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Progressive Education Societies
PES. Modern College Of Pharmacy
Sector No.21Yamunagar, Nigdi,Pune-411044
“Polysaccharide based Drug Delivery System For Periodontitis”
Presented By-
Ms.Vasundhara Pramod Patil
Final Year B. Pharm
( Div -B)
4071
Guided By-
Dr. Sangita. A. Kale
(Assistant Professor)
Department Of
Pharmaceutics
Contents
 Introduction
 Need Of Work
 Aim And Objective
 Plan Of Work
 Drug and Excipient Profile
 Experimental Work
 Result And Discussion
References
INTRODUCTION
 Periodontitis is a chronic inflammatory disease of Periodontium.
 It is the main cause of tooth loss and is considered one of the biggest threats to the
oral health.
 Periodontal diseases are mainly the result of Infections and inflammation of the
gums and bone that surround and support the teeth.
 In its early stage, it is called as Gingivitis, in which the gums can become swollen
and appears red and they may bleed.
 In its more serious form, it is called as Periodontitis, in which the gums can pull
away from the tooth and the teeth may loosen or even fall out.
 Periodontal disease is mostly seen in adults.
 Periodontal disease and tooth decay are the two biggest threats to dental health.
Comparison of Normal and Periodontal tooth
Fig no.1 Normal and Periodontal tooth
 Stages Of Periodontitis
Based on the severity and complexity of management
Stage I: Initial periodontitis
Stage II: Moderate periodontitis
Stage III: Severe periodontitis
Stage IV: Severe periodontitis with the potential loss of dentition
Based on the extent and distribution
a. Localized
b. Generalized
c. Molar-incisor distribution
Based On Grades
GradeA:Slow rate of progression
Grade B: Moderate rate of progression
Grade C: Rapid rate of progression
• Diagrammatic Representation of Stages of Periodontitis
Fig no.2 Stages of Periodontitis
 Symptoms and Causes of Periodontitis
SYMPTOMS
 Swollen and puffy gums.
 Sensitive teeth.
 Bright red, Dusky red, Purplish gums.
 Tender gums that bleed easily.
 New spaces form between teeth.
 Formation of Puss between teeth and gums.
 Painful chewing.
CAUSES
Bacteria's in the oral cavity are the main cause
of Periodontitis.
 Heredity.
 Poor oral health.
 Taking medication that causes dry mouth.
 Braces which do not fit properly.
In Situ Gel For Periodontitis
In situ gels are the solutions or suspensions that undergo gelation after reaching the particular
site due to contact with body fluids or physicochemical changes (i.e., pH, temperature, ionic
concentration, UV radiation, presence of specific molecules or ions, external triggers, etc).
The major importance of in-situ gel is administration of accurate & reproducible quantities
compared to already formed gel.
IMPORTANCE OF IN SITU GELLING SYSTEM
•In situ gel helps for the controlled and sustained release of the drug by its special Sol- Gel
transition.
•It helps to reduce frequency of drug administration.
•Low drug dose required and there will be no drug accumulation and no side effects of drug.
•More bioavailability of the drug.
•Increased residence time of the drug due to gel formation.
•The in situ gelling decreases wastage of the drug.
Fig no. 3 Pathophysiology of Periodontitis and working of In-situ gel
Advantages and Disadvantages Of In situ Gelling System
ADVANTAGES
To reduce medication waste.
For administrative convenience.
It can be administered to elderly and
unconscious patients.
It aids in the prolonged or longer release
of drugs.
It promotes more patient cooperation and
comfort.
Promotes biocompatibility and
biodegradation by employing natural
polymers.
DISADVANTAGES
Only small doses can be administered.
Due to chemical degradation, there is a
chance of instability.
It may results in premature dissolution
due to low mechanical strength.
Need and Rationale of work
Curcumin
• Curcumin has Anti-inflammatory and anti-bacterial activities which are used
to treat Periodontal symptoms.
TSP
• TSP shows Dual action Muco-adhesive action due to which the gel
stays adhere to the site of action.
• It is an Excellent biodegradable, bio-compatible, and non-irritant Bio-
polymer.
• TSP also act as a Gelling agent.
Carbapol
• It is pH dependent polymer, which stays in solution form at acidic pH but forms a low
viscosity gel at alkaline pH.
• It is used as Thickening and Gelling agent which are important properties for Gel
formation.
In-situ gel
• The in-situ gelling decreases wastage of the drug.
• It provides More bioavailability of the drug.
• In-situ gel shows sustained and controlled drug delivery.
Aim And Objective
Aim : To develop and evaluate In-situ gel for Periodontitis by using Tamarind seed
polysaccharide (TSP)
Objective:- To Evaluate In-situ gel containing TSP for Periodontitis.
Plan Of Work
 Literature review
 Drug and excipients profile
 Preliminary and Pre formulation study
a) Characterisation of drug
b) FTIR Spectroscopy
 Preparation of In situ gel
a) Preliminary development
b) Preparation of Gel by using Polysaccharide
 Evaluation of In situ gel
a) Rheological Study
b) In-vitro drug release
c) Antibacterial activity
Literature survey
Sr
no.
