Review Article

Liposomal Drug Delivery System-A Review

Deepthi V and Kavitha AN*
Krupanidhi College of Pharmacy, #12/1, Chikkabellandur Village, Carmelaram Post
Varthur Hobli, Bangalore 560035

ABSTRACT
Purpose of this paper: Liposomes have received a lot of attention during the past 30 years as pharmaceutical carriers
of great potential. More recently, many developments have been seen in the area of liposomal drugs-from clinically
approved products to new experimental applications. For further successful development of this field, promising trends
must be identified and exploited, with a clear understanding of the limitations of these approaches.
Design/methodology/approach: This review presents a panoramic view of current status of research in this field to
serve as a ready reference for future researchers.
Practical implications: The treasure of information provided in this review find wide utility by future researchers and
will serve as basis for further improvement in methodology and design of better formulations as well as evaluation
methods.
What is original/value of paper: In this article, basic characteristics, method of preparation and marketed formulations
of liposomes are discussed. The success of liposomes as drug carriers has been reflected in a number of liposome
based formulations, which are commercially available, or are currently undergoing clinical trials.
Keywords: Lipoidal vesicles, Hydrophillic and Hydrophobic drugs, Drug carriers.

INTRODUCTION with their hydrolysis products. Classifica-

The name liposome is derived from two
Greek words: Lipos meaning fat and
Soma meaning body. A liposome can be
formed in variety of sizes as uni-lamellar
or multi-lamellar construction, and its
name relates to its structural building
tion of liposomes is based on number of
lamellae, composition, method of prepa-
ration and its size (Table 1 and 2). Lipo-
somes can exhibit a range of sizes and
morphologies upon the assembly of pure Received Date : 05-05-2014
Revised Date : 17-06-2014
lipids or lipoidal mixtures suspended in an Accepted Date : 20-06-2014

blocks, phospholipids, and not to its size. aqueous medium. A common morphology DOI: 10.5530/rjps.2014.2.3
Liposomes were first described by British which is analogous to the eukaryotic cel-
Address for
hematologist Dr. Alec D Bangham in lular membrane is the unilamellar vesicles. correspondence
1961 (Published 1964), at the Babraham This is characterized by a single bilayer Mrs Kavitha AN
Asst. Professor
Institute, when he and R.W. Horne membrane which encapsulates an internal Krupanidhi College
were testing the institutes new electron aqueous solution, thus separating it from of Pharmacy, #12/1,
ChikkabellandurVillage,
microscope by adding negative stain to dry the external solution. Both cationic amine Carmelaram Post, Varthur
phospholipids.1,2 head groups and anionic phospholipid Hobli, Bangalore-560035
Mobile: 9886887421
Liposomes are simple microscopic vesicles head groups can form this single walled E-mail: kavithareddykcp@
in which lipid bilayer structure is present vesicle.3 Vesicle size falls into nanometer gmail.com

with an aqueous volume entirely enclosed to micrometer range: small unilamellar

by a membrane, composed of lipid mol-
ecules. There are number of components
present in liposomes, with phospholipid
and cholesterol being the main ingredients.
The type of phospholipids includes phos-
phoglycerides and sphingolipids, together
vesicles are 20200 nm, unilamellar vesi-
cles are 200 nm-1 m, and giant unilamel-
lar vesicles are larger than 1 m. In this
article, basic characteristics, method of
preparation and marketed formulations of
liposomes are discussed. www.rjps.in

RGUHS J Pharm Sci | Vol 4 | Issue 2 | AprJune, 2014 47

 Liposomal Drug Delivery System-A Review

Table 1: Classification of liposomes based on size and lamellarity4

SL. NO TYPES SIZE

1. Multilamellar large vesicles(MLV) (>0.5m)

2. Oligolamellar vesicles(OLV) 0.1-1 m

3. Unilamellar vesicles(UV) All sizes

4. Small unilamellar vesicles(SUV) 20-100 nm

5. Medium sized unilamellar vesicles(MUV) _

6. Large unilamellar vesicles(LUV) >100 nm

7. Giant unilamellar vesicles(GU) >1 m

8. Multivesicular vesicles(MVV) usually >1 m

Table 2: Classification of liposomes based on the method of preparation4

SL. NO. TYPES OF LIPOSOMES METHOD OF PREPARATION

REV(Reverse Evaporation
1. Single or Oligolemellar vesicles made by reverse osmosis
vesicles)

