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Drew 924 > Block3 Lecture2 > Flashcards

Block3 Lecture2 Flashcards

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
Q

PLA

A

poly(lactic acid)

26
Q

PLGA

A

poly(lactic-co-glycolic acid)

27
Q

PLA-PEG

A

PLA-poly(ethylene glycol)

28
Q

PCL

A

polycaprolactone

29
Q

PHB

A

poly(3-hydroxybutyrate)

30
Q

What is the most commonly used biodegradable polyester?

A

PLGA

31
Q

Which biodegradable polyesters are bioabsorbed?

A

PGA & PLA

32
Q

Where is PLGA used?

A

absorbable sutures, orthopedic implants, SQ/IM depots

33
Q

How does PLGA degrade?

A

non-enzymatic hydrolysis

34
Q

How do PLGA formulations vary?

A

1) varying lactic:glycolic ratio; 2) MW from 1-100 kDa

35
Q

What PLGA factors yield slower degradation?

A

more lactic acid, higher MW

36
Q

What are the 2 types of biodegradable polymers used in CR devices?

A

polyesters and polyanhydrides

37
Q

Which category of biodegradable polymers degrades quicker?

A

polyanhydrides

38
Q

What polyesters are used in CR devices?

A

1) PGA, 2) PLA, 3) PLGA, 4) PLA-PEG, 5) PCL, 6) PHB

39
Q

What polyanhydrides are used in CR devices?

A

1) pSA, 2) pCPP, 3) pCPP-SA, 4) POE, 5) PBCA

40
Q

pSA

A

poly(sebacic acid)

41
Q

pCPP

A

poly(3-carboxyphenoxypropane)

42
Q

pCPP-SA

A

poly(sebacic-co-3-carobxyphenoxypropane)

43
Q

POE

A

poly(orthoester)

44
Q

PBCA

A

poly(butylcyanoacrylate)

45
Q

Where is PBCA used?

A

GluStitch

46
Q

pH of small intestine

A

6.2-7.5

47
Q

pH of tumors

A

6.5

48
Q

pH in inflammation

A

6.5

49
Q

pH in endosomes

A

5-6.8

50
Q

pH of lysosomes

A

4.5-5

51
Q

pH of stomach

A

2

52
Q

What are types of dispersed solutions used for parental delivery?

A

1) liposomes, 2) polymeric carriers, 3) CR devices, 4) nanoparticulates

53
Q

Describe the structure of a polymer-drug physical mixture.

A

drug mixed with polymer and incorporated into microspheres or nanoparticles

54
Q

Describe the structure of a polymer-drug conjugate

A

drug covalently bound to polymer

55
Q

Describe the structure of a polymer-drug complex.

A

drug assembled into micelles

56
Q

What are the kinds of polymeric carriers?

A

1) physical mixtures, 2) conjugates, 3) complexes

Drew 924 (16 decks)

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