Name of the article Authors Result
1 Development and
Evaluation of in Situ
Gelling System for
Treatment of
Periodontitis
Khushbu S. Patel
Dr. K.R.Vadalia
Dr. J. K. Patel
Tinidazole is well reported for the treatment of periodontal disease, they have better
penetration into periodontal tissues, minimal bacterial resistance as compared to
many of the other drugs used for the treatment.The excipients used in this present
work are Gellan gum and Poloxamer 407 as gelling agent which form immediate
gel. The Methyl paraben and Propyl paraben is used as preservativesThe studies
revealed that drug and polymers were compatible.
2 Xyloglucan Based In Situ
Gel of Lidocaine HCl for
the Treatment of
Periodontosis
Ashlesha P.Pandit
Vinit S.Kulkarni
Lidocaine hydrochloride loaded periodontal temperature-sensitive in situ gel was
successfully developed by cold method using xyloglucan based mucoadhesive
polymer TSP for insertion into periodontal pocket to have painless treatment... Use
of natural, less costly, biodegradable, and easily available mucoadhesive TSP
polymer as well as avoidance of needle insertions during scaling and root planning
of periodontosis helped achieve patient compliance by ultimately reducing the cost
of the treatment.
3 Clinical and Anti-
Inflammatory Effect of
Curcumin Oral Gel as
Adjuncts in
Treatment of Periodontal
Pocket
Hayder Thabit
Farhood, Basma
Ghafori Ali
The periodontal disease is among the most popular medical situations which might
affect humans. Periodontal pocket that is known as a pathologically extended
gingival sulcus which is one of most essential clinical characteristics of the
periodontal disease.. An adjunct to scaling and root planning has been introducing
as curcumin. Curcumin possess antioxidant, anti-inflammatory, and anti-microbial
properties.
Sr no. Name of the article Authors Result
4. In situ gel drug
delivery system for
periodontitis: an
insight review
Ravishankar
Yadav,
Indu lata kunwar,
,vishal gaur
Novel in situ forming gel is introduced at the site that shows a promising
potential to overcome one of the main practical obstacles associated with
the treatment of local periodontitis: partial adhesion to the surrounding
tissue, causing in the accidental expulsion of at least parts of the
implants from patient’s pockets. This results in a large residence time of
the system at the site of action and the uncertainty of the final exposure
to the drug .From the reviewed literature, it is concluded that
experimental evidence suggests that the in situ gel-forming systems can
be useful in treating several common diseases of the oral cavity.
5. Evaluation and
Characterization of
Tamarind Gum
Polysaccharide:
The Biopolymer
Sonali sundaram,
Shivkanya fuloria,
Rishabha malavia
Tamarindus indica was isolated using distilled water as a solvent system
and ethyl alcohol as precipitating agent. Phytochemical investigation
showed the presence of carbohydrates while reducing sugar, glucose,
tannins, proteins, and polysaccharides were absent.
Drug And Excipient Profile
Curcumin
Curcumin is the Popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae)
and obtained from rhizomes of Curcuma longa L.
The Main curcuminoids are Curcumin (94%) ,de-methoxycurcumin (6%) and bis-demethoxycurcumin
(0.3%)
The curcuminoids are Polyphenols and are responsible for the Yellow color of turmeric.
 Properties of Curcumin
Molecular Formula- C21H20O6
Molecular Weight- 368.4 kDa
IUPAC Name - (1E,6E)-1,7-bis (4-hydroxy- 3-methoxyphenyl) -1,6- heptadiene-3,5-dione
Half life- 6-7 hrs
pKa -7.8 (basic)
Drug Category: Anti-inflammatory, Anticancer, Antimicrobial.
Fig no.4 Structure of Curcumin
Tamarind Seed Polysaccharide(TSP)
TSP is a plant polysaccharide derived from the Tamarindus indica Linn seed endosperm
belongs Fabaceae family.
It is a water-soluble, non-ionic, branched polysaccharide with hydrophilic, gel-forming, and
muco-adhesive characteristics.
TSP is also Biodegradable, Biocompatible, non-carcinogenic, and irritant-free.
It is used in the pharmaceutical, cosmetic, and food industries as a promising biopolymer.
 Properties of TSP
Molecular formula- (C6H10O3)n
Molecular weight – 1735 kDa
Description- White crystalline Powder
Category - Muco-adhesive
Application in pharmaceutical - Stabilizer, thickening agent, gelling agent.
Fig no.5 TSP
CARBOPOL-934
Carbopol-934 is a well-known pH dependent polymer, which stays in solution form at
acidic pH but forms a low viscosity gel at alkaline pH.
General Properties of Carbopol
Synonym: Acrylic acid polymer
IUPAC Name: prop-2-enoic acid
Molecular formula: (C3H4O2)n
Category: Gelling agent
Description: White amorphous powder
Solubility: soluble in water
 Application in pharmaceutical:
Stabilizer, Thickening agent, Gelling agent
Fig no. 6 Structure of Carbopol
 Experimental Work
Synthesis of Tamarind Seed Polysaccharide (TSP)
Formulation Of In-situ Gel
Evaluation Of In-situ Gel
 Isolation of Tamarind Seed Polysaccharide (TSP)
Tamarind seed polysaccharide (TSP) is Polysaccharide extracted from the kernel of seeds of
Tamarindus indica Lin, Family Leguminosae.
Synthesis of TSP-
250 gms of Tamarind seeds
were crushed and powdered
A viscous solution was
obtained when powder is
boiled with 500 ml of
distilled water with
continouse stirring
filter the solution and dry
the supernatant. the dried
supernatent is then referred
to as Tamarind kernel
powder.
