nanoparticles revised

Question 1

why are nanoparticles considered for drug delivery?

Answer 1

can be injected via IV
has unique distribution
can enter cells with proper surface modification
can potentially modify distribution of a drug to increase drug delivery to target tissues via IV

Question 2

types of nanoparticulate drug delivery systems

Answer 2

micelles/polymeric micelles
liposomes
protein nanoparticles (albumin)
polymeric nanoparticles

Question 3

micelles/polymeric micelles

Answer 3

surfactant (hydrophobic head and hydrophilic tails) molecules aggregate in aqueous solution to form micelles at certain concentration and temperature

Question 4

liposomes

Answer 4

vascular structures created from lipid bilayers
phospholipids and cholesterol

Question 5

albumin

Answer 5

natural carrier of hydrophobic molecules in blood

Question 6

albumin functions

Answer 6

reversibly bind to hydrophobic substances
facilitate endothelial transcytosis of albumin-bound drug through binding to gp60 receptor
preferential intratumoral accumulation of paclitaxel via binding to SPARC

Question 7

SPARC

Answer 7

secreted protein acidic and rich in cysteine
an extracellular matrix glycoprotein over expressed in a variety of cancers
album binds to it

Question 8

types of polymeric nanopartilces

Answer 8

all amphiphilic block-copolymer PLA
PAA
PGA

Question 9

polymeric nanoparticle function

Answer 9

help solubilize hydrophobic drugs in water
less toxic than surfactants
lower CMC so smaller amount of surfactants can be used

Question 10

taxol

Answer 10

paclitaxel and cremophor el
indications
- first line treatment of advanced carcinoma of ovary
- adjuvant treatment of node positive breast cancer
- first line treatment of non-small cell lung cancer
- 2nd line treatment of AIDS-releated Kaposi’s sarcoma

Question 11

usage of paclitaxel

Answer 11

used in taxol to prevent depolymerization of microtubules
bark of a pacific yew tree that is prepared via semi-synthetic process and is highly lipophilic and insoluble in water

Question 12

cremophor el

Answer 12

used in taxol as a non-ionic surfactant

Question 13

doxil

Answer 13

composed of doxorubicin HCl and PEGylated liposomes
side effect - hand foot syndrome
indications:
- ovarian cancer
- AIDs related Kaposi’s sarcoma
- multiple myeloma

Question 14

doxorubicin HCl

Answer 14

used in doxil as a DNA-intercalating agent
functions as topoisomerase-2 inhibitor

Question 15

PEGylated liposome

Answer 15

used in doxil
liposome decroated with PEG
also known as caelyx

Question 16

abraxane

Answer 16

paclitaxel protein-bound particles for injectable suspension (10% paclitaxel, 90% albumin)
indication:
- treatment of metastatic breast cancer

Question 17

reasoning for abraxane usage

Answer 17

free of solvents and surfactants so avoids related complications
the max tolerated dose is 50% higher than typical dose of taxol