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SCREENING MODELS OF ANTI-
INFLAMMATORY DRUGS
Presented by Mr.Gadage Ashish R.
M.Pharm sem 1
department of pharmacology
Under The Guidance of
Dr Dighe S.B
Head Of Department PhD In
Pharmacology
 Content
 INTRODUCTION
 TYPES OF INFLAMMATION
 ANTI-INFLAMMATORY DRUGS
 MOA OF ANTI-INFLAMMATORY DRUGS
 FIG .PLETHYSMOMETERys
 PRECLINICAL SCREENING METHODS FOR ANTI-INFLAMMATORY
AGENTS
A) In vitro models
B) In vivo models
 INTRODUCTION
 Inflammation is a universal host defensive process involving a
complex network of cell-cell, cell-mediator and tissue interaction
 The factors that can cause inflammation are bacteria, viruses,
fungi, parasites, antigen-antibodyreaction, mechanical trauma,
organic and inorganic poisons and foreign bodies.
 Inflammation is response to variety of harmful stimuli physical,
chemical, traumatic antigen challenge, infectious agents and
ionizing radiations.
FACTORS
 Xogenous:
Physical, chemical, mechanical, nutritional and biological etc
 Endogenous:
immunological reactions, neurological and genetical disorders
TYPES OF INFLAMMATION
 Acute inflammation is of relatively short duration (hours to
days) and is rapid onset . Characterized by exudation of fluid and
plasma proteins Activation of platelet and neutrophils
 Chronic inflammation is of longer duration (days to years)
Characterized by mononuclear infiltration, vascular proliferation
and tissue necrosi
 ANTI-INFLAMMATORY DRUGS
 Anti-inflammatory drugs are medicines that are widely used to
relieve pain, reduce inflammation.
 They're often used to relieve symptoms of: headaches. painful
periods. sprains and strains.
 E.g Ibuprofen,Aspirin
Classification of Antiiflammatory Drugs
MOA OF ANTI-INFLAMMATORY DRUGS
PRECLINICAL SCREENING METHODS FOR
ANTIINFLAMMATORY
A) IN VITRO MODELS
1) Cell Culture Models
2 )Enzyme Inhibition Assays
B) IN VIVO MODELS
1) Carrageen induced rat paw Oedema model.
2) Formalin induced oedema in rat paw .
3) UV-B induced erythema in guinea pigs.
 IN VITRO ASSAYS
1)Cell Culture Models:
Using cell lines or primary cells to simulate inflammation
and test the anti- inflammatory effects of compounds.
2)Enzyme Inhibition Assays:
Assessing the ability of compounds to inhibit specific
enzymes involved in the inflammatory process, such as
cyclooxygenase (COX) or lipoxygenase.
The inflammatory reaction is readily produced in rats in
the form of paw edema with the help of irritants.
• The substances such as
✓ Carrageenan
✔ Formalin
• when injected in the dorsum of foot of the rat, they
produce acute paw oedema within a few min of injection.
1) Carrageen induced rat paw Oedema model
Requirements:
• Animal: Rats (150-200 g)
• Drug/ Chemical: Carrageenan and Indomethacine
•Drug preparation:
a) Carrageenans (prepares 1% w/v solution and inject 0.1 ml
underneath the plantar region)
b) Indomethacin (20 mg/Kg, s.c.) prepare stock solution 4 mg/ml.
Inject in proportion of 0.5ml/100 g of body wt of the rat.
c) Normal saline injected in proportion of 0.5ml/100 g of body wt of
the rat.
• Equipment and Apparatus: Plethysmograph or Digital
Plethysmometer, , syringes, oral feeding tube, e
A plethysmometer measures slight changes in
oedema (fluid retention) and volume to
calculate the rodents' inflammatory response to
anti-inflammatory agents.
