Deck 8: Multifunctional Nanocarriers for Tumor Drug Delivery and Imaging
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Deck 8: Multifunctional Nanocarriers for Tumor Drug Delivery and Imaging
1
Which of the following problems are usually found in parenteral formulation of anti-cancer drugs?
A) High solubility of anti-cancer drugs
B) Aggregation upon intravenous administration
C) Toxicity related to the use of certain co-solvents or surfactants
D) Non-specific drug-exposure to healthy tissues
E) Long plasma half-lives
A) High solubility of anti-cancer drugs
B) Aggregation upon intravenous administration
C) Toxicity related to the use of certain co-solvents or surfactants
D) Non-specific drug-exposure to healthy tissues
E) Long plasma half-lives
B,C,D,E
2
Which of the following are common characteristics of liposomes?
A) Liposomes are monolayered lipid vesicles that have been used as drug delivery systems for more than 30 years.
B) Liposomes are bilayered lipid vesicles that have been used as drug delivery systems for more than 30 years.
C) Liposome are often composed of fatty acids and cholesterol
D) Liposome are often composed of phospholipids and cholesterol
E) Liposomes are prepared using biocompatible lipids and possess a low toxicity profile.
F) The structure of liposomes allows the incorporation of hydrophilic drugs in their hydrophilic core as well as hydrophobic drugs in the hydrophobic lipid bilayer.
G) Liposomes can be loaded only with water-soluble drugs
A) Liposomes are monolayered lipid vesicles that have been used as drug delivery systems for more than 30 years.
B) Liposomes are bilayered lipid vesicles that have been used as drug delivery systems for more than 30 years.
C) Liposome are often composed of fatty acids and cholesterol
D) Liposome are often composed of phospholipids and cholesterol
E) Liposomes are prepared using biocompatible lipids and possess a low toxicity profile.
F) The structure of liposomes allows the incorporation of hydrophilic drugs in their hydrophilic core as well as hydrophobic drugs in the hydrophobic lipid bilayer.
G) Liposomes can be loaded only with water-soluble drugs
B,D,E,F
3
Which of the following are common characteristics of micelles?
A) Similar to liposomes,micelles are bilayered lipid vesicles but with smaller sizes.
B) Micelles are formed by thermodynamically favored aggregation of amphiphiles at or below Critical Micelle Concentration (CMC).
C) Micelles are formed by thermodynamically favored aggregation of amphiphiles at or above Critical Micelle Concentration (CMC).
D) The CMC is a measure describing the physical properties of the micelle and refers to the micelle's stability.
A) Similar to liposomes,micelles are bilayered lipid vesicles but with smaller sizes.
B) Micelles are formed by thermodynamically favored aggregation of amphiphiles at or below Critical Micelle Concentration (CMC).
C) Micelles are formed by thermodynamically favored aggregation of amphiphiles at or above Critical Micelle Concentration (CMC).
D) The CMC is a measure describing the physical properties of the micelle and refers to the micelle's stability.
B,C,D
4
The suitability of a specific nanocarrier or the location of the drug within the nanocarrier depends on:
A) Potency/efficacy
B) Degradability
C) Molecular weight
D) Solubility
E) Charge of the drug
F) Organoleptic characteristics
A) Potency/efficacy
B) Degradability
C) Molecular weight
D) Solubility
E) Charge of the drug
F) Organoleptic characteristics
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5
Which of the following nanocarriers can adsorb or encapsulate drugs?
A) Liposomes
B) Micelles
C) Nanoparticles
D) Drug-protein conjugates
E) Polyplexes,lipoplexes,dendriplexes
A) Liposomes
B) Micelles
C) Nanoparticles
D) Drug-protein conjugates
E) Polyplexes,lipoplexes,dendriplexes
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6
Which of the following are characteristic features of tumor microenvironment?
A) Hypoxia
B) Low pH
C) Inefficient lymphatic drainage
D) Leaky and hypermeable vasculature
E) Fast blood flow
F) Low interstitial pressure
G) Increased number of overexpressed receptors in cancer cells as compared to normal ones
A) Hypoxia
B) Low pH
C) Inefficient lymphatic drainage
D) Leaky and hypermeable vasculature
E) Fast blood flow
F) Low interstitial pressure
G) Increased number of overexpressed receptors in cancer cells as compared to normal ones
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7
To take advantage of the peculiarities of solid tumors,multifunctional nanocarriers can be modified with different moieties to perform multiple functions. Please match the following moieties with their function.
___ PEG
A) Tumor Imaging
B) Passive Targeting
C) Redox Sensitive
D) Enhanced intracellular delivery
E) Active Targeting
___ PEG
A) Tumor Imaging
B) Passive Targeting
C) Redox Sensitive
D) Enhanced intracellular delivery
E) Active Targeting
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8
To take advantage of the peculiarities of solid tumors,multifunctional nanocarriers can be modified with different moieties to perform multiple functions. Please match the following moieties with their function.
___ Folate
A) Tumor Imaging
B) Passive Targeting
C) Redox Sensitive
D) Enhanced intracellular delivery
E) Active Targeting
___ Folate
A) Tumor Imaging
B) Passive Targeting
C) Redox Sensitive
D) Enhanced intracellular delivery
E) Active Targeting
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9
To take advantage of the peculiarities of solid tumors,multifunctional nanocarriers can be modified with different moieties to perform multiple functions. Please match the following moieties with their function.