2. MLV-REV Multilamellar vesicles made by Reverse Phase Evaporation method

3. SPLV Stable Plurilamellar vesicles

4. FATMLV Frozen and Thawed MLV

5. VET Vesicles prepared by Extrusion method

6. DRV Vesicles prepared by Dehydration-Rehydration method

CLASSIFICATION OF LIPOSOMES 2. Leakage and fusion of encapsulated drug/mol-

ecules can occur.
ADVANTAGES5 3. It has short half life-In reticuloendothelial sys-
tem, particularly the Kupffer cells in the liver
1. Liposomes are biocompatible, completely biode- remove liposomes from the circulation.6
gradable, non-toxic in nature.
2. They are suitable for delivery of hydrophobic,
METHODS OF LIPOSOME PREPARATION
amphipathic and hydrophilic drugs.
3. They protect the encapsulated drug from exter- Passive Loading Techniques
nal environment. a. Mechanical dispersion methods:
4. They reduce toxicity and increase stability-Since Lipid film hydration by hand shaking, non hand
therapeutic activity of chemotherapeutic agent shaking or freeze drying
can be improved through liposome encapsula-
Micro emulsification
tion. This reduces deleterious effects that are
observed at concentration similar to or lower Sonication
than those required for maximum therapeutic French pressure cell
activity. Membrane extrusion
5. It reduces exposure of sensitive tissue to toxic Dried reconstituted vesicles
drugs.
Freeze thawed liposomes
b. Solvent dispersion methods:
DISADVANTAGES
Ethanol injection
1. The production cost is high. Ether injection

