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Clare's lectures semester 2 > Drug solubilisation 2 > Flashcards

Drug solubilisation 2 Flashcards

1
Q

What are cyclodextrins?

A
  • They are cyclic oligasachharides that posses a rigid conical structure
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2
Q

Cyclodextrins include a hydrophilic exterior and a hydrophobic inner core. TRUE OR FLASE?

A

TRUE

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3
Q

The hydroxyl groups on the exterior of the cyclodextrin structure forms H-bond with water and as result forms inclusion complexes. TRUE OR FALSE?

A

TRUE

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4
Q

Hydrophobi drugs can be inserted in the hydrophobic inner core of the cyclodextrin to form hydrophobic-hydrophobic interactions. TRUE OR FALSE?

A

TRUE

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5
Q

What is the mechanism of encapsulation of cyclodextrins?

A
  • Inclusion complex is formed when water is removed and replaced by the lipophilic guest i.e hydrophobic drug
  • The central cavity plas host to hydrophobic drug forming non-covalent interactions with hydrophobic drug
  • This is an aletrnative ot micellear solubilisation
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6
Q

You can change the size of the core to accommodate the drug. TRUE OR FALSE?

A

TRUE

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7
Q

The solubility of the hydrophobic drug is enhanced by entrapment of inside the core. TRUE OR FALSE?

A

TRUE

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8
Q

what have cyclodextrins been prove to do?

A
  • Improve solubility
  • Enhave bioavailability
  • Protect drug while in vivo
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9
Q

The solubility of cyclodextrins is drug dependent on size and steric structure. TRUE OR FLASE?

A

TRUE

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10
Q

The drug must fit into the cyclodextrin core before ti becomes solubilised. TRUE OR FLASE?

A

TRUE

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11
Q

why are drug specific delivery systems problematic?

A
  • cost implications

- not in dynamic equilibrium

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12
Q

what are calixerenes?

A
  • They are a family of oligomers whihc have a 3 dimentional structures
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13
Q

when are calixerenes commonly used?

A
  • Commonly used as building blocks in supramolecular systems
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14
Q

Calixarenes form 3D cupe like structures with well defined upper rim a upper and lower rims containing a central cavity in both the solid state and in soluiton. TRUE OR FALSE?

A

TRUE

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15
Q

Claixarenes posses metal biding site and hydrophobic core for host guest interactions with organic molecules. TRUE OR FALSE?

A

TRUE

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16
Q

How do calixarenes enhance solubitlity of hydrophobic drugs?

A

Via hydrophobic interactions

17
Q

What affects the variation of calixarenes?

A
  • different solvents
  • Tempearture
  • functional groups
18
Q

Carixarenes are not rigid structures. TRUE OR FALSE?

A

TRUE

19
Q

what advantages do calixarene have over cyclodextrins?

A
  • Can be chemically modfied easily with low toxic chemical reactions
  • It allows more targeted delivery as functional groups can be attached to the upper or lower rim
  • they have low production costs and low toxicity
20
Q

Just with cyclodextrins, drugs have to be sterically stable (physically stable) in order to bind into the steric pocket of the calixarene. TRUE OR FLASE?

A

TRUE

21
Q

Calixarenes do not form generic drug solubilisers. TRUE OR FALSE?

A

TRUE

22
Q

Propofol has low physiochemical properties which results in low aqueous solubility and hence hinders its use. TRUE OR FALSE?

A

TRUE

23
Q

what is nanodrug formation?

A
  • When large insoluble drugs are milled down to nano sized particles
24
Q

The decrease in particle size leads to an increase in SA to volume ratio. TRUE OR FALSE?

A

TRUE

25
Q

what are the advantages of nanodrug formation?

A
  • Solubility will be enhanced leading to use via I.V
  • Can administer lower doses which will have similar effects to large doses
  • Fewer side effects and more cost effectiveness
26
Q

what are the advantages of nanodrug formation for oral drug delivery?

A
  • For oral drugs, increased SA leads to increased dissolution rate and hence bioavailability which means that drug will reach its target (GI tract)
27
Q

what are the advantages of nanodrug formation for pulmonary drug delivery?

A
  • the drug can reach deep down lung tissue

- Once in target site it can easily cross the mucus memebranes

28
Q

what are the disadvantages of nanonization (nanodrug formation)?

A
  • Does not apply to all drug molecules
  • stability issues
  • Does not rival use of excipients
29
Q

what are polymers?

A
  • They are long chain molecules made up of repeating units with high molecular weights
30
Q

Polymers are easily tailored for functionality using different chemistries. TRUE OR FALSE?

A

TRUE

31
Q

What does a polymer drug conjugate consist of?

A
  • Biocompatible polymer
  • Solubiliser
  • Drug
  • Targeting moiety
32
Q

what does the water soluble backbone do in a polymer drug-conjugate?

A
  • Increases aqueous solubility
33
Q

what does drug conjugate do in a polymer drug conjugate?

A
  • It allows for controlled delivery
34
Q

what does taregting moeity do in polymer drug conjugate do?

A
  • Enhances binding and cellular uptake
35
Q

high molecular weigth increases accummulation via enhanced permeability and retention effect. TRUE OR FLASE?

A

TRUE

36
Q

what are the advantages of polymer drug conjugates?

A
  • Can increase circulation time
  • Can increase drug penetration
  • Can protect the drug
  • Also has benefits that other nano technologies have
37
Q

what are the disadvantages of polymer drug conjugates?

A
  • Need to use complex chemistry for linkers

- drug can become permanetly conjugated

38
Q

what are the three types of nanottechnology used to solubilise drugs?

A
  • Cyclodextrins
  • Calixeranes
  • Polymer drug conjugates
  • Nanonization

Clare's lectures semester 2 (10 decks)

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