20 gm of tamarind kernel
powder and 200 ml
distilled water are mixed
to form slurry. 800 ml of
distilled water was added
with the slurry.
At 40 °C, the precipitate
the obtained was dried and
dried film was ground into
a fine powder to obtain
TSP.
Supernatent is added to
100% ethanol in a
volume that was double
its original size.
The solution was boiled
for 20 minutes With
constant stirring, the
supernatant was separated
Trial Batches Of In-situ Gel –
The various trial batches were formulated and compared to each other to determine the final
formula for the batch in which the Sol-Gel system is observed, when the solution is sprayed
in the Phosphate Buffer of suitable pH (pH of oral cavity).
Trial Batch
No.
Ingredients F1 F2 F3 F4 F5
1 Curcumin(gm) 0.1 0.1 0.1 0.1 0.1
2 TSP(gm) 0.1 0.1 0.2 0.3 0.1
3 Ethanol 1 1 1 1 1
4 Carbopol-934
(gm)
0.1 0.2 0.1 0.1 0.3
5 Water q.s q.s q.s q.s q.s
Table no.1 Trial batches of the formulation
 Optimized Batch of formulation –
The Optimized batch of the formulation is representsAccurate quantities of the ingredients
which are used to form the Ideal formulation.
The optimized batch is selected from various trial batched according to their ability to develop
Sol-gel system
The Optimized formula was developed and used for formulation of In-situ gel.
Sr No. Ingredients Quantity (gm) Role
1 Curcumin 0.1 API
2 TSP 0.3 Polymer
3 Ethanol 1 (ml) Solvent
4 Carbopol-934 0.1 Co-Polymer
5 Water q.s (ml) Vehicle
Table no.2 the final formula for the formulation
Gel formation at different pH-
The Gel formation of solution was tested by spraying the solution of in Buffers of
different pH to determine in which pH the solution turns into gel.
Observation –
The Oral cavity has pH of 6.8-7.4 and when the solution is sprayed in the Buffer of pH
6.8 the solution turns into Gel (Sol-Gel Transformation) in 5 sec.
Parameter Buffer
(pH 5)
Buffer
(pH 6)
Buffer (pH 6.8) Buffer
(pH 7)
Buffer
(pH 7.2)
Gel
Formation
- - Gel formation - -
Gel time - - 5 sec - -
Table no.3 Formation of Gel in Buffers of different pH
 Formulation Of In-situ Gel
Weight the 0.1 gm of drug (curcumin) dissolve in 1 ml of ethanol (S1)
In other beaker add 0.3 gm TSP and 0.1 gm Carbopol- 934 dissolve in
10 ml of water (S2)
The solution of curcumin (S1) was slowly added in the solution of
carbopol-934 (S2) with constant stirring.
The volume was made up by using water to form a solution
This solution when comes in contact with buffer of pH 6.8 (pH of oral
cavity) the Solution turns into Gel.
 Evaluation Parameters -
 Evaluation Parameter for Curcumin
Organoleptic Characteristics of Curcumin
 Evaluation Parameter for TSP
Organoleptic Properties of Tamarind Seed Polysaccharide (TSP)
Micro-meritic Properties of TSP
Fourier Transform Infrared Spectroscopy (FTIR) of TSP
 Evaluation Parameter for In-situ gel
Organoleptic Evaluation Of gel
In-vitro drug release
Anti-microbial activity
 Evaluation Parameter for In-situ gel
The various Evaluation Parameters of In-situ gel was performed and they results are observed
as follows-
Sr no. Parameter Result
1 Colour Yellow
2 Odour Pungent
3 Taste Slightly Bitter
4 pH 6
5 Viscosity 1.423 Pa.sec
6 Specific gravity 2.16
7 Density 1.256gm/ml
8 Sedimentation 0.2
Table no.4 Evaluation Parameters of In-situ gel
 Organoleptic Characteristics of Curcumin
Curcumin was tested for organoleptic characters such as Appearance, Colour and Odour.
Observation –
The curcumin was observed as crystalline powder, that was yellowish-orange in colour, had a
distinctive scent, and was compared to standard. It was reported that the results were consistent
with expectations.
Sr no. Parameters Standard Observation
1 Appearance Crystalline Powder Crystalline Powder
2 Odour Distinctive odour Distinctive odour
3 Colour Yellow -Orange Yellow -Orange
Table no. 5 Organoleptic characteristics of Curcumin
Evaluation Parameter for TSP-
Organoleptic Properties of Tamarind Seed Polysaccharide (TSP)
TSP was tested for organoleptic characters such as Appearance,Odour,Colour.
Observation- The TSP was found to be in Crystalline powder form which was odourless and
slightly brown in colour and it matches with the standard.
Sr no. Parameter Standard Observation
1. Appearance Crystalline
Powder
Crystalline
Powder
2. Odour Odour less Odour less
3. Colour Slightly brown Slightly
brown
Table no.6 Organoleptic Properties of TSP
Micro-meritic Properties of TSP-
The various micro-meritic properties of TSP was performed to determine the Physical stability of
TSP.
Observation- TSP showed an excellent flow property with Carr’s index 13, Hausner’s ratio 1.15
and angle of repose 21˚.