48 RGUHS J Pharm Sci | Vol 4 | Issue 2 | AprJune, 2014

 Liposomal Drug Delivery System-A Review
Double emulsion
Reverse phase evaporation vesicles
Stable pluri lamellar vesicles
c. Detergent removal methods:
Dialysis
Column chromatography
Dilution
Reconstituted Sendai virus enveloped
Active loading technique
GENERAL METHOD OF PREPARATION5,7,8
Liposomes are mainly manufactured using various pro-
cedures in which the water soluble (hydrophilic) materi-
als are entrapped by using aqueous solution of these
materials as hydrating fluid or by the addition of drug/
drug solution at some stage during manufacture of
liposomes. The lipid soluble (lipophilic) materials are
solubilized in the organic solution of the constitutive
lipid and then evaporated to a dry drug containing lipid
film followed by its hydration. These methods involve
loading of the entrapped agents before or during the
manufacturing procedure (Passive loading). However,
certain type of compounds with ionizable groups, and
those which display both lipid and water solubility, can
be introduced into the liposomes after the formation of
intact vesicles (remote loading).
MECHANICAL DISPERSION METHODS
Preparation of liposomes by lipid film hydration
When preparing liposomes with mixed lipid composi-
tion, the lipids must be dissolved and mixed in organic
solvent to assure a homogeneous mixture of lipids.
Usually this process is carried out using chloroform or
chloroform: methanol mixture. The purpose is to obtain
a clear lipid solution for complete mixing of lipids. Typi-
cally lipid solutions are prepared at 1020 mg lipid/ml
of organic solvent, although higher concentrations may
be used if the lipid solubility and mixing are acceptable.
Once the lipids are thoroughly mixed in the organic sol-
vent, the solvent is removed to yield a lipid film. For
small volumes of organic solvent (<1ml), the solvent
is evaporated by using dry nitrogen or argon stream in
a fume hood. For larger volumes, the organic solvent
should be removed by rotary evaporation yielding a
thin lipid film on the sides of round bottom flask. The
lipid film is thoroughly dried to remove residual organic
solvent by placing the vial or flask on a vacuum pump
overnight. If the use of chloroform is objectionable, an
alternative is to dissolve the lipids in tertiary butanol or
RGUHS J Pharm Sci | Vol 4 | Issue 2 | AprJune, 2014
cyclohexane. The lipid solution is transferred to con-
tainers and frozen by placing the containers on a block
of dry ice or swirling the container in a dry ice-acetone
or alcohol (ethanol or methanol) bath. Care should be
taken when using the bath procedure that, the container
can withstand sudden temperature changes without
cracking. After complete freezing, the frozen lipid cake
is placed on a vacuum pump and lyophilized until dry
(13 days depending on volume). The thickness of the
lipid cake should not be more than the diameter of the
container being used for lyophilization. Dry lipid films
or cake can be removed from the vacuum pump; the
container should be closed tightly, tapped and stored
frozen until ready to hydrate.
Hydration of Lipid Film/Cake
Hydration of the dry lipid film/cake is accomplished by
adding an aqueous medium to the container of dry lipid
and agitating. The temperature of the hydrating medium
should be above the gel liquid crystal transition tempera-
ture (Tc or Tm) of the lipid. After addition of the hydrat-
ing medium, the lipid suspension should be maintained
above the Tc during the hydration period. For high tran-
sition lipids, this is easily accomplished by transferring
the lipid suspension to a round bottom flask and plac-
ing the flask on a rotary evaporation system without a
vacuum. Spinning of round bottom flask in warm water
bath maintained at a temperature above the Tc of the
lipid suspension allows the lipid to hydrate in its fluid
phase with adequate agitation. Hydration time may dif-
fer slightly among lipid species and structure, however,
a hydration time of 1hr with vigorous shaking, mixing,
or stirring is highly recommended. It is also believed
that allowing the vesicle suspension to stand overnight
prior to downsizing makes the sizing process easier
and improves the homogeneity of the size distribution.
Aging is not recommended for high transition lipids as
lipid hydrolysis increases with elevated temperatures.
The hydration medium is generally determined by the
application of the lipid vesicles. Suitable hydration media
include distilled water, buffer solutions, saline, and non-
electrolytes such as sugar solutions. Generally accepted
solutions which meet these conditions are 0.9% saline,
5% dextrose and 10% sucrose. During hydration some
lipids form complexes unique to their structure. Highly
charged lipids have been observed to form a viscous
gel when hydrated with low ionic strength solutions.
The problem can be alleviated by addition of salt or by
downsizing the lipid suspension. Poorly hydrating lipids
such as phosphatidylethanolamine have a tendency to
self aggregate upon hydration. Lipid vesicles contain-
ing more than 60% phosphatidylethanolamine form
particles having a small hydration layer surrounding the
vesicle. As particles approach one another there is no
49
 Liposomal Drug Delivery System-A Review
hydration repulsion to repel the approaching particle
and the two membranes fall into an energy well where
they adhere and form aggregates. The aggregates settle
out of solution as large flocculates which will disperse
on agitation but reform upon settling. The product of
hydration is a large multilamellar vesicle (LMV) analo-
gous in structure, with each lipid bilayer separated by
a water layer. The spacing between lipid layers is dic-
tated by composition with poly-hydrating layers being
closer together than highly charged layers which sepa-
rate on electrostatic repulsion. Once a stable, hydrated
LMV suspension has been produced, the particles can
be downsized by a variety of techniques, including soni-
cation or extrusion.
Sizing of Lipid Suspension
Sonication
Disruption of LMV suspensions using sonic energy
(sonication) typically produces small, unilamellar ves-
icles (SUV) with diameters in the range of 15-50nm.
The most common instrumentation for preparation of
sonicated particle is bath and probe tip sonicators. Cup-
horn sonicators, although less widely used, but they have
successfully produced SUV. Probe tip sonicators deliver
Figure 1: Liposomes prepared by lipid film hydration and sizing9
French Pressure Cell Method
The method involves the extrusion of MLV at 20,000
psi at 4C through a small orifice. The method has
several advantages over sonication method. The method
