Definition of Surfactant
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APPLICATION OF NIOSOMES
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A) Ophthalmic Drug Delivery
o From ocular dosage form like ophthalmic solution, suspension and ointment it is
difficult to achieve excellent bioavailability of drug due to the tear production,
impermeability of corneal epithelium, non-productive absorption and transient
residence time.Niosomes are nonionic
surfactant based multi
lamellar or unilamellar
vesicles in which an
aqueous solution of
solute(s) is entirely
enclosed by a membrane
resulted from the
organization of surfactant
macromolecules as bilayers
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?Excellent unique features and abilities make these surfactants a potential
candidate for a wide range of applications in various bio-medicinal fields
such as dermatology, drug delivery, anticancer treatment, surfactant therapy,
vaccine formulation, personal hygiene care products and many more.They are surface-active compounds having the ability to
decrease surface and interfacial tension at the interfaces
between gases, liquids, and solids, thus enabling them to
blend or diffuse voluntarily like emulsions in water or
other liquids.The vesicles forming
amphiphile is a non-
ionic surfactant
stabilized by addition of
cholesterol and small
amount of anionic
surfactant such as
dicetyl phosphate
NIOSOMES
Figure 3: Vesicle of niosome (Aitha S, 2013)
Figure 4: Structure of Niosomes
STRUCTURE OF
NIOSOMES
?Addition of cholesterol molecule to
Niosomal system
oMakes the membrane rigid
oReduces leakage of drug from the
Niosome
oIncreases the chain order of bilayer
oStrengthen the non-polar tail of the
non-ionic surfactant
oIncrease in the entrapment efficiency
MEMBRANE ADDITIVES
Cholesterol
?Over the decades many researchers have reported the antimicrobial, anti-
adhesive, antibiofilm, anti-inflammatory, antioxidant activities of
surfactants regarding its utility in medicinal purposes.Niosomes vesicle would
consist of a vesicle
forming amphiphile i.e. a
non-ionic surfactant such
as Span- 60, which is
usually stabilized by the
addition of cholesterol
Figure 5: Structure of niosome (Makeshwar KB, 2013)
?oNiosomes prepared by the span 60 has high resistance
against proteolyticenzyme and exhibit good stability in
storage temperature and in presence of sodium deoxycholate
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Improve Drugs Stability and Physical
Properties
?The surfactants play an active part in the designing and
manufacturing of industrial and customer products,
comprising cosmetics, detergents, paints, paper products,
and pharmaceuticals.Surfactants after reaching their CMC (Critical
Micellar Concentration) produce micelles/reverse
micelles which indeed work as nano-sized supra-
molecules in solubilization, emulsification of drugs.Examples: Dicetyl phosphate (DCP) and Stearyl
amine (SA)
MEMBRANE ADDITIVES
NIOSOME DELIVERY
APPLICATIONS
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Other Application
i. Sustained release
Sustained release action of niosomes can be applied to drugs
which have low therapeutic index and have low solubility with
water since those could be maintained in the circulation via
niosomal encapsulation.The formation of bilayer vesicles rather than micelles depends
on the hydrophilic-lipophilic balance (HLB) of the surfactant,
and the chemical structure of the components
Composition of Spanlastics
?The kind of fatty acid connected to the polyoxyethylene sorbitan component of
the molecule determines the shape of Spans: Span80 (monooleate), Span60
(monostearate), Span40 (monopalmitate), and Span 20.o The cationic, anionic, zwitterionic and neutral
surfactants have their specific applications in
bio-medicinal and pharmaceutical fields.The drug interacts with surfactant
head groups and develops the
charge that creates mutual
repulsion between surfactant
bilayers, and hence increases
vesicle size.Charge inducers are one of the membrane
additives which are often included in Niosomes
because
?Increase surface charge density
?Prevent vesicles flocculation, Aggregation and Fusion.Niosomes of doxorubicin prepared from C16 monoalkylglycerol ether with or
without cholesterol, exhibited an increased level of doxorubicin in tumor cells,
serum and lungs, but not in liver and spleen.o Transdermal drug delivery system of niosomes and proniosomes has led to
increasing the penetration rate thereby enhancing therapeutic efficiency and
bioavailability of the drug .ii. Localized drug action
Drug delivery through niosomes is one of the approaches to
achieve localized drug action, since their size and low
penetrability through epithelium and connective tissue keeps the
drug localized at the site of administration.However, the produced vesicles are more sustainable in Span 60 contains