___ Disulfide bond containing-lipids or -polymers
A) Tumor Imaging
B) Passive Targeting
C) Redox Sensitive
D) Enhanced intracellular delivery
E) Active Targeting
___ Disulfide bond containing-lipids or -polymers
A) Tumor Imaging
B) Passive Targeting
C) Redox Sensitive
D) Enhanced intracellular delivery
E) Active Targeting
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10
To take advantage of the peculiarities of solid tumors,multifunctional nanocarriers can be modified with different moieties to perform multiple functions. Please match the following moieties with their function.
___ RGD
A) Tumor Imaging
B) Passive Targeting
C) Redox Sensitive
D) Enhanced intracellular delivery
E) Active Targeting
___ RGD
A) Tumor Imaging
B) Passive Targeting
C) Redox Sensitive
D) Enhanced intracellular delivery
E) Active Targeting
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11
To take advantage of the peculiarities of solid tumors,multifunctional nanocarriers can be modified with different moieties to perform multiple functions. Please match the following moieties with their function.
___ Gadolinium
A) Tumor Imaging
B) Passive Targeting
C) Redox Sensitive
D) Enhanced intracellular delivery
E) Active Targeting
___ Gadolinium
A) Tumor Imaging
B) Passive Targeting
C) Redox Sensitive
D) Enhanced intracellular delivery
E) Active Targeting
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12
Which of the following statements are true about conjugation polymers and ligands to nanocarrier's surface?
A) Conjugation of proteins or polymers can proceed covalently and non-covalently
B) Reactive thiol-groups are preferred in protein bioconjugation because they are less ubiquitous than carboxylic ones
C) Activation of carboxylic groups can drive protein-to protein crosslinking
D) Protein-to protein crosslinking often increases the binding activity of proteins attached to the nanocarrier.
E) Proteins and polymers capped with lipidic moieties can be easily adsorbed in the hydrophobic surface of nanoparticles or in liposome membranes
A) Conjugation of proteins or polymers can proceed covalently and non-covalently
B) Reactive thiol-groups are preferred in protein bioconjugation because they are less ubiquitous than carboxylic ones
C) Activation of carboxylic groups can drive protein-to protein crosslinking
D) Protein-to protein crosslinking often increases the binding activity of proteins attached to the nanocarrier.
E) Proteins and polymers capped with lipidic moieties can be easily adsorbed in the hydrophobic surface of nanoparticles or in liposome membranes
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13
Which of the following ligands can be attached to the surface of the nanocarriers to provide active targeting towards tumors?
A) anti-HER-2 mAb (monoclonal antibody)
B) Folate
C) PEG
D) Cy5.5
E) anti-EGFR Fab' (mAb fragments)
A) anti-HER-2 mAb (monoclonal antibody)
B) Folate
C) PEG
D) Cy5.5
E) anti-EGFR Fab' (mAb fragments)
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14
Which of the following statements are true about PEG?
A) PEG stands for Polyethyleneglycol
B) The most common method for prolonging the circulation and improving the biocompatibility of nanocarriers is to cover their surface with hydrophilic polymers,such as polyethylene glycol (PEG).
C) Introduction of PEG blocks in nanocarriers decreases their opsonization and their clearance by MPS (mononuclear phagocyte system).
D) Despite its wide use in drug delivery,PEG is not approved by the FDA
E) In addition to its protective function,PEG is often used as a spacer arm to attach ligands to nanocarriers
A) PEG stands for Polyethyleneglycol
B) The most common method for prolonging the circulation and improving the biocompatibility of nanocarriers is to cover their surface with hydrophilic polymers,such as polyethylene glycol (PEG).
C) Introduction of PEG blocks in nanocarriers decreases their opsonization and their clearance by MPS (mononuclear phagocyte system).
D) Despite its wide use in drug delivery,PEG is not approved by the FDA
E) In addition to its protective function,PEG is often used as a spacer arm to attach ligands to nanocarriers
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15
Increasing the solubility of poorly soluble chemotherapeutics with traditional formulation leads to toxicity and side effects.
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16
EPR effect is the limiting barrier for tumor drug delivery.
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17
Site-specific therapy is possible because of the presence of an increased number of overexpressed receptors on tumor cells when compared to normal cells.
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18
Passive targeting approaches are feasible due to EPR effect.
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19
PEG is used as an intracellular delivery moiety on different nanocarriers.
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20
Ultrasound,magnetic field,temperature and light are Local/external stimuli sensitivity
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21
Opsonization is the interaction of nanocarriers with the cell membrane.
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22
Passive tumor targeting relies on the EPR phenomenon.
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23
To benefit from EPR effect,nanocarriers should have a long-circulating property.
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24
Temperature-sensitive liposomes frequently include dipalmitoylphosphatidylcholine (DPPC) as a key component.
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25
The overall slightly positive charge of the nanocarrier facilitates the interaction of the particle with proteoglycans responsible for the negative charge on the cell surface.
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26
Cell-penetrating peptides (CPP) are short peptides that facilitate cellular uptake of various molecular cargos.
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27
CPP-mediated transport of large molecules and nanoparticles has been reported to occur via energy-dependent routes.
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28
Mononuclear phagocyte system (MPS) is primarily responsible for nanocarrier clearance from body.
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29
What features of nanocarriers enhance the efficacy of cancer drug delivery?
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30
What type of drugs can be encapsulated into nanocarriers?
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31
Name one of the strategies used to extend the half-life of the delivery system without imparting the elimination phase?
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32
What are the elimination sites (organs) of the nanocarrier from the body?
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33
What are the structural differences between solid tumor site and normal tissues?
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34
What is the EPR effect (enhanced permeability and retention effect)?
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35
What is the common method to prolong circulation of nanocarriers?
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36
Define passive and active targeting.
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37
What are some of the local condition/stimuli that can be used to trigger release of cargo from multifunctional nanocarriers?
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