is simple, rapid, and reproducible and involves gentle
50
high energy input to the lipid suspension but suffer from
overheating of the lipid suspension causing degradation.
Sonication tips also tend to release titanium particles into
the lipid suspension which must be removed by centrif-
ugation prior to use. For these reasons, bath sonicators
are the most widely used instrument for preparation of
SUV. Sonication of an LMV dispersion is accomplished
by placing a test tube containing the suspension in a bath
sonicator (or placing the tip of the sonicator in the test
tube) and sonicating for 510 minutes above the Tc of the
lipid. The lipid suspension should begin to clarify to yield
a slightly hazy transparent solution. The haziness is due to
light scattering induced by residual large particles remain-
ing in the suspension. These particles can be removed by
centrifugation to yield a clear suspension of SUV. Mean
size and distribution is influenced by composition and
concentration, temperature, sonication time and power,
volume, and sonicator tuning. Since it is nearly impossi-
ble to reproduce the conditions of sonication, Size varia-
tion between batches produced at different times is not
uncommon. Also, due to the high degree of curvature of
these membranes, SUV are inherently unstable and will
spontaneously fuse to form larger vesicles when stored
below their phase transition temperature (Figure 1).
handling of unstable materials (Figure 2). The resulting
liposomes are somewhat larger than sonicated SUVs.
The drawbacks of the method are that the required
temperature is difficult to achieve and the working
volumes are relatively small.
RGUHS J Pharm Sci | Vol 4 | Issue 2 | AprJune, 2014
 Liposomal Drug Delivery System-A Review
Figure 2: Liposomes prepared by French Pressure
Cell method9
Dried Reconstituted Vesicles (DRVs)
In dried reconstituted vesicles method preformed lipo-
somes are added to an aqueous solution containing an
active agent or are mixed with a lyophilized protein, fol-
lowed by rehydration of mixture. This leads to a disper-
sion of solid lipids in finely subdivided form (Figure 3).
However; this method is suitable only for unilamellar
vesicles, as the incorporation rates with multi lamellar
vesicles are quite low.
Figure 3: Liposomes Prepared By Dried Reconstituted Vesicles (DRVs) and Freeze
Thaw Sonication (FTS) Method9
RGUHS J Pharm Sci | Vol 4 | Issue 2 | AprJune, 2014
Freeze thaw method
In this method, SUVs are rapidly frozen and followed
by slow thawing. The brief sonication disperses aggre-
gated materials to LUV. The formation of unilamellar
vesicles is due to the fusion of SUV during the process
of freezing or thawing. This type of fusion is strongly
inhibited by increasing the ionic strength of the medium
and by increasing the phospholipids concentration
(Figure 3).The encapsulation efficiencies from 2030%
were obtained. The disadvantages with the method are
divalent metal ions; sucrose and high ionic strength salt
solutions cannot be entrapped efficiently.
Solvent Dispersion Methods
Ether Injection Method
A solution of lipids dissolved in diethyl ether or ether/
methanol mixture is slowly injected to an aqueous solu-
tion of the material to be encapsulated at 5565. The
subsequent removal of ether under vacuum leads to the
formation of liposomes. The main disadvantage with
the method is liposomes produced are heterogeneous in
nature (70190 nm) and the material to be encapsulated
will be exposed to higher temperature (Figure 4).
Ethanol Injection Method
A lipid solution of ethanol is rapidly injected to a vast
excess of buffer. The MLVs are immediately formed.
The drawbacks of the method are that the population
is heterogeneous (30110 nm), liposomes are very
dilute, it is difficult to remove residual ethanol because
51
 Liposomal Drug Delivery System-A Review
Figure 4: Liposomes prepared by (a) Ethanol injection method; and (b) Ether injection method
it forms azeotrope with water and the possibility of
various biologically active macromolecules to inactiva-
tion in the presence of even low amounts of ethanol
(Figure 4).
Reverse Phase Evaporation Method
Water in oil emulsion is formed by brief sonication of
two phase system containing phospholipids in organic
solvent (diethyl ether or isopropyl ether or mixture of
isopropyl ether and chloroform) and aqueous buffer.
The organic solvents are removed under reduced pres-
sure, resulting in the formation of a viscous gel. The
liposomes are formed when residual solvent is removed
by continued rotary evaporation under reduced pres-
sure. With this method high encapsulation efficiency
up to 65% can be obtained in a medium of low ionic
strength (0.01M NaCl). The method has been used to
encapsulate small and large macromolecules. The main
disadvantage of the method is the exposure of materi-
als to be encapsulated to organic solvents and to brief
periods of sonication.
Detergent Removal Method
The detergents at their critical micelle concentrations
have been used to solubilize lipids. As detergent is
removed the micelles become progressively rich in
phospholipid and finally combine to form LUVs.
The detergents can be removed by dialysis. The
advantages of detergent dialysis method are excellent
52
reproducibility and production of liposomes which
are homogenous in size. The main drawback of the
method is the retention of traces of detergent within
the liposomes. A commercial device called LIPOPREP
which is a version of dialysis system available for the
removal of detergents. Other techniques have been
used for the removal of detergents: (a) by using Gel
Chromatography involving a column of Sephadex
G-259 (b) by adsorption or binding of Triton X-100
(detergent) to Bio-Beads SM-210 (c) by binding of
octylglucoside (detergent) to Amberlite XAD-2beads.
MARKETED PRODUCTS
In clinical applications, liposomal drugs have been
proven to be most useful for their ability to passively
accumulate at site of increased vasculature perme-
ability, when their average diameter is in the ultra
filterable range, and for their ability to reduce the
side effects of the encapsulated drugs relative to free
drugs. This has resulted in an overall increase in ther-
apeutic index, which measures efficacy over toxicity.
However, the gains in the rapeutic index have been
more on the side of reduced toxicity than on the side
of increased efficacy. Liposomes have diverse appli-
cations in the treatment of infections, vaccine and
gene delivery, cancer treatment, lung diseases and
skin conditions (Table 3).
RGUHS J Pharm Sci | Vol 4 | Issue 2 | AprJune, 2014
 Liposomal Drug Delivery System-A Review

