12: Nanoparticles Flashcards

1
Q

list some challenges of standard drug therapy with conventional dosage forms

A
Low water solubility  
Poor absorption  
Short biological life  
Non-specificity  
Non-selectivity  
Adverse effects and toxicity  
Low cellular uptake
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2
Q

<1nm is classified as

A

molecular

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3
Q

1nm-0.5um is classified as

A

colloidal

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4
Q

all colloids are ____

A

nanomeds

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5
Q

> 0.5um are classifed as

A

coarse

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6
Q

what are some common nanodelivery systems

A
lipid based nanocarriers
polymer based nanocarriers
inorganic nanocarriers
viral nanoparticles
drug conjugates
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7
Q

why are solubilizing agents like cremophor and tweens not used

A

toxicity

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8
Q

what to use instead of cremophor and tweens

A

liposomes

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9
Q

what are 4 reasons to use drug targeting

A

difficulty in accessing site of action + maintaining stability all the way there
unwanted drug effects
lower required dose

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10
Q

describe first order targeting

A

target to diseased organ or tissue

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11
Q

describe second order targeting

A

target to cells in tissue or organ

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12
Q

describe third order targeting

A

target intracellular organelles

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13
Q

a nanomedicine targets T cells in the lymph nodes. what order targeting is this

A

second

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14
Q

3 approaches for drug targeting

A

magic bullet
magic shotgun
prodrug approach

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15
Q

what is the magic bullet approach

A

bio active agents that are both potent and selective to a particular target in the body

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16
Q

preparation of pharmacologically inactive substances that become active at site of action describes the ___ approach

A

prodrug

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17
Q

what is the magic shotgun approach

A

using macromolecule carriers that direct the drug to specific sites in the body

18
Q

what is required to use the prodrug approach of targeting?

A

the enzyme or chemical process involved in its transformation to be present at the active site

19
Q

when a drug is in a carrier, the fat of the drug in vivo will be governed by the

A

physiochemical properties of the carrier

20
Q

taking advantage of normal physiological conditions describes _____ targeting

A

passive

21
Q

blood capillaries are divided into 3 types

A

continuous
fenestrated
sinusoidal

22
Q

how big does your molecule have to be to not pass through continuous endothelium

A

> 2nm

23
Q

how big are the cell junctions between fenetrated capillaries

A

20-80nm

24
Q

why is there enhanced permeability in tumors

A

leaky vasculatur and disorganized tissues

25
Q

why is there an enhanced retention effect at tumor tissues

A

collapsed lymph drainage system = no way to get out

26
Q

what is active targeting

A

taking advantage of overexpression of receptors to get increased cell uptake or specific cell attachment

27
Q

what is physical targeting

A

taking advantage of environmental factors in organs

28
Q

designing a drug to go to an area with low pH is an example of _____ targeting

A

environmental

29
Q

if a drug is released very slowly from the liposome, the PK of the drug reflects the PK of the

A

carrier

30
Q

if a drug is released rapidly from a liposome, then the PK of the drug reflects the

A

PK of the drug

31
Q

when a liposome has a coating that prevents recognition by the phagocytic system, it is called a

A

stealth liposome

32
Q

what are some side effects of doxil or caelyx

A

increased mucositis and hand-foot syndrome

33
Q

the toxicity profile of caelyx vs free doxorubicin is similar to ______ vs_________

A

continuous infusion vs bolus injection

34
Q

why is the drug irinotecan administered in a liposome

A

poor water solubility otherwise

35
Q

what is the difference between nanocapsules and nanospheres

A
nanocapsules = one big reservoir system
nanosphere = many tiny bubbles of drug in the particle
36
Q

what is abraxane and what are its perks

A

an injectable suspension of paclitaxel and albumin, the serum albumin solubilizes and carries the drug = reduction in acute toxicity = can be more aggressively dosed

37
Q

T or F: abraxane’s lowered toxicity is due to being cremophor free

A

T

38
Q

what are the 3 nanodispersed systems for transdermal drug delivery

A

liposomes
nanoemulsion
lipid nanoparticle

39
Q

what is the difference between a nanoemulsion and a lipid nanoparticle

A

nanoemulsion = liquid lipid core

lipid nanoparticle = solid lipid core

40
Q

what is a lipid bilayer enclosing an aueous core

A

liposome

41
Q

what is PNKP

A

DNA repair enzyme that phosphorylates 5 and dephos 3’ to allow DNA ligase to rejoin the strands

a target for anticancer drugs

42
Q

if PNKP is inhibited, cells should become sensitive to

A

IR and TOPI inhibitors