Protein Formulations

Question 1

What two factors determine bio distribution?

Answer 1

Ability of macromolecule to be transported across the endothelium

Difference in relative blood flow to different tissues

Question 2

How are small proteins and oligonucleotides eliminated?

Answer 2

By glomerular filtration In the kidney

Question 3

How are serum proteins and macromolecules eliminated?

Answer 3

By receptors in liver on parenchymal cells and on macrophages

Question 4

Give examples of receptors which clear macromolecules

Answer 4

Asialoglycoprotein receptor ASGPR

N-Acetylgalactosamine/ mannose receptor on macrophages

Flucose receptor on liver parenchymal cells

Question 5

How are other proteins such as albumin and LDLs removed?

Answer 5

Age by becoming acetylated and are cleared by receptor recognising acetylated proteins

Question 6

Once macromolecules are bound to a receptor what happens to them afterwards?

Answer 6

Proteins are endocytosed and sent to lysosomes.

Question 7

Are proteins and peptide drugs well transported and have a high bioavailability?

Answer 7

No and low F

Question 8

Are proteins chemically, physically and biologically stable?

Answer 8

No

Question 9

What does Mw and size depend upon relating to macromolecules?

Answer 9

Shape