposome engineered by immobilizing Hb with
polymerizable phospholipids”.
ERYTHROSOMES
“Liposomal system in which chemically cross linked human
erythrocytes cytoskeletons are used as support to which lipid
bilayer is coated”.
ENZYMOSOMES
“Enzymes are covalently immobilized or coupled to the
surface of liposomes”.

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Saurabh Bansal, A comparative review on vesicular drug delivery system and
stability issues, IJRPC, 2012, 704-715.
Patel j. k, Aquasomes: a self-assembling nanobiopharmaceutical carrier system for
bioactive molecules: a review, IJPRS(2), 2012, 11-21.
Mayank Gangwar, Recent advances in various emerging vesicular systems: an
overview, APJTB, 2012, S1177-S1188.
Seema M. Jadhav, Novel vesicular system: an overview, JAPS (01); 2012,193-202.
Nishith Patel, Liposome Drug delivery system: a Critic Review, JPSBR(2), 2012,
169-175.
REFERENCES

50. 50
Sreedevi A, A Pharmacosomes – a review, IJPR (12), 2012; 114-117.
N. Bharti, Proniosomes: a recent advancement in nanotechnology as a drug
carrier, IJPRD, 2012(12), 67-75.
Deepthi Annakula, „Provesicular drug delivery systems: An overview and
appraisal, AASR(4), 2010, 135-146.
Kombath Ravindran Vinod, Critical issues related to Transferosomes – Novel
Vesicular System, ASPTA (1) 2012, 67-82.
REFERENCES

51. THANK
YOU