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Biosci 3110: BME > Drug Delivery > Flashcards

Drug Delivery Flashcards

1
Q

Maximum Effect

A

when the logarithm of concentration is plotted versus effect, the concentration above which no greater effect is achieved

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2
Q

EC50, UNITS

A

50% Effective Concentration (EC50): the concentration at which 50% of the maximum effect is achieved mg/L

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3
Q

Single compartment model, UNITS

A

XO->[X1]->K

X0 in mg, X1 in mg,K in (fraction) per hour

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4
Q

V=X/C, UNITS

A

Volume of distribution (L) is equal to dose (mg) divided by concentration (mg/L)

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5
Q

What types of bonds are degradable? Which are not?

A

Carbon-carbon bonds and amides are not, those with heteroatoms in their backbones are

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6
Q

Step Growth Polymerization

A

React functional groups to form chains, place heteroatoms in backbone
Functional groups can be hydrolyzed or degraded by an enzyme

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7
Q

Chain Polymerization or Free Radical Polymerization

A

Use radicals to initiation polymerization of double bonds

Produces polymers with carbon-carbon backbones, not degradable

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8
Q

Poly(2-hydroxypropyl methacrylamide) or Poly(HPMA)

A

the first polymer drugs were attached to

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9
Q

Poly(lactic-co-glycolic acid) or PLGA

A

the most famous polymer after PEG/PEO and has esters in its backbone that make it degrade into lactic acid and glycolic acid
Amount of each monomer type can change hydrolysis rates

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10
Q

Polyethylene Glycol (PEG) and Polyethylene Oxide (PEO)

A

Hydrophilic and biocompatible, but not biodegradable

Oxygens in backbone increase solubility by forming a water shell to shield from immune system

Easy to make and control size

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11
Q

Polymer-Drug Conjugates, components

A

Connect hydrophilic (sugar, hydroxyl, amides) polymer with drug using degradable linkage

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12
Q

Drug release rates for amides, peptides, phenyl esters, and alkyl esters

A

Peptides → Phenyl Esters → Alkyl Esters → Amides

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13
Q

Polymer-Drug Conjugates, advantages and disadvantages

A

Easier to make than liposomes
May be difficult to attach certain drugs or certain combinations of drugs, may produce side reactions, hard to make in large quantities

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14
Q

Hydrazone bonds

A

Ketone + Hydrazide → Hydrazone bond that is stable at pH 7.4 (blood) but unstable when in the acidic conditions of an endosome or lysosome

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15
Q

Polymerizable Prodrug Monomers, components

A

Polymerizable Group + Cleavable Linkage (hydrolyze or enzyme) + Therapeutic Agent all held together by hydrophilic comonomer spacers

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16
Q

Polymerizable Prodrug Monomers, advantages and creation

A

Avoid cross-reactivity with functional groups, easier to control amount of drug

Created in a single polymerization by free radical chain growth

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17
Q

Micelles, hydrophobic/hydrophillic

A

Cores are hydrophobic, accept hydrophobic drugs (no charge or polar groups)
Hydrophilic outside with positive charges

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18
Q

Micelles, bilayer, tails, possible components

A

Do not have a bilayer

Prepared from single tailed species (heads on outside)
Can be formed from surfacants or by polymers with a hydrophobic and hydrophilic side (these may also form polymersomes)

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19
Q

Liposomes, hydrophobic/hydrophillic

A

Cores are aqueous, accept hydrophilic drugs

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20
Q

Liposomes, bilayer, tails, possible components

A

Require twin tails

Contain bilayer (head-tail-head, philic-phobic-philic)

Lipids or polymers

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21
Q

Liposomes, possible additions

A

Can be coated with PEG to hide from immune system

Can be attached to targeting groups like antibodies, vitamins, folic acid, peptides

Can increase circulation time and change destination (ex: targeting, large size)

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22
Q

Liposomes, advantages and disadvantages

A

Hard to make, but still common

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23
Q

Nucleic Acids, examples, charges, carriers, active in

A

mRNA, siRNA

Only active in the cytoplasm, cannot enter the cell due to polarity

High negative charge (hard to attach to carrier), large and hydrophilic

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24
Q

NP or +/- ratio with nucleic acid biologic drug

A

DNA is -, Cation is +
NP ratio or +/- ratio

May not want to unstick, need to mess with ratio

Net positive is active/stable/toxic, net negative is as stable but less active/toxic

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25
Q

Nucleic acid biologic drug, circulation, additions

A

Adding PEG decreases both the toxicity and activity

Vulnerable to nucleases
Short circulation times

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26
Q

Nucleic acid biologic drug, carriers

A

Liposomes with cationic lipids (NH3+), polyelectrolyte complex

Cationic polymers (still toxic, lyse cell membranes and endosomes)

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27
Q

Protein biologic drugs

A

Antibodies, Enzymes
Can be involved in protein-protein interactions considered undruggable
A bit more stable and less charge than nucleic acids
Very effective and specific

28
Q

Viral and special carriers of biologic drugs

A

Viruses are non-specific and may cause cancer
Carriers should sense pH change
Viruses can change from a stable conformation to one that lyses the endosomes and enters the cytoplasm

29
Q

Three challenges of drug delivery

A

solubility, stability, physical barriers

30
Q

Low Molecular Weight Drugs

A

Include antibiotics, worried about getting into solution and first pass, usually diffuse well if not too polar

31
Q

Protein Therapeutics

A

Can modify protein-protein interactions, great specificity, cannot diffuse past membranes, without vehicle will go through endocytosis (bad), proteases (not as big as a deal)

32
Q

Nucleic Acid Therapeutics

A

Vulnerable to nucleases, viral carriers are nonspecific

33
Q

What groups are polar/hydrophilic?

