Nano and biotech drugs Flashcards
Which of the following is NOT considered a form of nanomedicine?
a. Sirolimus nanocrystal
b. Paclitaxel nanoparticles
c. Spironolactone suspension
d. Doxorubicin liposomes
e. All of the above are nanomedicine
c. Spironolactone suspension
Which of the following is TRUE about Tricor?
a. It consists of drug crystals of fenofibrate of about 100 mm size
b. It is a drug with high water-solubility
c. It is a typical example of new formulation of a BCS Class I drug
d. Its bioavailability is less dependent on taking with food than original fenofibrate
e. It is prepared by lyophilization
d. Its bioavailability is less dependent on taking with food than original fenofibrate
Which of the following is the other name(s) of Abraxane? Choose the BEST answer.
a. Nab-paclitaxel
b. Solvent-free paclitaxel
c. Taxol
d. A and B are both correct
e. A, B and C are all correct
d. A and B are both correct
Which of the following refers to spherical vesicles made of phospholipid bilayers?
a. Liposomes
b. Lipid nanoparticles
c. Quantum dots
d. Micelles
e. Emulsion
a. Liposomes
Which of the following ingredients in a liposomal formulation helps to physically stabilize the
bilayer structure (i.e. to “harden” the liposome)?
a. Tocopherol
b. Hydrogenated soy phophatidylcholine
c. Span 20
d. Distearolyphophatidyl glycerol
e. Cholesterol
e. Cholesterol
A drug X with high Vd (volume of distribution) and short plasma t1/2 (half-life) is reformulated
as liposomal product. The Vd is substantially reduced and t1/2 prolonged. What has happened
according to what I mentioned in class?
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a. Drug X in liposomes becomes much more quickly metabolized
b. Drug X in liposomes is getting cleared by the immune system
c. Drug X in liposomes stays in circulation much longer instead of binding to peripheral
tissues
d. Drug X in liposomes now distribute to the peripheral tissues more extensively than
before
e. Drug X in liposomes must have trapped in certain organs
c. Drug X in liposomes stays in circulation much longer instead of binding to peripheral
tissues
Which of the following is FALSE comparing Fungisome (the new liposomal formulation) with
Fungizone (free drug)?
a. Fungisome penetrates into the brain better
b. Fungisome can be used at higher dose per day than Fungizone
c. Fungisome causes more toxicity in general than Fungizone
d. Fungisome is likely more expensive
e. The drug delivered by fungisome stays in systemic circulation longer
c. Fungisome causes more toxicity in general than Fungizone
Which of the following is NOT a common advantage of nanomedicine?
a. Allow targeted delivery if properly tagged with targeting ligands
b. No risk of flocculation and coalescence
c. May sometimes improve pharmacokinetics
d. Potentially enter inside cells for drug trafficking effect
e. Can sometimes achieve solvent- or surfactant free drug solubilization
b. No risk of flocculation and coalescence
Which of the following excipients of a Doxil (liposome formulation of doxorubicin) allows the
liposomes to stay longer in the circulation without being eliminated by immune system?
a. mPEG -distearolyphophatidyl-glycerol
b. Soy phosphatidylcholine
c. Cholesterol
d. α-Tocopherol
e. water for injection
a. mPEG -distearolyphophatidyl-glycerol
Which of the following is/are TRUE about Abraxane? Please choose the BEST answer?
a. Reconstitution is achieved by injecting the diluent onto the wall of the vial and not directly to
the drug
b. Reconstitution needs to be quickly done at bedside by mixing the diluent with shaking
c. If any foaming or clumping is observed, discard the product right away
d. A and B are both correct
e. A, B and C are all correct
a. Reconstitution is achieved by injecting the diluent onto the wall of the vial and not directly to
the drug
If a nanocarrier is modified with ligands such as monoclonal antibodies to increase its
specificity for a particular tissue or organ, this is known as ____________
a. Targeted delivery
b. Drug solubilization
c. Drug trafficking
d. Stealth delivery
e. Controlled drug release
a. Targeted delivery
A rDNA technology product is
a. a peptide or protein
b. a DNA
c. a RNA
d. a small molecule
e. an antisense macromolecule
a. a peptide or protein
According to what I said in lecture, which of the following molecules is LEAST likely to trigger
an immune response via immunoglobulins?
