Drug solubilisation 2

Question 1

What are cyclodextrins?

Answer 1

• They are cyclic oligasachharides that posses a rigid conical structure

Question 2

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

Answer 2

TRUE

Question 3

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

Answer 3

TRUE

Question 4

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

Answer 4

TRUE

Question 5

What is the mechanism of encapsulation of cyclodextrins?

Answer 5

• 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

Question 6

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

Answer 6

TRUE

Question 7

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

Answer 7

TRUE

Question 8

what have cyclodextrins been prove to do?

Answer 8

• Improve solubility
• Enhave bioavailability
• Protect drug while in vivo

Question 9

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

Answer 9

TRUE

Question 10

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

Answer 10

TRUE

Question 11

why are drug specific delivery systems problematic?

Answer 11

• cost implications

- not in dynamic equilibrium

Question 12

what are calixerenes?

Answer 12

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

Question 13

when are calixerenes commonly used?

Answer 13

• Commonly used as building blocks in supramolecular systems

Question 14

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?

Answer 14

TRUE

Question 15

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

Answer 15

TRUE

Question 16

How do calixarenes enhance solubitlity of hydrophobic drugs?

Answer 16

Via hydrophobic interactions

Question 17

What affects the variation of calixarenes?

Answer 17

• different solvents
• Tempearture
• functional groups

Question 18

Carixarenes are not rigid structures. TRUE OR FALSE?

Answer 18

TRUE

Question 19

what advantages do calixarene have over cyclodextrins?

Answer 19

• 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

Question 20

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?

Answer 20

TRUE

Question 21

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

Answer 21

TRUE

Question 22

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

Answer 22

TRUE

Question 23

what is nanodrug formation?

Answer 23

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

Question 24

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

Answer 24

TRUE

Question 25

what are the advantages of nanodrug formation?

Answer 25

- 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

Question 26

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

Answer 26

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

Question 27

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

Answer 27

- the drug can reach deep down lung tissue | - Once in target site it can easily cross the mucus memebranes

Question 28

what are the disadvantages of nanonization (nanodrug formation)?

Answer 28

- Does not apply to all drug molecules - stability issues - Does not rival use of excipients

Question 29

what are polymers?

Answer 29

- They are long chain molecules made up of repeating units with high molecular weights

Question 30

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

Answer 30

TRUE

Question 31

What does a polymer drug conjugate consist of?

Answer 31

- Biocompatible polymer - Solubiliser - Drug - Targeting moiety

Question 32

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

Answer 32

- Increases aqueous solubility

Question 33

what does drug conjugate do in a polymer drug conjugate?

Answer 33

- It allows for controlled delivery

Question 34

what does taregting moeity do in polymer drug conjugate do?

Answer 34

- Enhances binding and cellular uptake

Question 35

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

Answer 35

TRUE

Question 36

what are the advantages of polymer drug conjugates?

Answer 36

- Can increase circulation time - Can increase drug penetration - Can protect the drug - Also has benefits that other nano technologies have

Question 37

what are the disadvantages of polymer drug conjugates?

Answer 37

- Need to use complex chemistry for linkers | - drug can become permanetly conjugated

Question 38

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

Answer 38

- Cyclodextrins - Calixeranes - Polymer drug conjugates - Nanonization