Parameters TSP Flow Property
Angle of repose (˚) 21.92± 1.1 Excellent
Tapped density (g/cm3) 0.363± 0.001 -
Bulk Density (g/cm3) 0.465± 0.06 -
Carr’s Index % 13 Excellent
Hausners ratio 1.15 Excellent
Table no.8 Micro- meritic Properties of TSP
 Fourier Transform Infrared Spectroscopy (FTIR) of TSP
The FTIR spectrum of TSP was recorded and compared with that of the standard in the literature.
The spectrum shows correspondences with that of the standard, thus confirming the genuineness
of the TSP.
Fig no.7 FTIR of TSP
 Interpretation of peaks obtained in the IR spectra of TSPalong with their
corresponding functional group.
Wave number
standard (cm -1)
Wave number
Observed (cm -1)
Group identified
3600-3400 3413.39 OH
2950-2260 2925.48 C-H str
2000-1650 - -
1732-1750 1715.37 COO str
1300-800 1229.4 C-H ben
1050 1031.73 C-O str
Table no.9 Interpretation of Peaks obtained in the IR spectra of TSP
 In-vitro drug release-
In-vitro drug release of In-situ gel was Performed by using Franz diffusion membrane in the Phosphate
buffer of pH 6.8( pH of oral cavity) for 90 minutes and the temperature is maintained at 37 °C
Procedure-
Before the experiment, the diffusion membrane was soaked in Phosphate Buffer (pH 6.8) for 24 hrs.
The 1gm of gel was placed in the diffusion membrane ( Donor compartment) and the membrane was kept in
contact with 100 ml of Phosphate buffer of pH 6.8 (Receptor compartment).
Then 1ml of buffer solution was withdrawn by using pippete into 10 ml volumetric flasks and replaced by same
amount of phosphate 6.8 pH buffer.
The solution was removed from receptor medium at time interval of 5,10,20,35,60,90 minutes in to determine the
diffusion of drug into solution at different time.
The buffer solution was then diluted by using distilled water and volume was made up to 10 ml.
Dilutions were observed under UV visible spectrometer at wavelength 420 nm to determine the drug release.
Observation- The standard calibration curve was used for the determination of in-vitro release
of drug, drug content in In-situ gel Calibration curve for curcumin was performed at λ 420 nm.
Concentration (µg/ml) Absorbance
2 0.2547
4 0.4099
6 0.6109
8 0.8236
10 0.9986
 Determination of calibration curve of Curcumin by UV analytical method:
Table no.10 Conc. and Absorbance of Curcumin
Time
(min)
y M c x (mcg) Conc.
(mg)
C %CDR
5 0.009 0.0098 0.0023 0.68 0.68 0.68 0.68
10 0.24 0.0098 0.0023 2.21 2.21 2.89 2.89
20 0.29 0.0098 0.0023 2.72 2.72 5.62 5.62
35 0.38 0.0098 0.0023 3.64 3.64 9.26 9.26
60 0.41 0.0098 0.0023 3.95 3.95 13.21 13.21
90 0.45 0.0098 0.0023 4.36 4.36 17.57 17.57
Fig no.8 Drug-release curve
%CDR
Table no.11 In-vitro diffusion of curcumin
The main causative agent for Peridontitis are number of Gram+ ve and Gram – ve bacterias like Bacteroides
forsythus, Capnocytophaga, streptoccocus bacillus, E.coli etc.
The Anti-microbial study of In-situ gel was performed against Bacillus (gram+ve) and E-coli (gram-ve) and
compared with Standard (2%) Mertronidazole gel.
Fig no.8 ZOI against Bacillus (gram+ve) Fig no.9 ZOI against E-coli (gram-ve)
Observation –
 The zone of inhibition of of standard was found to be 3.1cm and ZOI of In-situ gel was found to be 2.9 cm against
Bacillus( gram + ve ) which shows that the In-situ gel shows anti-microbial activity against bacillus ( gram + ve).
 The zone of inhibition of of standard was found to be 3 cm and ZOI of In-situ gel was found to be 2.6 cm against
E-coli (gram-ve) which shows that the In-situ gel shows anti-microbial activity against E-coli (gram-ve).
 Anti-microbial activity
 Conclusion-
Biocompatible In-situ gel by using TSP was Formulated and evaluated.
The Optimized formulation demonstrated good release profile.
The In-situ gel shows Anti-microbial activity which is same as the Standard
formulation therefore, the formulation is effective against the Periodontitis.
Future scope
 In-vivo study
 Anti-Inflammatory activity
 References-
Sarada K, Firoz S, Padmini K. In-situ gelling system: a review. Int J Curr Pharm Rev Res
2014;5:76-90
Jannavi R. Srinivasan, Ph. D., and reviewed by Eugenia Dessipri,Tamarind Seed
Polysaccharide CTA 2017 pg- 1
Suisha F et.al Xyloglucan gels as sustained release vehicles for intraperitoneal administration
of mitomycin C. Int J Pharm, 1998; 172: 27-32.
Abe Y, Hashimoto S, Horie T. Curcumin inhibition of inflammatory cytokine production by
human peripheral blood monocytes and alveolar macrophages. Journal of Pharmacology
Research.39; 1999: 41-47.
 Nirmal HB et al. In situ gel: New trends in controlled and sustained drug delivery system.
Ramya DD et al. In-Situ Gelling System – Potential Tool For Improving Therapeutic Effects Of
Drugs. Int J Pharm And Pharma Sci., 2013; 5(3): 27-30.