A

Include neutral groups such as hydroxyls and amides as well as charged particles

34
Q

What groups are nonpolar/hydrophobic?

A

c-c bonds

35
Q

What are lipids/surfactants?

A

Organic molecules that are amphiphilic containing both hydrophobic tails and hydrophilic heads

36
Q

Different head possibilities for lipids/surfacants

A

Cationic polar heads are toxic, but can deliver nucleic acids
Anionic polar heads are vulnerable to kupffer cells in liver
→ Want neutral hydrophilic heads

37
Q

What are the types of neutral hydrophilic heads?

A

Include zwitterions (+ attached to -, include cell membranes), PEG chains, hydroxyls, amides

38
Q

Structure of phosphatidylcholine

A

twin tails with single double bond, esters, PO4, NC3+

39
Q

Absorption

A

the process of a substance entering blood circulation

Very important for oral drugs to get through liver first pass

40
Q

Distribution

A

dispersion throughout the fluids and tissues of body

41
Q

Metabolism

A

recognition by organism and transformation into daughter metabolites, usually by adding polar groups
May make the drug more toxic

42
Q

Excretion

A

the removal of substances from the body

43
Q

Pharmacokinetics

A

the study of how the organism affects the drug

or

the study of the time course of drug absorption, distribution, metabolism, and excretion

44
Q

Pharmacodynamics

A

the study of how the drug affects the organism (factors include density of receptors, second messengers, regulatory factors)

relates drug concentration to drug effect

45
Q

First Pass Effect

A

the phenomenon of drug metabolism whereby the concentration of a drug is greatly reduced (by the liver) before it reaches the systemic circulation

46
Q

Clinical Pharmacokinetics

A

the application of pharmacokinetic principles to safely and effectively administer drugs to patients by developing correlations between drug concentration and pharmacologic response

47
Q

Clinical Pharmacokinetics, goals

A

Want to increase efficacy and decrease toxicity

48
Q

Kinetic Homogeneity

A

the description of the predictable relationship between plasma drug concentrations and concentrations at the receptor site

49
Q

Plasma

A

the fluid portion without the formed elements

50
Q

Serum

A

plasma without fibrinogen

51
Q

Fibrinogen

A

soluble protein that produces fibrin by the enzyme thrombin

52
Q

Fibrin

A

insoluble protein formed from fibrinogen during blood clotting that forms a fibrous mesh

53
Q

Distribution of water: % in body

A

60

54
Q

Distribution of water: Intracellular v Extracellular

A

58% is intracellular and 42% is extracellular

55
Q

Distribution of water: Extracellular components

A

Of the extracellular fluid, 16% is plasma and 84% is interstitial

56
Q

One-compartment model, describes and assumes

A

All body tissues are fluids are part of the compartment

After a drug is administered, it distributes instantaneously to all body areas

57
Q

Intravenous bolus dosing

A

administering a dose of drug over a very short time period

58
Q

First-Order, Ln (concentration) v time

A

line

59
Q

V = XC, meaning of V

A

V is volume to account for all drug if concentrations in tissues are the same as the plasma drug concentrations

Volumes below extracellular fluid is mostly in fluid, volumes higher is mostly in tissues (sources of error are from diff con in tissues/plasma)

60
Q

Therapeutic Drug Monitoring

A

the use of assays to determine the plasma drug concentration and application of these data to develop safe and effective drug regimens

61
Q

Therapeutic Drug Monitoring, uses

A

Used when there is a good correlation between response and plasma concentration, wide intersubject variation, and narrow therapeutic index (and effects that cannot be assessed by other means)

Plots probability (%) by drug concentration (mg/L) for response and toxicity

62
Q

Clearance, meaning

A

Clearance includes renal (kidneys), liver, biliary (bile duct), and other routes

Volume/time

a measure of the removal of drug from a volume of plasma in a given unit of time (volume that would be drug-free if concentration were held constant)

63
Q

Clearance, blood flow, excretion ratio

A

Equal to excretion ratio by blood flow → Cl = QE
Q is blood flow in mL/min
E is excretion ratio, unitless
Cl is clearance in volume/time

Model independent, summation of all organs (liver/kidneys)

64
Q

Excretion ratio

A

E is excretion ratio (concentration in-concentration out)/(concentration in), unitless

65
Q

Fraction removed constant, amount different ->

Fraction removed different, amount constant ->

A

First-order, Ln concentration v time linear

Zero-order, concentration v time linear

Biosci 3110: BME (6 decks)

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