لخّصلي

Definition of Surfactant ? 3/15/2024 Dr. Doaa Hussien Hassen 31 APPLICATION OF NIOSOMES 32 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 3/15/2024 Dr. Doaa Hussien Hassen 16 ?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 3/15/2024 Dr. Doaa Hussien Hassen 33 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 ?37 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 3/15/2024 Dr. Doaa Hussien Hassen 25 ?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 3/15/2024 Dr. Doaa Hussien Hassen 8 ?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 3/15/2024 Dr. Doaa Hussien Hassen 30 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 35 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 3/15/2024 Dr. Doaa Hussien Hassen 12 ?surfactants: are important in pharmaceutical dosage development 3/15/2024 Dr. Doaa Hussien Hassen 13 ?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 ????????????????????????2.?????????????????????????

Definition of Surfactant
 Surfactants
 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.
 These compounds are nonbiodegradable and usually toxic
to the environment
Composition of Surfactant
▪ Surfactant molecules structurally consist of two portions:
▪ 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.
▪ Structurally these two groups are contradictory in directions, but
their ends are linked to the same molecule, developing an
asymmetric and polar structure.
▪ The molecules of surfactant possess amphiphilic arrangement
providing an allurement for both water and oil.
▪ Usually, the hydrophilic group possesses -SO3H, - COOH, and a
polyoxyethylene chain;
▪ While lipophilic group normally possesses -CF2,-CF, - Si, and a
polyoxypropylene chain.
Composition of Surfactant
• In surfactant molecules, the hydrophilicity and
lipophilicity alter with molecular composition and
arrangement.
• For example, when the lipophilic group is weaker than
the hydrophilic, the surfactant becomes water-soluble
• It becomes oil-soluble surfactant when a lipophilic group
is stronger than hydrophilic part.
• Both water-soluble and oil- soluble yields a significant
physio-chemical consideration of surfactant use. It is a
significant source for a realistic surfactant’s choice. Importance of Surfactants
3/15/2024 Dr. Doaa Hussien Hassen
7
 The surfactants play an active part in the designing and
manufacturing of industrial and customer products,
comprising cosmetics, detergents, paints, paper products,
and pharmaceuticals.
 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.
 These surfactants are fascinating as they usually are
effortlessly biodegraded
Importance of Surfactants
3/15/2024 Dr. Doaa Hussien Hassen
8
 Surfactants are amphoteric and solubilize both
organic and inorganic substances.
 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.
 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
• According to the charge of the head groups,
surfactants are classified into four different
categories.
• The cationic, anionic, zwitterionic and neutral
surfactants have their specific applications in
bio-medicinal and pharmaceutical fields. surfactants: are important in
pharmaceutical dosage development
3/15/2024 Dr. Doaa Hussien Hassen
12
 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 mainly used as an active component of emulsion and act as
stabilizer.
 The self-assembly property of surfactants is a very powerful function for
drug delivery systems .
 Most of the pharmaceutical products show poor aqueous solubility and, in
this regard, surfactants are inevitable to influence the solubility of the
products.
surfactants: are important in
pharmaceutical dosage development
3/15/2024 Dr. Doaa Hussien Hassen
13
 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. They are also used to enhance the extent of
drug absorption as well as drug penetration. Besides that, surfactants are
also used to stabilize semisolid formulations .
 Over the decades many researchers have reported the antimicrobial, anti-
adhesive, antibiofilm, anti-inflammatory, antioxidant activities of
surfactants regarding its utility in medicinal purposes. In some reports
surfactants are found to have spermicidal and laxative activity too
Niosomes
 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
3/15/2024 Dr. Doaa Hussien Hassen 16
 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
 similar to liposomes, in that
they are also made up of a
bilayer.
 However, the bilayer in the case
of Niosomes is made up of non-
ionic surface-active agents
rather than phospholipids.
 Made of a surfactant bilayer
with its hydrophilic ends
exposed on the outside and
inside of the vesicle, while the
hydrophobic chains face each
other within the bilayer. STRUCTURE OF NIOSOMES
 vesicle holds hydrophilic
drugs within the space
enclosed in the vesicle,
while hydrophobic drugs
are embedded within the
bilayer itself.
 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)
 Entrap solutes in a manner analogous to liposomes.
 Accommodate the drug molecules with a wide range of solubility.
 Exhibits flexibility in their structural characteristics (composition, fluidity and
size)
 Performance of the drug molecules is increased.
 Better availability to the particular site by protecting the drug from biological
environment.
 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
 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.
 Handling and storage of surfactants requires no special conditions.
 Bioavailability of poorly absorbed drugs is increased.
 Targeted to the site of action by oral, parenteral as well as topical routes.
ADVANTAGES OF NIOSOMES
DELIVERY SYSTEM
 According to the nature of lamellarity