Rehaman S et al. Site Specific Delivery System for the treatment of Periodontitis. Ind J Pharma
Sci March-April, 2003; 106 – 112.
Thank You !!!

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Polysaccharide Based Drug Delivery System for Periodontitis-PPT.pptx

  • 1. Progressive Education Societies PES. Modern College Of Pharmacy Sector No.21Yamunagar, Nigdi,Pune-411044 “Polysaccharide based Drug Delivery System For Periodontitis” Presented By- Ms.Vasundhara Pramod Patil Final Year B. Pharm ( Div -B) 4071 Guided By- Dr. Sangita. A. Kale (Assistant Professor) Department Of Pharmaceutics
  • 2. Contents  Introduction  Need Of Work  Aim And Objective  Plan Of Work  Drug and Excipient Profile  Experimental Work  Result And Discussion References
  • 3. INTRODUCTION  Periodontitis is a chronic inflammatory disease of Periodontium.  It is the main cause of tooth loss and is considered one of the biggest threats to the oral health.  Periodontal diseases are mainly the result of Infections and inflammation of the gums and bone that surround and support the teeth.  In its early stage, it is called as Gingivitis, in which the gums can become swollen and appears red and they may bleed.  In its more serious form, it is called as Periodontitis, in which the gums can pull away from the tooth and the teeth may loosen or even fall out.  Periodontal disease is mostly seen in adults.  Periodontal disease and tooth decay are the two biggest threats to dental health.
  • 4. Comparison of Normal and Periodontal tooth Fig no.1 Normal and Periodontal tooth
  • 5.  Stages Of Periodontitis Based on the severity and complexity of management Stage I: Initial periodontitis Stage II: Moderate periodontitis Stage III: Severe periodontitis Stage IV: Severe periodontitis with the potential loss of dentition Based on the extent and distribution a. Localized b. Generalized c. Molar-incisor distribution Based On Grades GradeA:Slow rate of progression Grade B: Moderate rate of progression Grade C: Rapid rate of progression
  • 6. • Diagrammatic Representation of Stages of Periodontitis Fig no.2 Stages of Periodontitis
  • 7.  Symptoms and Causes of Periodontitis SYMPTOMS  Swollen and puffy gums.  Sensitive teeth.  Bright red, Dusky red, Purplish gums.  Tender gums that bleed easily.  New spaces form between teeth.  Formation of Puss between teeth and gums.  Painful chewing. CAUSES Bacteria's in the oral cavity are the main cause of Periodontitis.  Heredity.  Poor oral health.  Taking medication that causes dry mouth.  Braces which do not fit properly.
  • 8. In Situ Gel For Periodontitis In situ gels are the solutions or suspensions that undergo gelation after reaching the particular site due to contact with body fluids or physicochemical changes (i.e., pH, temperature, ionic concentration, UV radiation, presence of specific molecules or ions, external triggers, etc). The major importance of in-situ gel is administration of accurate & reproducible quantities compared to already formed gel. IMPORTANCE OF IN SITU GELLING SYSTEM •In situ gel helps for the controlled and sustained release of the drug by its special Sol- Gel transition. •It helps to reduce frequency of drug administration. •Low drug dose required and there will be no drug accumulation and no side effects of drug. •More bioavailability of the drug. •Increased residence time of the drug due to gel formation. •The in situ gelling decreases wastage of the drug.
  • 9. Fig no. 3 Pathophysiology of Periodontitis and working of In-situ gel
  • 10. Advantages and Disadvantages Of In situ Gelling System ADVANTAGES To reduce medication waste. For administrative convenience. It can be administered to elderly and unconscious patients. It aids in the prolonged or longer release of drugs. It promotes more patient cooperation and comfort. Promotes biocompatibility and biodegradation by employing natural polymers. DISADVANTAGES Only small doses can be administered. Due to chemical degradation, there is a chance of instability. It may results in premature dissolution due to low mechanical strength.
  • 11. Need and Rationale of work Curcumin • Curcumin has Anti-inflammatory and anti-bacterial activities which are used to treat Periodontal symptoms. TSP • TSP shows Dual action Muco-adhesive action due to which the gel stays adhere to the site of action. • It is an Excellent biodegradable, bio-compatible, and non-irritant Bio- polymer. • TSP also act as a Gelling agent. Carbapol • It is pH dependent polymer, which stays in solution form at acidic pH but forms a low viscosity gel at alkaline pH. • It is used as Thickening and Gelling agent which are important properties for Gel formation. In-situ gel • The in-situ gelling decreases wastage of the drug. • It provides More bioavailability of the drug. • In-situ gel shows sustained and controlled drug delivery.
  • 12. Aim And Objective Aim : To develop and evaluate In-situ gel for Periodontitis by using Tamarind seed polysaccharide (TSP) Objective:- To Evaluate In-situ gel containing TSP for Periodontitis.