a. Cholesterol in cell membrane
b. Protein units of the sheath of virus
c. Polysaccharide units on the cell wall of micro-organism
d. Toxins released from bacteria
e. High molecular weight glycoproteins extracted from goat milk
a. Cholesterol in cell membrane
Which of the following is NOT a biotechnology product?
a. Glucagon-like peptides
b. Glucagon
c. Human growth hormone
d. Aspirin
e. Calcitonin
d. Aspirin
Which of the following is FALSE about biotechnology drug products?
a. Often “mechanism driven” targeting a specific pathway
b. May be related to pharmacogenomics
c. Easy to develop generic drugs
d. Often quite potent
e. Often considered biologics
c. Easy to develop generic drugs
Which of the following is/are the potential disadvantages of biotechnology products? Please
choose the BEST answer.
a. High risk of triggering immune responses
b. Highly specific therapeutic activity may not be good for some diseases
c. Limited to oral dosage forms
d. A and B are both correct
e. A, B and C are all correct
d. A and B are both correct
Which of the following is NOT a factor that normally affects whether a recombinant DNA
product dissolves in an aqueous diluent or not?
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a. DNAase concentration in the diluent
b. pH of the diluent
c. Ionic strength of the diluent
d. Molecular weight of the product
e. Amino acid composition of the product
a. DNAase concentration in the diluent
Which of the following peptides has LOWEST water solubility?
a. Contain 4 amino acid units
b. Contain 15% of hydrophobic amino acid and 35% of ionizable amino acid
c. Contain mostly of serine, glutamate and aspartate
d. Contain 50% of tryptophan and phenylalanine plus mostly other neutral amino acids
e. Contain 50% of tryptophan and phenylalanine plus mostly arginine and lysine
d. Contain 50% of tryptophan and phenylalanine plus mostly other neutral amino acids
Many protein drugs may precipitate in the presence of high concentration of oppositely charged
ions. This is known as ________________
a. Salting out
b. Chelation
c. Creaming
d. Ostrich ripening
e. Ionic repulsion
a. Salting out
- Replacing the Fc portion of monoclonal antibody generated from mice with human Fc (i.e. to
“humanize”) is intended to
a. Increase specificity of the antibody
b. Reduce undesirable immune response against the antibody
c. Reduce the cost of production
d. Increase the strength of binding to the antigen
e. Improve bioavailability from the injection site
b. Reduce undesirable immune response against the antibody
When reconstituting some protein drugs such as Neupogen, which of the following is sometimes
added at high concentration to block surface binding of the drugs to the plastic surface?
a. Dextrose
b. Human albumin
c. Sodium chloride
d. Lactose
e. Tween
b. Human albumin
Which of the following is true regarding Lantus insulin?
a. It is a cloudy suspension at pH 4 because the insulin forms microcystals with zinc
b. It is a clear solution at pH 4 because its arginine units are uncharged
c. It is a cloudy suspension at pH 7.4 because it forms fine microcystals with zinc
d. It is a clear solution at pH 7.4 because its arginine units are charged
e. None of the above is true
c. It is a cloudy suspension at pH 7.4 because it forms fine microcystals with zinc
In the table showing the top selling biotech products, which of the following is NOT one of their
therapeutic application?
a. Anticancer
b. Immunosuppression
c. Vaccine
d. Suppression of organ transplant rejection
e. Pain killing
e. Pain killing
In the COVID-19 vaccines, ionizable phospholipids are one of the main ingredients. What is
their main role?
