Block3 Lecture2 Flashcards

(56 cards)

1
Q

What is the size of a capillary lumen?

A

5-20 microns

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2
Q

What is the USP 32 size requirement for particles greater than 10 microns?

A

less than/equal to 25 particles/mL

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3
Q

What is the USP 32 size requirement for particles greater than 25 microns?

A

less than/equal to 3 particles/mL

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4
Q

What USP chapter regulates particle size in parental products?

A

32

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5
Q

Describe the structure of a liposome.

A

natural phospholipid biomolecules arranged in a spherical bilayer

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6
Q

What are the various morphologies of liposomes?

A

MLV, LUV, SUV, MVV

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7
Q

What is an MLV?

A

multi-lamellar vesicle

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8
Q

What is an LUV?

A

large uni-lamellar vesicle

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9
Q

What is an SUV?

A

small uni-lamellar vesicle

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10
Q

What is an MVV

A

multi-vesicular vesicle

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11
Q

What is the diameter of a large liposome?

A

100 - 200 nm

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12
Q

What is the diameter of a small liposome?

A

less than 100 nm

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13
Q

How do liposomes vary?

A

morpholgy and size

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14
Q

What is the CMC?

A

critical micelle concentration; the point at which micelles precipitate

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15
Q

How is amphotericin B toxic?

A

nephrotoxic - insertion into cell membranes - acute tubular necrosis, even with the deoxycholate form

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16
Q

What side effects does an Amphotericin B infusion cause?

A

N/V, fever, HA, nephrotoxicity

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17
Q

Why does Ambisome offer fewer ADRs compared to Amphotericin B?

A

increased amphob solubility = shorter infusion time, liposomes prevent AmphoB tubular access

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18
Q

How are liposomes synergistic with amphob?

A

liposomes also bind to and disrupt fungal cell membranes

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19
Q

How is ambisome supplied and prepared?

A

as a lyophilized powder, Reconstitute with SWFI and shake for 30 seconds

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20
Q

What is the EPR effect?

A

tumors rapidly neovascularized with leaky vessles and poor lymphatic drainage; thus, small particles accumulate in a tumor

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21
Q

Describe the preparation of Doxil

A

translucent red stealth liposomal dispersion in D5W only

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22
Q

What advantages does Doxil offer over doxorubicin?

A

slower clearance, selective EPR accumulation; decreased cardiotoxicity

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23
Q

How do stealth liposomes have a longer circulation time?

A

PEG coating prevents protein (Ab) binding to decrease phagocytosis and protect from the RES

24
Q

PGA

A

poly(glycolic acid)

25
PLA
poly(lactic acid)
26
PLGA
poly(lactic-co-glycolic acid)
27
PLA-PEG
PLA-poly(ethylene glycol)
28
PCL
polycaprolactone
29
PHB
poly(3-hydroxybutyrate)
30
What is the most commonly used biodegradable polyester?
PLGA
31
Which biodegradable polyesters are bioabsorbed?
PGA & PLA
32
Where is PLGA used?
absorbable sutures, orthopedic implants, SQ/IM depots
33
How does PLGA degrade?
non-enzymatic hydrolysis
34
How do PLGA formulations vary?
1) varying lactic:glycolic ratio; 2) MW from 1-100 kDa
35
What PLGA factors yield slower degradation?
more lactic acid, higher MW
36
What are the 2 types of biodegradable polymers used in CR devices?
polyesters and polyanhydrides
37
Which category of biodegradable polymers degrades quicker?
polyanhydrides
38
What polyesters are used in CR devices?
1) PGA, 2) PLA, 3) PLGA, 4) PLA-PEG, 5) PCL, 6) PHB
39
What polyanhydrides are used in CR devices?
1) pSA, 2) pCPP, 3) pCPP-SA, 4) POE, 5) PBCA
40
pSA
poly(sebacic acid)
41
pCPP
poly(3-carboxyphenoxypropane)
42
pCPP-SA
poly(sebacic-co-3-carobxyphenoxypropane)
43
POE
poly(orthoester)
44
PBCA
poly(butylcyanoacrylate)
45
Where is PBCA used?
GluStitch
46
pH of small intestine
6.2-7.5
47
pH of tumors
6.5
48
pH in inflammation
6.5
49
pH in endosomes
5-6.8
50
pH of lysosomes
4.5-5
51
pH of stomach
2
52
What are types of dispersed solutions used for parental delivery?
1) liposomes, 2) polymeric carriers, 3) CR devices, 4) nanoparticulates
53
Describe the structure of a polymer-drug physical mixture.
drug mixed with polymer and incorporated into microspheres or nanoparticles
54
Describe the structure of a polymer-drug conjugate
drug covalently bound to polymer
55
Describe the structure of a polymer-drug complex.
drug assembled into micelles
56
What are the kinds of polymeric carriers?
1) physical mixtures, 2) conjugates, 3) complexes