  • 13. Plan Of Work  Literature review  Drug and excipients profile  Preliminary and Pre formulation study a) Characterisation of drug b) FTIR Spectroscopy  Preparation of In situ gel a) Preliminary development b) Preparation of Gel by using Polysaccharide  Evaluation of In situ gel a) Rheological Study b) In-vitro drug release c) Antibacterial activity
  • 14. Literature survey Sr no. Name of the article Authors Result 1 Development and Evaluation of in Situ Gelling System for Treatment of Periodontitis Khushbu S. Patel Dr. K.R.Vadalia Dr. J. K. Patel Tinidazole is well reported for the treatment of periodontal disease, they have better penetration into periodontal tissues, minimal bacterial resistance as compared to many of the other drugs used for the treatment.The excipients used in this present work are Gellan gum and Poloxamer 407 as gelling agent which form immediate gel. The Methyl paraben and Propyl paraben is used as preservativesThe studies revealed that drug and polymers were compatible. 2 Xyloglucan Based In Situ Gel of Lidocaine HCl for the Treatment of Periodontosis Ashlesha P.Pandit Vinit S.Kulkarni Lidocaine hydrochloride loaded periodontal temperature-sensitive in situ gel was successfully developed by cold method using xyloglucan based mucoadhesive polymer TSP for insertion into periodontal pocket to have painless treatment... Use of natural, less costly, biodegradable, and easily available mucoadhesive TSP polymer as well as avoidance of needle insertions during scaling and root planning of periodontosis helped achieve patient compliance by ultimately reducing the cost of the treatment. 3 Clinical and Anti- Inflammatory Effect of Curcumin Oral Gel as Adjuncts in Treatment of Periodontal Pocket Hayder Thabit Farhood, Basma Ghafori Ali The periodontal disease is among the most popular medical situations which might affect humans. Periodontal pocket that is known as a pathologically extended gingival sulcus which is one of most essential clinical characteristics of the periodontal disease.. An adjunct to scaling and root planning has been introducing as curcumin. Curcumin possess antioxidant, anti-inflammatory, and anti-microbial properties.
  • 15. Sr no. Name of the article Authors Result 4. In situ gel drug delivery system for periodontitis: an insight review Ravishankar Yadav, Indu lata kunwar, ,vishal gaur Novel in situ forming gel is introduced at the site that shows a promising potential to overcome one of the main practical obstacles associated with the treatment of local periodontitis: partial adhesion to the surrounding tissue, causing in the accidental expulsion of at least parts of the implants from patient’s pockets. This results in a large residence time of the system at the site of action and the uncertainty of the final exposure to the drug .From the reviewed literature, it is concluded that experimental evidence suggests that the in situ gel-forming systems can be useful in treating several common diseases of the oral cavity. 5. Evaluation and Characterization of Tamarind Gum Polysaccharide: The Biopolymer Sonali sundaram, Shivkanya fuloria, Rishabha malavia Tamarindus indica was isolated using distilled water as a solvent system and ethyl alcohol as precipitating agent. Phytochemical investigation showed the presence of carbohydrates while reducing sugar, glucose, tannins, proteins, and polysaccharides were absent.
  • 16. Drug And Excipient Profile Curcumin Curcumin is the Popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae) and obtained from rhizomes of Curcuma longa L. The Main curcuminoids are Curcumin (94%) ,de-methoxycurcumin (6%) and bis-demethoxycurcumin (0.3%) The curcuminoids are Polyphenols and are responsible for the Yellow color of turmeric.  Properties of Curcumin Molecular Formula- C21H20O6 Molecular Weight- 368.4 kDa IUPAC Name - (1E,6E)-1,7-bis (4-hydroxy- 3-methoxyphenyl) -1,6- heptadiene-3,5-dione Half life- 6-7 hrs pKa -7.8 (basic) Drug Category: Anti-inflammatory, Anticancer, Antimicrobial. Fig no.4 Structure of Curcumin
  • 17. Tamarind Seed Polysaccharide(TSP) TSP is a plant polysaccharide derived from the Tamarindus indica Linn seed endosperm belongs Fabaceae family. It is a water-soluble, non-ionic, branched polysaccharide with hydrophilic, gel-forming, and muco-adhesive characteristics. TSP is also Biodegradable, Biocompatible, non-carcinogenic, and irritant-free. It is used in the pharmaceutical, cosmetic, and food industries as a promising biopolymer.  Properties of TSP Molecular formula- (C6H10O3)n Molecular weight – 1735 kDa Description- White crystalline Powder Category - Muco-adhesive Application in pharmaceutical - Stabilizer, thickening agent, gelling agent. Fig no.5 TSP
  • 18. CARBOPOL-934 Carbopol-934 is a well-known pH dependent polymer, which stays in solution form at acidic pH but forms a low viscosity gel at alkaline pH. General Properties of Carbopol Synonym: Acrylic acid polymer IUPAC Name: prop-2-enoic acid Molecular formula: (C3H4O2)n Category: Gelling agent Description: White amorphous powder Solubility: soluble in water  Application in pharmaceutical: Stabilizer, Thickening agent, Gelling agent Fig no. 6 Structure of Carbopol