1. Multilamellar vesicles (MLV) 1-5 μm in size.


2. Large Unilamellar vesicles (LUV) 0.1– 1μm in size


3. Small Unilamellar vesicles (SUV) 25– 500 nm in size.
    According to the size


4. Small Niosomes (100 nm– 200 nm)


5. Large Niosomes (800 nm– 900 nm)


6. Big Niosomes (2 μm– 4 μm ) NATURE OF SURFACTANT
    Type of surfactant
   influences encapsulation
   efficiency, toxicity, and
   stability of Niosomes
    Mean size of Niosomes
   increases proportionally
   with increase in the HLB
   of surfactants
   3/15/2024 Dr. Doaa Hussien Hassen 25
    The surfactant/lipid ratio is generally
   10-30 mM (1-2.5% w/w)
    Increasing the surfactant/lipid level
   increases the total amount of drug
   encapsulated
   SURFACTANT AND LIPID
   LEVELS
   NATURE OF THE DRUG
    The Physio-chemical properties
   of encapsulated drug influence
   charge and rigidity of the
   Niosome bilayer.
    The drug interacts with surfactant
   head groups and develops the
   charge that creates mutual
   repulsion between surfactant
   bilayers, and hence increases
   vesicle size.
    The aggregation of vesicles is
   prevented due to the charge
   development on bilayer.
   Table 1: Effect of the nature of drug on
   formation vesicle (Kazi KM et al, 2010)
   CHOLESTEROL
    Addition of cholesterol molecule to
   Niosomal system
   •Makes the membrane rigid
   •Reduces leakage of drug from the
   Niosome
   •Increases the chain order of bilayer
   •Strengthen the non-polar tail of the
   non-ionic surfactant
   •Increase in the entrapment efficiency
   MEMBRANE ADDITIVES
   Cholesterol
    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.
    Examples: Dicetyl phosphate (DCP) and Stearyl
   amine (SA)
   MEMBRANE ADDITIVES
   NIOSOME DELIVERY
   APPLICATIONS
    The applications can be mainly classified into three categories
    1 )For Controlled Release of Drugs
    Ophthalmic Drug Delivery
    2) To Improve the Stability and Physical Properties of the Drugs
    To Increase Oral Bioavailability
    For Improvement of Stability of Peptide Drugs
    To Promote Transdermal Delivery of Drugs
    Improvement of Stability of Immunological Products
    Improve Anti-inflammatory Activity
   3/15/2024 Dr. Doaa Hussien Hassen 30
   NIOSOME DELIVERY
   APPLICATIONS
    3) For Targeting and Retention of Drug in Blood Circulation
    For Liver Targeting
    To Improve the Efficacy of Drugs in Cancer Therapy
    In Treatment of Localized Psoriasis
    In Leishmaniasis
    In Diagnostic Imaging
    Carrier for Haemoglobin.
   3/15/2024 Dr. Doaa Hussien Hassen 31
   APPLICATION OF NIOSOMES
   32
   A) Ophthalmic Drug Delivery
   • 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.
   • But niosomal and liposomal delivery systems can be used to achieve good
   bioavailability of drug.
   Example :
   • Experimental results of the water-soluble antibiotic Gentamicin sulphate showed a
   substantial change in the release rate . Beside this, the percent entrapment efficiency of
   gentamicin sulphate was altered when administered as niosomes . Also, as compared to
   normal drug solution, niosomes of drug show slow release
   Improve Drugs Stability and Physical
   Properties
    Increase Oral Bioavailability:
    With the formulation of niosomes, the oral bioavailability of
   the Acyclovir as well as Griseofulvin was increased as
   compared to the drug alone.
    Improvement of Stability of Peptide Drugs:
    •Niosomes prepared by the span 60 has high resistance
   against proteolyticenzyme and exhibit good stability in
   storage temperature and in presence of sodium deoxycholate
   3/15/2024 Dr. Doaa Hussien Hassen 33
   Improve Drugs Stability and Physical
   Properties
    To Promote Transdermal Delivery of Drugs
    Many drugs such as lidocaine, estradiol, cyclosporine etc. are used for topical
   and transdermal drug delivery system by formulating them as niosomes
    Improvement of Stability of Immunological Products:
    Important tool for immunological selectivity, low toxicity and more stability of
   the incorporated active moiety.
    Niosomesare better stimulant of IgG2.
    Improve Anti-inflammatory Activity:
    •Niosomal formulation of diclofenacsodium prepared with 70% cholesterol
   showed greater anti-inflammatory effect as compared to the free drug.
   3/15/2024 Dr. Doaa Hussien Hassen 34
   35
   Carrier for hemoglobin
   Niosomes used as hemoglobin carriers.
   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.
   Improve the Efficacy of Drugs in Cancer Therapy:
   Niosomes can also be used as a suitable delivery system for the administration of
   drugs like 5-FU.
   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.
   36
   Transdermal delivery of drugs through niosomes and proniosomes
   • The major drawback of transdermal drug delivery is the slow penetration
   through the skin.
   • Transdermal drug delivery system of niosomes and proniosomes has led to
   increasing the penetration rate thereby enhancing therapeutic efficiency and
   bioavailability of the drug .
   37
   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.
   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.
    Unfortunately, there is not enough research conducted to
   investigate toxicity of Niosomes.
    It was determined that the ester type surfactants are less toxic
   than ether type surfactants.
    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.
    Nasal applications of these formulations caused toxicity in the