A highly useful tool in the measurement of
small volume changes
This test is typically used to
✔To Follow the evolution of the
inflammatory response experimentally
induced in rodents
✔To screen potential anti-inflammatory or
anti-oedema properties pharmacological
substances
FIG .PLETHYSMOMETER
Procedure:
1. Weigh the animals and number them
2. Make the mark on both the hind paw (right and left) just beyond
the tibio-tarsal junction so that one can ensure that every time the
paw is dipped in the mercury column up to the fixed mark
3. Note the initial paw volume (both right and left) of each rat by
mercury displacement method.
4 Divide the animals in 02 groups (control and Indomethacine-
treated group) each comprising of at least 06 rats.
5. Control group inject saline and to test group inject Indomethacin
by subcutaneous (s.c). route
6. After 30 min, inject 0.1 ml 1% (w/v) carrageenan in plantar
region of left paw of control group as well as Indomethacine
treated group.
7. Right paw of each rat will serve as reference non-inflamed paw
for comparison.
8 Note the paw volume of both the legs of control treated with
normal saline and Indomethacine-treated rats at 15, 30, 60 and 120
min of carrageenan challenge
9.Calculate the % difference in right and left paw volumes of each
rat of control and Indomethacine- treated group.
10. Compare the mean % change in paw volume in control and
drug treated rats Express the % oedema inhibited by anti-
inflammatory drug- Indomethacin
OBSERVATION TABLE
INFERENCE
Indomethacin showed anti-inflammatory activity against
carrageenan-induced paw oedema
Vehical Treated Drug Treated
0.75 0.51
0.73 0.49
0.78 0.53
0.74 0.55
0,74 0.58
0.77 0.56
0.75 0.53 Average
REFERENCE:
1. Screening of methods in pharmacolgy volume 1,by Robert A. Turner.
2. Drug discovery and evaluation :pharmacological assays 2nd edition,By
Gerhard vogel.
3. Powerpoint presentation acknowledgement :Mr Jaineel Dharod. LMCP
4. Review on “Emerging trends and modification of In Vivo and In Vitro
Screening techquies of diuretic activity” by Kiran Kulkarni,Manish
Kondawar.JCRT
Thank you

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Navigating the Landscape: Innovative Screening Models for Anti-Inflammatory Drug Discovery

  • 1. SCREENING MODELS OF ANTI- INFLAMMATORY DRUGS Presented by Mr.Gadage Ashish R. M.Pharm sem 1 department of pharmacology Under The Guidance of Dr Dighe S.B Head Of Department PhD In Pharmacology
  • 2.  Content  INTRODUCTION  TYPES OF INFLAMMATION  ANTI-INFLAMMATORY DRUGS  MOA OF ANTI-INFLAMMATORY DRUGS  FIG .PLETHYSMOMETERys  PRECLINICAL SCREENING METHODS FOR ANTI-INFLAMMATORY AGENTS A) In vitro models B) In vivo models
  • 3.  INTRODUCTION  Inflammation is a universal host defensive process involving a complex network of cell-cell, cell-mediator and tissue interaction  The factors that can cause inflammation are bacteria, viruses, fungi, parasites, antigen-antibodyreaction, mechanical trauma, organic and inorganic poisons and foreign bodies.  Inflammation is response to variety of harmful stimuli physical, chemical, traumatic antigen challenge, infectious agents and ionizing radiations.
  • 4. FACTORS  Xogenous: Physical, chemical, mechanical, nutritional and biological etc  Endogenous: immunological reactions, neurological and genetical disorders
  • 5. TYPES OF INFLAMMATION  Acute inflammation is of relatively short duration (hours to days) and is rapid onset . Characterized by exudation of fluid and plasma proteins Activation of platelet and neutrophils  Chronic inflammation is of longer duration (days to years) Characterized by mononuclear infiltration, vascular proliferation and tissue necrosi
  • 6.  ANTI-INFLAMMATORY DRUGS  Anti-inflammatory drugs are medicines that are widely used to relieve pain, reduce inflammation.  They're often used to relieve symptoms of: headaches. painful periods. sprains and strains.  E.g Ibuprofen,Aspirin
  • 9. PRECLINICAL SCREENING METHODS FOR ANTIINFLAMMATORY A) IN VITRO MODELS 1) Cell Culture Models 2 )Enzyme Inhibition Assays B) IN VIVO MODELS 1) Carrageen induced rat paw Oedema model. 2) Formalin induced oedema in rat paw . 3) UV-B induced erythema in guinea pigs.