a. Form complexes with mRNA to entrap them in the nanoparticles
b. They provide “stealth” function
c. They stabilize the lipid structure of the nanoparticles
d. They serve as antioxidant
e. They are surfactants to avoid aggregation
a. Form complexes with mRNA to entrap them in the nanoparticles
If you receive a newly marketed product named Gozillakingkongmab and are not sure about its
storage/handling procedures, based on general knowledge about biotech drugs, which of the
following should be avoided? Choose the BEST answer.
a. Vigorous shaking
b. Freezing
c. Refrigeration at 4 o
C
d. A and B should both be avoided
e. A, B and C should all be avoided
d. A and B should both be avoided
Avadar is a high molecular weight glycoprotein (MW = 123 kDa) with some hydrophobic
amino acids, a few anionic, acidic amino acid units and multiple disulphide bridges. What is the
most likely response of Avadar when it is diluted in a vehicle with low pH (e.g. pH 4)?
a. will become more soluble as acidic amino acid units will become charged at low pH
b. will become less soluble as acidic amino acid units will lose their charges at low pH
c. will become more soluble as the disulphide links will become charged at low pH
d. will become less soluble as the disulphide links will lose their charges at low pH
e. will remain soluble regardless of pH change because at this molecular weight, the protein should
be water-soluble
b. will become less soluble as acidic amino acid units will lose their charges at low pH
what is nanomedicine?
small devices with 100-300 nm in diameter to treat a disease or serve as a vehicle to carry therapeutic agents for disease treatment (also for diagnosis)
types of nanomedicine
-nanoparticles/nanospheres
- liposomes
- drug nanocrystals
-micelles
-quantum dots
particles made of solid lipids, polymers, or colloids, used for drug delivery (e.g. lipid nanoparticles, polymer nanoparticles, albumin nanoparticles)
nanoparticles or nanospheres
spherical vesicles made of phospholipids
liposomes
crystalline particle w/ dimension less than 1000 nm and useful for drug delivery when the drug is insoluble in water
nanocrystals
clusters of amphiphilic molecules for delivery of hydrophobic drugs
micelles
10-50 nm semiconductor (e.g. cadmium selenide), more often used for imaging, also proposed for cancer therapy
quantum dots
what type of nanomedicine includes emulsions or microemulsions
quantum dots
nanodelivery refers to
very small vehicles to deliver hard to deliver drugs (BCS class II to IV drugs)
why nanomedicine?
- solubilization of poorly soluble drugs
- prevent degradation of unstable drugs
- favorable PK (e.g longer 1/2 life, higher AUC» improved bioavailability)
-alters tissue distribution (e.g. BBB, can be penetrated by well designed nanosystems) - unique inrxn at cellular and intracellular levels
-targeted delivery
BCS __: immediate dissolution and absorption “plenty of both”
optimal
class 1
BCS __: dissolution limited “limited aqueous solubility”
class 2
BCS __: permeation limited
“too water soluble or not enough permeability”
class 3
BCS __: bioavailability is unpredictable
“ not enough solubility or permeability”
class 4
what type of surface area distribute well on cell membrane (e.g. quantum dots for cell imaging)
large
endocytosis of nanosystems may sneak large therapeutic biomolecules across cell membrane (e.g. gene therapy, therapeutic peptides)
drug trafficking
challenges of nanomedicine
- PK is altered. behaviours of biomaterials also change at nanoscale. patient response can be unpredictable
-antibodies, interferon,etc may also be elicited when being exposed to some polymers, proteins or synthetic lipids - immune system will remove foreign particulate matters through phagocytosis
- extreme large surface area of nanosystems implies vulnerability to flocculation, coalescence
- GMP issue ( control of size , charge, composition, sterility)
-reproducability - upscalability
-regulatory issues
how are nanocrystals manufactured
- downsizing bigger drug crystals (e.g. homogenization,milling)
- micro-precipitation from drug solution