Table 3: Marketed Products

NAME TRADE NAME COMPANY INDICATION

Liposomal Amphoterecin B10 Abelcet Enzon Fungal infection

Liposomal Amphoterecin B11 Ambisome Gilead Sciences Fungal and Protozoal infection

Liposomal cytarabine12 Depocyt Pacira(Skye Pharma) Malignant lymphomatous meningitis

Liposomal Daunorubicin13 Daunoxome Gilead Sciences HIV-related Kaposis Sarcoma

Liposomal doxorubicin14 Myocet Zeneus Combination therapy with cyclophosphamide in

metastatic breast cancer

Liposomal IRIV15 Epaxal Crucell Hepatitis A

Liposomal IRIV Vaccine16 Inflexal V Berna Biotech Influenza

Liposomal morphine 17
DepoDur Skye Pharma, Endo Post-surgical analgesia

Liposomal verteporfin18 Visudyne QLT, Novartis Age-related macular degeneration, pathologic

myopia, ocular histoplasmosis

Liposome- Proteins SP-B and Curosurf Chiesi Farmaceutici, Pulmonary Surfactant for Respiratory Distress
SP-C19,20 S.p.A Syndrome (RDS)

Liposome- PEG doxorubicin21 Doxil/ Caelyx Ortho Biotech, HIV-related Kaposis sarcoma, metastatic breast
Schering-plough cancer, metastatic ovarian cancer

Micellular estradiol22 Estrasorb Novavax Menopausal therapy

Liposomal vincristine23 Marqibo Spectrum Acute Lymphoblastic Leukemia (ALL) and Melanoma
pharmaceuticals