  • 10.  IN VITRO ASSAYS 1)Cell Culture Models: Using cell lines or primary cells to simulate inflammation and test the anti- inflammatory effects of compounds. 2)Enzyme Inhibition Assays: Assessing the ability of compounds to inhibit specific enzymes involved in the inflammatory process, such as cyclooxygenase (COX) or lipoxygenase.
  • 11. The inflammatory reaction is readily produced in rats in the form of paw edema with the help of irritants. • The substances such as ✓ Carrageenan ✔ Formalin • when injected in the dorsum of foot of the rat, they produce acute paw oedema within a few min of injection.
  • 12. 1) Carrageen induced rat paw Oedema model Requirements: • Animal: Rats (150-200 g) • Drug/ Chemical: Carrageenan and Indomethacine •Drug preparation: a) Carrageenans (prepares 1% w/v solution and inject 0.1 ml underneath the plantar region) b) Indomethacin (20 mg/Kg, s.c.) prepare stock solution 4 mg/ml. Inject in proportion of 0.5ml/100 g of body wt of the rat. c) Normal saline injected in proportion of 0.5ml/100 g of body wt of the rat. • Equipment and Apparatus: Plethysmograph or Digital Plethysmometer, , syringes, oral feeding tube, e
  • 13. A plethysmometer measures slight changes in oedema (fluid retention) and volume to calculate the rodents' inflammatory response to anti-inflammatory agents. A highly useful tool in the measurement of small volume changes This test is typically used to ✔To Follow the evolution of the inflammatory response experimentally induced in rodents ✔To screen potential anti-inflammatory or anti-oedema properties pharmacological substances FIG .PLETHYSMOMETER
  • 14. Procedure: 1. Weigh the animals and number them 2. Make the mark on both the hind paw (right and left) just beyond the tibio-tarsal junction so that one can ensure that every time the paw is dipped in the mercury column up to the fixed mark 3. Note the initial paw volume (both right and left) of each rat by mercury displacement method. 4 Divide the animals in 02 groups (control and Indomethacine- treated group) each comprising of at least 06 rats. 5. Control group inject saline and to test group inject Indomethacin by subcutaneous (s.c). route
  • 15. 6. After 30 min, inject 0.1 ml 1% (w/v) carrageenan in plantar region of left paw of control group as well as Indomethacine treated group. 7. Right paw of each rat will serve as reference non-inflamed paw for comparison. 8 Note the paw volume of both the legs of control treated with normal saline and Indomethacine-treated rats at 15, 30, 60 and 120 min of carrageenan challenge 9.Calculate the % difference in right and left paw volumes of each rat of control and Indomethacine- treated group. 10. Compare the mean % change in paw volume in control and drug treated rats Express the % oedema inhibited by anti- inflammatory drug- Indomethacin
  • 16. OBSERVATION TABLE INFERENCE Indomethacin showed anti-inflammatory activity against carrageenan-induced paw oedema Vehical Treated Drug Treated 0.75 0.51 0.73 0.49 0.78 0.53 0.74 0.55 0,74 0.58 0.77 0.56 0.75 0.53 Average
  • 17. REFERENCE: 1. Screening of methods in pharmacolgy volume 1,by Robert A. Turner. 2. Drug discovery and evaluation :pharmacological assays 2nd edition,By Gerhard vogel. 3. Powerpoint presentation acknowledgement :Mr Jaineel Dharod. LMCP 4. Review on “Emerging trends and modification of In Vivo and In Vitro Screening techquies of diuretic activity” by Kiran Kulkarni,Manish Kondawar.JCRT