Deck 17: Peptide and Protein Drug Delivery

Question 1

Fill in the blanks: Peptide and protein drugs are often sought after because of their high ________ and _________.

Answer 1

Specificity,Potency

Question 2

Which of the following are physicochemical differences between small molecule and peptide and protein drugs?

A) Physical Stability
B) Chemical Stability
C) Size
D) Conformational Flexibility
E) All of the Above

Answer 2

E

Question 3

List the four common classifications of amino acids.

Answer 3

Aliphatic,Unsubstituted,Acyclic,Apolar; Aliphatic,Substituted,Acyclic,Polar; Aliphatic,Substituted,Acyclic,Apolar; Cyclic Apolar/Polar

Question 4

Higher-order properties of peptide and protein drugs only depend on amino acid composition,not amino acid order.

Question 5

Which of the following amino acids does not favor α-helix formation?

A) Tyrosine
B) Alanine
C) Glutamic Acid
D) Leucine
E) None of the Above

Question 6

It is often more difficult for peptide and protein drugs than small molecule drugs to permeate cell barriers due to differences in size,polarity,charge,etc.

Question 7

Only large protein drugs are able to permeate by the paracellular route.

Question 8

Fill in the blanks: Most protein and peptide drugs depend on ____________,___________,or ___________ routes of transcellular permeation

Question 9

The average half-life of peptide and protein drugs is shorter than that of small molecule therapeutics due to the enzymatic action of peptidases and proteases.

Question 10

The average half-life of peptide and protein drugs is shorter than that of small molecule therapeutics due to the enzymatic action of peptidases and proteases.

Question 11

Briefly describe the mechanism of adsorptive endocytosis for peptide and protein drugs and how this mechanism is exploited in drug delivery.

Question 12

List three physiological limitations to delivery of oral delivery of peptide and protein drugs

Question 13

Protein and peptide drugs are often very potent and have a narrow therapeutic index

Question 14

Currently marketed protein and peptide drugs exhibit high bioavailabilites.

Question 15

What are the two primary strategies for creating a viable peptide or protein drug for oral delivery?

Question 16

Fill in the blank: The _______________ route of delivery is the most common for peptide and protein drugs.

Question 17

The ω-dihedral angle plays an important role in controlling the primary structure of peptides and proteins.

Question 18

Fill in the blank: The primary adverse reaction to recombinant erythropoietin (EPO) is an example of _______________.

Question 19

Pulmonary delivery of peptide and protein drugs can be utilized for both local and systemic actions.

Question 20

Fill in the blanks: Peptide and protein drugs formulated for pulmonary delivery must have particles of a certain ___________,_____________,and _____________ to for maximum alveolar deposition.

Question 21

List 3 barriers to pulmonary peptide and protein delivery.

Question 22

Nasal delivery is often utilized for peptide and protein drug delivery due to its high surface area.

Question 23

Wider tight junctions found in the nasal cavity lead to increased permeability by what route of permeation?

A) Endocytosis
B) Active Transcellular
C) Paracellular
D) Passive Trancellular
E) Facilitative Transcellular

Question 24

Peptide and protein drug delivery by the nasal route is complicated by disease state mostly due to higher mucus levels leading to increased residence time and half-life.

Question 25

Fill in the blank: Nasal delivery shows promise in delivery of peptide and protein drugs to the brain by allowing API to bypass the ________________ through endocytosis by olfactory cells.

Question 26

Non-invasive,controlled release formulations of peptide and protein drugs for transdermal delivery may increase patient compliance.

Question 27

List 3 physicochemical properties of a peptide or protein drug that will determine its extent of permeation through the transdermal route.

Question 28

Enhancement of peptide and protein permeation through the skin's thick stratum corneum can be accomplished by both chemical permeation enhancers such as _______________,or physical permeation enhancement such as ________________.

Question 29

Permeation through buccal delivery of peptide and protein drugs is greater than in skin due to the presence of saliva.

Question 30

Delivery of insulin through the _______ route is regarded as the Holy Grail of drug delivery.

Question 31

Use of mucoadhesives leads to enhanced absorption through the buccal mucosa due to:

A) Breakdown of tight junctions
B) Increase in pH
C) Increased contact time
D) Solubilization of peptide or protein drugs
E) None of the above

Question 32

List 3 formulation strategies for buccal delivery of peptide and protein drugs.

Question 33

The biggest confounders in mimicking physiological insulin secretion are variability in ___________ and __________.

Question 34

The narrow therapeutic index of insulin combined with inter- and intra-patient variability of absorption through the GI tract reduce the likelihood of replacement of parenteral insulin delivery with oral delivery.

Question 35

Enteric coating of peptide and protein drugs may lead to increased bioavailability due to

A) Protection from low pH
B) Increased residence time in the stomach
C) Protection from gastric enzymes in the stomach
D) All of the above
E) a and c

Question 36

Fill in the blanks: PEGylation,hyperglycosylation,and nanoparticle carriers are all utilized to enhance peptide and protein delivery by increasing ____________.

Question 37

β-sheet conformations are present in a protein to enable longer secondary structural regions to fold back upon themselves.

Question 38

Choose one alternative method of peptide and protein delivery and discuss advantages and weaknesses when compared with peroral delivery.

Question 39

Choose one challenge facing the delivery of protein/peptide drugs and discuss a novel strategy to circumvent this challenge.

Question 40

Several strategies are currently under investigation for increasing the oral absorption of peptides. Please choose one strategy and highlight the critical aspects of the formulation approach that lead to enhanced intestinal absorption.