CHARACTERIZATION OF LIPOSOMES Encapsulation efficiency25: It describes the

Vesicle shape and lamellarity: The shape and
lamellarity of liposome is measured by electron
microscopy or by spectroscopic techniques. Most
frequently the nuclear magnetic resonance spec-
trum of liposome is recorded with and without
the addition of a paramagnetic agent that shifts
or bleaches the signal of the observed nuclei on
the outer surface of liposomes.
Vesicle size and size distribution: The size dis-
tribution is normally measured by dynamic light
scattering. This method is reliable for liposomes
with relatively homogenous size distribution.
A simple but powerful method is gel exclusion
chromatography, in which a truly hydrodynamic
radius can be detected. Sephacryl-S100 can sepa-
rate liposome in size range of 30-300nm.Sep-
harose -4B and-2B columns can separate SUV
from micelles.
Surface charge determination24: Liposomes
are usually prepared using charge imparting con-
stituting lipids and hence it is imperative to study
the charge on the vesicle surface. The free flow
electrophoresis and zeta potential measurement
will be done to determine the charge on the sur-
face of vesicles.
RGUHS J Pharm Sci | Vol 4 | Issue 2 | AprJune, 2014
percent of drug in aqueous phase and hence per-
cent of water soluble drug ultimately entrapped
during preparation of liposomes and is usually
expressed as % entrapment/mg lipid. Encapsu-
lation efficiency is assessed using two techniques
including mini column centrifugation method
and protamine aggregation method. In mini
column centrifugation method, the hydrated
gel is filled in a barrel of 1 ml syringe without
plunger which is plugged with Whatman GF/B
filter pad. This barrel is rested in a centrifuge
tube. This tube is spun at 2000 rpm for 3 min
to remove excess saline solution from gel. After
centrifugation the gel column should be dried
and the eluted saline is removed from collection
tube. Liposome suspension of 0.2 ml is applied
drop wise to top gel bed, and the column is spun
at 2000 rpm for 3min to expel the void volume
containing the liposomes into centrifugation
tube. The elution is then removed and set aside
for assay.
Entrapped volume: The entrapped volume of
a population of liposomes (in l/mg phospho-
53
 Liposomal Drug Delivery System-A Review
lipids) can often be deduced from measurements
of total quantity of solute entrapped inside lipo-
some assuring that the concentration of solute in
the aqueous medium inside liposome is the same
after separation from entrapped material.
Phase Response and transitional behavior:
Liposome and lipid bilayer exhibit various phase
transition that are studied for their role in trig-
gered drug release or stimulus mediated fusion
of liposomal constituent with target cell. An
understanding of phase transition and fluidity
of phospholipids membrane is important both
in manufacture and exploitation of liposomes
since phase behavior of liposomal membrane
determine such properties such as permeability,
fusion, aggregation and protein binding. The
phase transition has been evaluated using freeze
fracture electron microscopy. They are more
comprehensive verified by differential scanning
calorimeter analysis.
Stability of liposomes: Liposomal stability
includes physical, chemical and biological sta-
bility. The physical stability indicates mostly
the constancy of the size and the ratio of lipid
to active agent. The cationic liposomes can be
stable at 4o for long period of time, if properly
sterilized. The chemical instability mainly con-
cerns two degradation pathways, oxidative and
hydrolytic. Oxidation of phospholipids in lipo-
somes mainly takes place in unsaturated fatty
acyl chaincarrying phospholipids. These chains
are oxidized via a free radical chain mechanism
in the absence of particular oxidants. Storage
at low temperatures and protection from light
and oxygen will reduce the chance of oxidation.
Further protection could be enhanced with the
addition of antioxidants such as -tocopherol
and butyl hydroxyl toluene. Working under
nitrogen or argon also minimizes the oxidation
of lipids during preparation. The hydrolysis of
ester bonds can also be reduced by optimizing
pH, temperature, ionic strength, chain length
and head group and the amount of choles-
terol incorporated into the bilayer.26 Biologi-
cal stability of liposomes is limited. Cationic
liposomes in plasma are prone to aggregation
and exhibit leakage. High density lipoproteins
are responsible for destabilization of liposomes
prior to interaction of liposomes with circulat-
ing phagocytic cells such as monocytes. The
destabilization of liposomes is due to the lipid
exchange between liposomes and high density
lipids.
54
Drug release27: The drug release from the lipo-
somes can be assessed by the use of well cali-
brated in vitro diffusion cell. The liposome based
formulation can be subjected to in vitro assays
to predict pharmacokinetics and bio availability
of drug before employing costly and time con-
suming in vivo studies. The dilution induced drug
release in buffer and plasma was employed as
predictor for pharmacokinetic performance of
liposomal formulations and another assay which
determined intracellular drug release induced by
liposome degradation in presence of mouse-liver
lysosomelysate was used to assess the bioavail-
ability of the drug.
APPLICATIONS
Cancer chemotherapy28: The long term ther-
apy of anticancer drug leads to several toxic side
effects. The liposomal therapy to the tumour cell
has revolutionized the world of cancer therapy
with least side effects. It has been said that the
small and stable liposomes are passively targeted
to different tumor because they can circulate for
longer time and they can extra vasate in tissue
with enhanced vascular permeability.