  • 19.  Experimental Work Synthesis of Tamarind Seed Polysaccharide (TSP) Formulation Of In-situ Gel Evaluation Of In-situ Gel
  • 20.  Isolation of Tamarind Seed Polysaccharide (TSP) Tamarind seed polysaccharide (TSP) is Polysaccharide extracted from the kernel of seeds of Tamarindus indica Lin, Family Leguminosae. Synthesis of TSP- 250 gms of Tamarind seeds were crushed and powdered A viscous solution was obtained when powder is boiled with 500 ml of distilled water with continouse stirring filter the solution and dry the supernatant. the dried supernatent is then referred to as Tamarind kernel powder. 20 gm of tamarind kernel powder and 200 ml distilled water are mixed to form slurry. 800 ml of distilled water was added with the slurry. At 40 °C, the precipitate the obtained was dried and dried film was ground into a fine powder to obtain TSP. Supernatent is added to 100% ethanol in a volume that was double its original size. The solution was boiled for 20 minutes With constant stirring, the supernatant was separated
  • 21. Trial Batches Of In-situ Gel – The various trial batches were formulated and compared to each other to determine the final formula for the batch in which the Sol-Gel system is observed, when the solution is sprayed in the Phosphate Buffer of suitable pH (pH of oral cavity). Trial Batch No. Ingredients F1 F2 F3 F4 F5 1 Curcumin(gm) 0.1 0.1 0.1 0.1 0.1 2 TSP(gm) 0.1 0.1 0.2 0.3 0.1 3 Ethanol 1 1 1 1 1 4 Carbopol-934 (gm) 0.1 0.2 0.1 0.1 0.3 5 Water q.s q.s q.s q.s q.s Table no.1 Trial batches of the formulation
  • 22.  Optimized Batch of formulation – The Optimized batch of the formulation is representsAccurate quantities of the ingredients which are used to form the Ideal formulation. The optimized batch is selected from various trial batched according to their ability to develop Sol-gel system The Optimized formula was developed and used for formulation of In-situ gel. Sr No. Ingredients Quantity (gm) Role 1 Curcumin 0.1 API 2 TSP 0.3 Polymer 3 Ethanol 1 (ml) Solvent 4 Carbopol-934 0.1 Co-Polymer 5 Water q.s (ml) Vehicle Table no.2 the final formula for the formulation
  • 23. Gel formation at different pH- The Gel formation of solution was tested by spraying the solution of in Buffers of different pH to determine in which pH the solution turns into gel. Observation – The Oral cavity has pH of 6.8-7.4 and when the solution is sprayed in the Buffer of pH 6.8 the solution turns into Gel (Sol-Gel Transformation) in 5 sec. Parameter Buffer (pH 5) Buffer (pH 6) Buffer (pH 6.8) Buffer (pH 7) Buffer (pH 7.2) Gel Formation - - Gel formation - - Gel time - - 5 sec - - Table no.3 Formation of Gel in Buffers of different pH
  • 24.  Formulation Of In-situ Gel Weight the 0.1 gm of drug (curcumin) dissolve in 1 ml of ethanol (S1) In other beaker add 0.3 gm TSP and 0.1 gm Carbopol- 934 dissolve in 10 ml of water (S2) The solution of curcumin (S1) was slowly added in the solution of carbopol-934 (S2) with constant stirring. The volume was made up by using water to form a solution This solution when comes in contact with buffer of pH 6.8 (pH of oral cavity) the Solution turns into Gel.
  • 25.  Evaluation Parameters -  Evaluation Parameter for Curcumin Organoleptic Characteristics of Curcumin  Evaluation Parameter for TSP Organoleptic Properties of Tamarind Seed Polysaccharide (TSP) Micro-meritic Properties of TSP Fourier Transform Infrared Spectroscopy (FTIR) of TSP  Evaluation Parameter for In-situ gel Organoleptic Evaluation Of gel In-vitro drug release Anti-microbial activity
  • 26.  Evaluation Parameter for In-situ gel The various Evaluation Parameters of In-situ gel was performed and they results are observed as follows- Sr no. Parameter Result 1 Colour Yellow 2 Odour Pungent 3 Taste Slightly Bitter 4 pH 6 5 Viscosity 1.423 Pa.sec 6 Specific gravity 2.16 7 Density 1.256gm/ml 8 Sedimentation 0.2 Table no.4 Evaluation Parameters of In-situ gel
  • 27.  Organoleptic Characteristics of Curcumin Curcumin was tested for organoleptic characters such as Appearance, Colour and Odour. Observation – The curcumin was observed as crystalline powder, that was yellowish-orange in colour, had a distinctive scent, and was compared to standard. It was reported that the results were consistent with expectations. Sr no. Parameters Standard Observation 1 Appearance Crystalline Powder Crystalline Powder 2 Odour Distinctive odour Distinctive odour 3 Colour Yellow -Orange Yellow -Orange Table no. 5 Organoleptic characteristics of Curcumin
  • 28. Evaluation Parameter for TSP- Organoleptic Properties of Tamarind Seed Polysaccharide (TSP) TSP was tested for organoleptic characters such as Appearance,Odour,Colour. Observation- The TSP was found to be in Crystalline powder form which was odourless and slightly brown in colour and it matches with the standard. Sr no. Parameter Standard Observation 1. Appearance Crystalline Powder Crystalline Powder 2. Odour Odour less Odour less 3. Colour Slightly brown Slightly brown Table no.6 Organoleptic Properties of TSP