   case of liquid crystal type Niosomes.
   TOXICITY OF NIOSOMES
   Spanlastic
    Spanlastics are novel nanovesicular
   carriers composed of non-ionic
   surfactants or a blend of
   surfactants, along with an edge
   activator.
    They have an elastic and
   deformable nature, allowing them
   to carry a wide range of drug
   molecules and penetrate the skin
   for transdermal drug delivery.
    Spanlastics have shown enhanced
   therapeutic efficacy, improved drug
   bioavailability, and reduced drug
   toxicity compared to other drug
   delivery systems. Composition of Spanlastics
    Non-ionic surfactants
    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.
    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
    Non-ionic surfactants
    One significant group of nonionic surfactants is the sorbitan alkylesters (Spans).
    The organization of Spans into concentric bilayers gives Spanlastics its vesicular
   structure.
    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.
    Vesicles based on Span 80 and Span 40 exhibit significant disruption,
   aggregation, and instability.
    However, the produced vesicles are more sustainable in Span 60 contains
   saturated alkyl chains
   Composition of Spanlastics
    Ethanol:
    The characteristics of these nano-vesicular carriers are improved by
   ethanol.
    It aids in enhancing drug entrapment and partitioning within the
   vesicles.
    Ethanol’s capacity to condense on membranes results in a reduction
   in vesicular membrane thickness, which in turn leads to smaller
   vesicles.
    By adjusting the system’s net charge towards a negative zeta
   potential, steric stability is achieved to some extent
   Composition of Spanlastics
    Spanlastics have concentric bilayers that resemble liposomes.
    These come in both unilamellar and multilamellar (MLV)
   varieties.
    Depend into their size, these may be (SUVs) small unilamellar
   vesicles (10-100nm) or (LUVs) large unilamellar vesicles
   (100-3000nm).
    The term "spanlastic systems“ refers to spheroid structures
   composed of amphiphilic molecules that exhibit exceptional
   properties as a matrix for bioencapsulation
   Morphology of Spanlastics
    Edge activators (EAs) induce a reduction in the stability of lipid bilayers, hence enhancing
   the deformability of vesicles.
    These vesicles’ surfactant induces holes in membranes and other lipid structures, and at
   greater concentrations, it also promotes solubilization (lysis).
    As a result, elastic vesicles can squeeze through intercellular spaces when a water gradient is
   present.
    There are two drug penetration mechanisms:
    The first mechanism: The intercellular lipid lamellae are altered as a result of the elastic
   vesicles’ interactions and penetration-enhancing functions with the epithelial cell membrane.
    The second mechanism: When used as drug delivery systems, elastic vesicles allow intact
   drug-carrying vesicles to breach biological membranes and transit through intercellular
   spaces.
   Leciplex
    Leciplex is self-assembled phospholipid based cationic
   nanocarriers for the improved delivery of hydrophobic drugs.
    The advantage of leciplex over traditional vesicular systems is in
   simplicity of preparation as it is a one-step fabrication process
   that yields nanosized vesicular systems by simple mixing.
    The major components of a leciplex system are soy
   phosphatidylcholine (SPC), a cationic agent and a bio-
   compatible solvent like Transcutol
   3/15/2024 Dr. Doaa Hussien Hassen 48
   Quatsomes
    Quatsomes are unilamellar nanovesicles made mainly of cholesterol and
   quaternary ammonium surfactants (QAS).
    Quatsomes have excellent stability, homogeneity ,and high drug-loading
   capacity.
    In addition, quatsomes enhance the bioactivity and stability of proteins.
    Furthermore, quatsomes can be labeled with fluorescent dyes for
   bioimaging and biodistribution assays
    Therefore, quatsomes are considered promising alternatives to
   conventional liposomes.
   3/15/2024 Dr. Doaa Hussien Hassen 49
   Quatsomes
    Moreover, the presence of QAS that possess antimicrobial activity in the
   components of quatsomes is considered beneficial intreating wounds.
    However, the cationic nanoparticles formulated with QAS, especially with
   dimethyldidodecyl ammonium bromide (DDAB) or cetyltrimethyl
   ammonium bromide(CTAB), bear a greater risk of toxicity, despite several
   studies that pointed out that the toxicity of QAS has been greatly
   diminished after association with lipidic molecules as soylecithin
    further studies are needed to assess the toxicity of quatsomes
   3/15/2024 Dr. Doaa Hussien Hassen 50
   Bilosomes
    Bilosomes are elastic nano-sized colloidal carriers similar to niosomes in structural
   composition (non-ionic surfactant and cholesterol) but incorporating bile salts.
    Bile salt acts also as permeability enhancer through biological barriers including the
   intestinal membrane and blood brain barrier (BBB).
    Moreover, Bile salt gives the vesicles a negative charge which provide higher storage
   stability and promote drug uptake through M-cells in the Peyer’s patch followed by
   cellular processes which extend into the underlying lymphoid tissue leading to drug
   transport via intestinal lymphatic system as well as the avoidance of hepatic first pass
   metabolism.
    Bilosomes have been reported to enhance oral bioavailability of many drugs as reported
   in several literatures