The light sensitive liposomes have been pre-
pared, where light triggers the release of antican-
cer drugs, like doxorubicin. The light triggered
system will reduce the potential toxicity and lead
to more effective therapy.29
Gene delivery30: Negatively charged or classical
liposomes have been used as vehicles for gene
transfer into cell in culture. The cationic lipids
are able to interact spontaneously with negatively
charged DNA to form cluster or aggregated ves-
icles along the nucleic acid. At a critical liposome
density the DNA is condensed and becomes
encapsulated with in a lipid bilayer.
Liposomes for topical applications31,32: Lipo-
somes are proved to be effective in deliver-
ing drugs in to the skin. Liposomes increase
the permeability of skin for various entrapped
drugs. Liposomes can exert different functions
after topical application. They can improve drug
deposition within the skin at the site of action
where the goal is to reduce systemic absorption
and thus minimize side effects .They can provide
targeted delivery to skin appendages in addition
to their potential for transdermal delivery.
In the recent studies, it is shown that liposomes
penetrate effectively into hair follicles and thus
hair follicle penetration can be increased by
RGUHS J Pharm Sci | Vol 4 | Issue 2 | AprJune, 2014
 Liposomal Drug Delivery System-A Review
massaging the skin, which stimulates the in vivo
movement of hairs in the hair follicles.33
Liposomes for pulmonary delivery34,35: Tar-
geted drug delivery to the lungs, has evolved
to be one of the most widely investigated sys-
temic or local drug delivery approaches. The
use of drug delivery system for the treatment
of pulmonary diseases is increasing because
of their potential for localized topical therapy
in the lungs. This route also makes it possible
to deposit drugs more site specific at high con-
centrations within the diseased lung there by
reducing the overall amount of drug given to
patients, as well as increasing local drug activ-
ity while reducing systemic side effects and first
pass metabolism.
Liposome for Nasal administration36: For
nasally administered products good penetration,
is of little use if the formulation is not able to
remain in contact with the mucosal surface for a
long enough time to enable penetration to occur.
Therefore mucoadhesion is a key characteristic
of nasally administered formulations.
The liposomes coated with alginates, chitosan or
trimethyl chitosan, which are able to penetrate
through the nasal mucosa and offer enhanced
penetration over uncoated liposomes when deliv-
ered as dry powders. The coating of liposomes
may result in some reduction in encapsulation
efficiency, still maintained between 6069% and
the structural integrity of the entrapped protein
and its release characteristics were maintained.
Liposomes in parasitic diseases37: The conven-
tional liposomes are digested by phagocytic cells
in the body after intravenous management; they
are ideal vehicles for the targeting drug mole-
cules into these macrophages. Leishmaniasis is a
parasitic infection of macrophages which affects
over 100 million people in tropical regions and
is often deadly. The effectual dose of drugs,
mostly different antimonials, is not much lower
than the toxic one. Liposomes accumulate in the
very same cell population which is infected. The
best results reported so far in human therapy are
probably liposomes as carriers for Amphoter-
ecin B in antifungal therapies. This is the drug of
choice in dispersed fungal infections.
Ophthalmic delivery of drugs38: Liposomes
has been investigated for ophthalmic drug deliv-
ery since it offers advantages as a carrier system.
It is biodegradable and biocompatible nano car-
rier. It can enhance the permeation of poorly
RGUHS J Pharm Sci | Vol 4 | Issue 2 | AprJune, 2014
absorbed drug molecules by binding to the cor-
neal surface and improving residence time.
To reduce the drug loss and side effects asso-
ciated with conventional eye drops, a novel
approach was introduced, where the liposomes
made up of dimyristoylphosphatidylcholine are
dispersed in contact lens hydrogels made up
of poly-2-hydroxyethyl methacrylate. The con-
tact lens loaded with hydrogels is transparent in
nature and deliver drugs at therapeutic level for
few days.39
Liposomes for Brain targeting40: The liposo-
mal technology is quite advanced to design with
better site specific action. The basic reason for
the acceptance of liposomal carrier is due to
their controlled profile or drug release nature as
well as due to their selected targeting mechanism.
The surface modified liposomes can be used to
directly encapsulate drug molecules to diseased
tissues or organs.
The brain distribution of liposomes can be modulated
by conjugation of appropriate targeting vectors, like
monoclonal antibody. The mechanism involved in the
concentration of liposomes in brain by crossing blood
brain barriercoupling of liposomes with brain drug
transport vector through absorptive mediated transcys-
tosis or by receptor mediated transcystosis.
CONCLUSION
Liposomes are extremely useful carrier systems for tar-
geted drug delivery. The flexibility of their behavior can
be exploited for the drug delivery through any route of
administration and for any drug material irrespective of
their solubility properties. There is even greater prom-
ise in future for marketing of more sophisticated and
highly stabilized liposomal formulations. The use of
liposomes in the delivery of the drugs and genes are
promising and is sure to undergo further development
in future. The liposomal drug delivery system will rev-
olutionize the vesicular systems with wide application
especially in the treatment of cancer.
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RGUHS J Pharm Sci | Vol 4 | Issue 2 | AprJune, 2014