  • 29. Micro-meritic Properties of TSP- The various micro-meritic properties of TSP was performed to determine the Physical stability of TSP. Observation- TSP showed an excellent flow property with Carr’s index 13, Hausner’s ratio 1.15 and angle of repose 21˚. Parameters TSP Flow Property Angle of repose (˚) 21.92± 1.1 Excellent Tapped density (g/cm3) 0.363± 0.001 - Bulk Density (g/cm3) 0.465± 0.06 - Carr’s Index % 13 Excellent Hausners ratio 1.15 Excellent Table no.8 Micro- meritic Properties of TSP
  • 30.  Fourier Transform Infrared Spectroscopy (FTIR) of TSP The FTIR spectrum of TSP was recorded and compared with that of the standard in the literature. The spectrum shows correspondences with that of the standard, thus confirming the genuineness of the TSP. Fig no.7 FTIR of TSP
  • 31.  Interpretation of peaks obtained in the IR spectra of TSPalong with their corresponding functional group. Wave number standard (cm -1) Wave number Observed (cm -1) Group identified 3600-3400 3413.39 OH 2950-2260 2925.48 C-H str 2000-1650 - - 1732-1750 1715.37 COO str 1300-800 1229.4 C-H ben 1050 1031.73 C-O str Table no.9 Interpretation of Peaks obtained in the IR spectra of TSP
  • 32.  In-vitro drug release- In-vitro drug release of In-situ gel was Performed by using Franz diffusion membrane in the Phosphate buffer of pH 6.8( pH of oral cavity) for 90 minutes and the temperature is maintained at 37 °C Procedure- Before the experiment, the diffusion membrane was soaked in Phosphate Buffer (pH 6.8) for 24 hrs. The 1gm of gel was placed in the diffusion membrane ( Donor compartment) and the membrane was kept in contact with 100 ml of Phosphate buffer of pH 6.8 (Receptor compartment). Then 1ml of buffer solution was withdrawn by using pippete into 10 ml volumetric flasks and replaced by same amount of phosphate 6.8 pH buffer. The solution was removed from receptor medium at time interval of 5,10,20,35,60,90 minutes in to determine the diffusion of drug into solution at different time. The buffer solution was then diluted by using distilled water and volume was made up to 10 ml. Dilutions were observed under UV visible spectrometer at wavelength 420 nm to determine the drug release.
  • 33. Observation- The standard calibration curve was used for the determination of in-vitro release of drug, drug content in In-situ gel Calibration curve for curcumin was performed at λ 420 nm. Concentration (µg/ml) Absorbance 2 0.2547 4 0.4099 6 0.6109 8 0.8236 10 0.9986  Determination of calibration curve of Curcumin by UV analytical method: Table no.10 Conc. and Absorbance of Curcumin
  • 34. Time (min) y M c x (mcg) Conc. (mg) C %CDR 5 0.009 0.0098 0.0023 0.68 0.68 0.68 0.68 10 0.24 0.0098 0.0023 2.21 2.21 2.89 2.89 20 0.29 0.0098 0.0023 2.72 2.72 5.62 5.62 35 0.38 0.0098 0.0023 3.64 3.64 9.26 9.26 60 0.41 0.0098 0.0023 3.95 3.95 13.21 13.21 90 0.45 0.0098 0.0023 4.36 4.36 17.57 17.57 Fig no.8 Drug-release curve %CDR Table no.11 In-vitro diffusion of curcumin
  • 35. The main causative agent for Peridontitis are number of Gram+ ve and Gram – ve bacterias like Bacteroides forsythus, Capnocytophaga, streptoccocus bacillus, E.coli etc. The Anti-microbial study of In-situ gel was performed against Bacillus (gram+ve) and E-coli (gram-ve) and compared with Standard (2%) Mertronidazole gel. Fig no.8 ZOI against Bacillus (gram+ve) Fig no.9 ZOI against E-coli (gram-ve) Observation –  The zone of inhibition of of standard was found to be 3.1cm and ZOI of In-situ gel was found to be 2.9 cm against Bacillus( gram + ve ) which shows that the In-situ gel shows anti-microbial activity against bacillus ( gram + ve).  The zone of inhibition of of standard was found to be 3 cm and ZOI of In-situ gel was found to be 2.6 cm against E-coli (gram-ve) which shows that the In-situ gel shows anti-microbial activity against E-coli (gram-ve).  Anti-microbial activity
  • 36.  Conclusion- Biocompatible In-situ gel by using TSP was Formulated and evaluated. The Optimized formulation demonstrated good release profile. The In-situ gel shows Anti-microbial activity which is same as the Standard formulation therefore, the formulation is effective against the Periodontitis.
  • 37. Future scope  In-vivo study  Anti-Inflammatory activity
  • 38.  References- Sarada K, Firoz S, Padmini K. In-situ gelling system: a review. Int J Curr Pharm Rev Res 2014;5:76-90 Jannavi R. Srinivasan, Ph. D., and reviewed by Eugenia Dessipri,Tamarind Seed Polysaccharide CTA 2017 pg- 1 Suisha F et.al Xyloglucan gels as sustained release vehicles for intraperitoneal administration of mitomycin C. Int J Pharm, 1998; 172: 27-32. Abe Y, Hashimoto S, Horie T. Curcumin inhibition of inflammatory cytokine production by human peripheral blood monocytes and alveolar macrophages. Journal of Pharmacology Research.39; 1999: 41-47.  Nirmal HB et al. In situ gel: New trends in controlled and sustained drug delivery system. Ramya DD et al. In-Situ Gelling System – Potential Tool For Improving Therapeutic Effects Of Drugs. Int J Pharm And Pharma Sci., 2013; 5(3): 27-30. Rehaman S et al. Site Specific Delivery System for the treatment of Periodontitis. Ind J Pharma Sci March-April, 2003; 106 – 112.