saturated alkyl chains
Composition of Spanlastics
?The last few decades displayed an enormous curiosity in
work related to the synthesis of surfactants from natural
products such as sugar-based surfactants fatty acids and
sterols.This wonderful quality of surfactants is most useful in
the bio-medical and bio-chemical fields to improve
production, purification and delivery of drugs
Classification of surfactants
o According to the charge of the head groups,
surfactants are classified into four different
categories.Niosomal dispersion in an aqueous phase can be emulsified in a nonaqueous
phase to
Regulate the delivery rate of drug
Administer normal vesicle in external non-aqueous phase.Spanlastics are novel nanovesicular
carriers composed of non-ionic
surfactants or a blend of
surfactants, along with an edge
activator.Ethanol's capacity to condense on membranes results in a reduction
in vesicular membrane thickness, which in turn leads to smaller
vesicles.Structurally these two groups are contradictory in directions, but
their ends are linked to the same molecule, developing an
asymmetric and polar structure.Mean size of Niosomes
increases proportionally
with increase in the HLB
of surfactants
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?Targeting and Retention of Drug in Blood Circulation
Liver Targeting:
Methotrexate was reported to be selectively taken up by liver cells after
administration as a niosomaldrug delivery system.Spanlastics have shown enhanced
therapeutic efficacy, improved drug
bioavailability, and reduced drug
toxicity compared to other drug
delivery systems.Non-ionic surfactants are the foremost ordinary type of
surfactant employed in preparing vesicles, due to their superior
advantages.They convey better stability, compatibility, and low toxicity
related to their anionic, amphoteric ,or cationic surfactants.By adjusting the system's net charge towards a negative zeta
potential, steric stability is achieved to some extent
Composition of Spanlastics
?One portion is hydrophilic in nature and soluble in an aqueous
medium, while the second portion is lipophilic, which is soluble in
oil but insoluble in an aqueous medium.Composition of Surfactant
o In surfactant molecules, the hydrophilicity and
lipophilicity alter with molecular composition and
arrangement.These surfactants are fascinating as they usually are
effortlessly biodegraded
Importance of Surfactants
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?Most of the pharmaceutical products show poor aqueous solubility and, in
this regard, surfactants are inevitable to influence the solubility of the
products.Surfactants used in preparation are biodegradable, biocompatible and non-
immunogenic
FEATURES OF NIOSOMES
?Improve the therapeutic performance of the drug molecules by
Delayed clearance from the circulation
Protecting the drug from biological environment
Restricting effects to target cells
?Type of surfactant
influences encapsulation
efficiency, toxicity, and
stability of Niosomes
?Improve Anti-inflammatory Activity
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NIOSOME DELIVERY
APPLICATIONS
?Beside this, the percent entrapment efficiency of
gentamicin sulphate was altered when administered as niosomes .With the formulation of niosomes, the oral bioavailability of
the Acyclovir as well as Griseofulvin was increased as
compared to the drug alone.Important tool for immunological selectivity, low toxicity and more stability of
the incorporated active moiety.3/15/2024 Dr. Doaa Hussien Hassen 34
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Carrier for hemoglobin
Niosomes used as hemoglobin carriers.In general, the physical form of Niosomes did not influence
their toxicity as evident in a study comparing the formulations
prepared in the form of liquid crystals and gels.Vesicles based on Span 80 and Span 40 exhibit significant disruption,
aggregation, and instability.The molecules of surfactant possess amphiphilic arrangement
providing an allurement for both water and oil.o Both water-soluble and oil- soluble yields a significant
physio-chemical consideration of surfactant use.Surfactants are amphoteric and solubilize both
organic and inorganic substances.surfactants: are important in
pharmaceutical dosage development
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?surfactants: are important in
pharmaceutical dosage development
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?In medicinal drinks, surfactants are used to solubilize Vitamin E, D, other
medicinal materials, and other necessary oil ingredients.Surfactants are useful in ointments formulations as well as in case of
creams, lubricants and gels.Exhibits flexibility in their structural characteristics (composition, fluidity and
size)
?Non-ionic surfactants
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