Chemical Pentration Enhancer Lect 3 Part1

Question 1

What are the chemical pentration enhancer?

Answer 1

1_ surfactant
2_bile salts and derivatives
3_ fatty acids and derivatives
4_chelating agents
5_Sulfoxide
6_Monohydricalcohol
7_Miscellaneous
8_Polyols

Question 2

How the penetration enhancers act?

Answer 2

It acts by : 1_increasing the drug permeability through the skin by causing reversible damage to the stratum corneum.
2_increasing the pation coefficient of the drug to promot its release from vehicle to the skin.

Question 3

The water content of stratum corneum is ……%

Answer 3

15-20%

Question 4

What are the mode of action of water in chemical pentration enhancing ?

Answer 4

1_Free water acts as solvent and alter solubility of permeants and so its partioning
2_The cells take up water and swell, shuch swelling of cell would impact upon the lipid structure between the cells causing some disruptionto the bilayer packing.

Question 5

First chemically design molcule as a pentration enhancer

Answer 5

Azones

Question 6

Promote flux both hydrophilic and lipophilic permeant

Answer 6

Azones

Question 7

Highly lipophilic with log o/w =6.2

Answer 7

Azones

Question 8

Azones are effective at concentration ……% to ….%

Answer 8

0.1%-5%

Question 9

Azones are effective in high concentration (T or F)

Answer 9

F at low concentration (0.1% -5%)

Question 10

Azones are soluble and compatible most organic solvents (T or F)

Answer 10

T

Question 11

Enhances permiation of steroids, antiviral, antibiotics.

Answer 11

Azones

Question 12

What is the mode of action of azones?

Answer 12

1_(fluidization) interact with thr lipid domains of the stratum corneum.
2_partition into the lipid bilayer to distrupt their packing arrangement.

Question 13

Is used most commonly in patches

Answer 13

Ethanol

Question 14

What happened if we use alcohol at high concentration?

Answer 14

At high concentration causes dehydration of biological membrane and decrease the permeation.

Question 15

Alcohol used in concentration…..%

Answer 15

1-10%

Question 16

The most effective one in alcohols is the ethanol(T or F)

Answer 16

F the butanol

Question 17

The most used in alcohol is butanol(T or F)

Answer 17

F the ethanol

Question 18

If the alcohol is branshed therefore its activity will increase (T or F)

Answer 18

F will have lower activity.

Question 19

What is the mode of action of alcohols?

Answer 19

1(membran thining) because it is act as a solvent
2 volatile nature of ethanol help in modifying thermodynamic activity of drug .due to evaporation of ethanol drug concentration increases providing supersarurated state with greater driving force.
3_ solvent drug may carry permeant into the tissue. (بيشيل الدواء خلال الاغشية)

Question 20

Give reason. Volatile nature of ethanol helps in modifying thermodynamic activity od drug.

Answer 20

Due to evaporation of ethanol; drug concentration increases providing supersaturated state with greater driving force.

Question 21

Have potential to damage human skin

Answer 21

Surfactant

Question 22

Non ionic surfactants have minor (lower) effect but it is more safe
Anionic surfactant have pronounced effect(more effective) but it less safe
(T or F)

Answer 22

T

Question 23

What is the mode of action of surfactants?

Answer 23

Solubalise the lipophilic active ingredient and also have potential to solubalise lipids within the stratum corneum.

Question 24

Give reason the surfactant can not be able to do repultion(disrupt) the lipid bilayer packing arrangement as the fatty acids do.

Answer 24

Bacause the stracture of the surfactent are smaller than the stracture of the fatty acids

Question 25

Using in scaling condition such as psoriasis

Answer 25

Urea

Question 26

Usually urea used in combination with ....... for keratolysis

Answer 26

Salicylic acid

Question 27

What are the mode of action of urea?

Answer 27

1_Natural moisturizing factor binds with water to the skin, the increasing skin hydration increaseing drug permeation. 2_Has kyratolytic properties. 3_It produce significant stratume corneum hydration, produces hydrophilic diffusion channels.

Question 28

It is maily used (acts) as a vehicles to carry the drug

Answer 28

Phospholipids

Question 29

What is the MOA of phspholipids?

Answer 29

1_ Occlude the skin surface and increase tissue hydration. | 2_ phospholipids fuse with the stratum corneum lipids.

Question 30

Small amphiphilic molecules

Answer 30

DMSO

Question 31

Used in chemistry as aprotic solvent

Answer 31

DMSO

Question 32

What is the MOA of DMSO at low conc.?

Answer 32

1_induces membrane thining | 2_ increases the fluidity of the membran's hydrophopic core

Question 33

What is the MOA od DMSO at high conc.(60%)

Answer 33

1_DMSO induces transient water pores into the membrane. 2_ DMSO binds to water, promoting water defect in the membrane, which lead to reorientation in the membrane structure resulting in bore formation

Question 34

What is the conc. Of the optimum action of DMSO?

Answer 34

More than 60%

Question 35

What are the MOA of DMSO?

Answer 35

1_ change the keratin conformation from a(alpha) helical to B(beta) sheet. 2_ interacts with the head groups of some bilayer lipids to distrot to the packing geometry.

Question 36

Fatty acids are effective at high concentration (t or f)

Answer 36

F at low conc. (<10%)

Question 37

It is colourless liquid

Answer 37

Linoleic acid

Question 38

It is un saturated omega 6 fatty acid

Answer 38

Lenoleic acid

Question 39

Lenoleic acid presence in .......

Answer 39

Safflower oil and poppy oil in conc. 70 -78%

Question 40

What are the uses of lenoleic acid ?

Answer 40

Is used in making soap as emulsifier and quick drying oils

Question 41

Is used in making soap as emulsifier and quick drying oils

Answer 41

Lenoleic acid

Question 42

A monosaturated fatty acid

Answer 42

Oleic acid

Question 43

What are the MOA of Oleic acid?

Answer 43

Acts as a pentration enhancer by lipid fluidization and lipid phase separation

Question 44

Is a saturated fatty acid with an 18 carbon chain.

Answer 44

Stearic acid

Question 45

Write a ahort note about the lipid phase separation.

Answer 45

The pentration enhancer insert its self between the phospholipid molcules of the bilayer of cell surface membrane, forming a change in the orientation of the molcules, resulting in formation of spease between the phospholipids allowing the drug to pentrate easier and faster.