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H. R. Patel Institute of Pharmaceutical Education and
Research, Shirpur
Presented By:
Pratik Anil Sonar
M. Pharm 1st year
(Dept. of P’ceutics)
Guided By :
Dr. P. K. Deshmukh
(Dept. of P’ceutics)
“Phytosomes”
27-05-2020Phytosomes prepared by Pratik sonar MPH10
1
Content:
1. Introduction
2. Structure of phytosomes
3. Strength of phytosomes
4. Advantages
5. Disadvantages
6. Method of preparation
7. Evaluation parameter
8. Application
9. Conclusion
10.References
27-05-2020Phytosomes prepared by Pratik sonar MPH10
2
Introduction[1]
• The term “phyto” suggests that plant whereas “somes”
suggests that cellular or cell like structure.
27-05-2020Phytosomes prepared by Pratik sonar MPH10
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Introduction cont…
• The Phytosome technology, developed by Indena S.P.A. of Italy.
• Phytosome is a patented technology (U.S. Patent).
• better absorbed and produces better results.
• Phytosomes are more bioavailable.
• Phytosome is novel drug delivery system is a that combines
hydrophilic bioactive phytoconstituents of herbal extracts and
bound by phospholipids.
(e.g. soybean phospholipids ,lecithin)
27-05-2020Phytosomes prepared by pratik sonar MPH10
4
Structure of phytosomes
• PC (Phosphatidylcholine) is a bifunctional compound. Specifically
the choline head (hydrophilic) binds to these compounds while the
phosphatidyl portion (lipophilic) comprising the body and tail which
then envelopes the choline bound material and forms phyto-
phospholipid complex.
• Phosphatidyl-choline - phospholipid
• Phosphatidyl moiety - lipophilic
• Choline moiety - Hydrophilic
27-05-2020Phytosomes prepared by pratik sonar MPH10
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Strength of phytosomes[2]
• Strength of phytosomes Phytosomes show better stability as chemical bond is
formed between phospholipid molecule and phytoconstituent(s).
• Dose of phytoconstituents is reduced due to more bioavailability of the
phytoconstituents in the complex form. Duration of action is increased.
• Phytoconstituents complex with phospholipids are more stable in gastric sections
and resist the action of gut bacteria. Enhanced permeability of phytoconstituents
across the biological membranes.
• Absorption of lipid insoluble polar phytoconstituents through different routes
shows better absorption, hence shows significantly higher therapeutic effects.
• Phoshatidylcholine used in the formation of phytosomes, besides acting as a
carrier also possess several therapeutic properties, hence gives the synergistic
effect when particular substance is given.
• Drug entrapment is not a problem with phytosome as the complex is
biodegradable.
27-05-2020Phytosomes prepared by Pratik sonar MPH10
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Advantages of Phytosomes[2]
1. Better bioavailability.
2. Reduced dose.
3. Enhanced absorption of herbal constituents.
4. Better stability profile.
5. Greater therapeutics benefit.
27-05-2020Phytosomes prepared by Pratik sonar MPH10
7
Disadvantages of phytosomes[2]
1. Phytoconstituent from phytosomes are rapidly eliminated.
27-05-2020Phytosomes prepared by Pratik sonar MPH10
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Method of preparation of phytosomes[1]
1. Solvent evaporation methods
2. Rotary evaporation technique
3. Anti-solvent Precipitation Technique
27-05-2020Phytosomes prepared by Pratik sonar MPH10
9
1)Solvent evaporation methods
27-05-2020Phytosomes prepared by pratik sonar MPH10
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Drug, polymer and Phospholipids
Take in RBF
Reflux with specific solvent at temp 50-60ºC
Mixture may be conc.To 5-10ml to get ppt
Filtered and collected
Stored in amber colored glass bottle at RT.
2)Rotary evaporation technique
27-05-2020Phytosomes prepared by pratik sonar MPH10
11
Drug, polymer and Phospholipids
Dissolve in specific solvent in a rotary spherical bottom
flask followed by stirring for 3 hrs. at temp 40ºC.
Thin film of sample obtained, in which n- hexane added
and stirred continuously by magnetic stirrer
Ppt phytosome collected and stored in amber colored glass
bottle at RT
3)Anti-solvent Precipitation Technique
27-05-2020Phytosomes prepared by pratik sonar MPH10
12
Drug, polymer and Phospholipids
Taken in RBF & reflux with specific solvent at temp. not
exceeding 60◦C
Mixture can conc. to 5-10 ml
Add n-hexane carefully with continuous stirring
To get ppt, filtered & collected, stored in vacuum desiccators
The dried ppt. crushed in mortar & sieved through #100 meshes
The dried ppt, phytosome loaded placed in amber colored bottle at
RT
Evaluation of Phytosomes[3]
• Visualization: Visualization of phytosomes can be achieved
using transmission electron microscopy (TEM) and by
scanning electron microscopy (SEM).
• Vesicle size and zeta potential: The particle size and zeta
potential can be determined by dynamic light scattering
(DLS) using a computerized inspection system.
• Entrapment efficiency: The entrapment efficiency of a
drug by phytosomes can be measured by the
ultracentrifugation technique .
27-05-2020Phytosomes prepared by Pratik sonar MPH10
13
• Transition temperature: The transition temperature of the
vesicular lipid systems can be determined by differential
scanning calorimeter (DSC).
• Surface tension activity measurement: The surface
tension activity of the drug in aqueous solution can be
measured by the ring method in a Du Nouy ring tensiometer.
• Drug content: The amount of drug can quantified by a
suitable spectroscopic method.
27-05-2020Phytosomes prepared by pratik sonar MPH10
14
• FTIR: The spectroscopic evaluation of the formed
complex can be confirmed by FTIR simply by comparing
the spectrum of the complex and the individual
components.
• In vitro and in vivo evaluations: Models of in‐vitro and
in‐vivo evaluations are selected on the basis of the
expected therapeutic activity of biologically active
phytoconstituents present in the phytosomes.
• Spectroscopic evaluations:
• 1HNMR
• 13CNMR
27-05-2020Phytosomes prepared by pratik sonar MPH10
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Application[4]
• Enhancing Bioavalability:Evodiamine,a quinoline alkaloid,
these pytosomes reduce the first-pass metabolism by passing
liver and therefore avoiding the contact of the hepatic
metabolism enzymes.
• Antioxidant properties: A phytosomal formulation of
Quercetin was prepared with higher encapsulation efficiency and
physical stability to improve its efficacy in intestinal absorption
and its preservation from oxidation in foodstuffs.
27-05-2020Phytosomes prepared by Pratik sonar MPH10
16
• Hepato-Protective: Andrographolide(AN) obtained from
Andrographis paniculata linn include treatment of
hepatic impairment.
• Cancer treatment: Silybin (silibum marianum)is a
natural polyphenol with antioxidant and anti-cancer
properties which bloks estrogen receptor which are over
expresses in breast cancer.
27-05-2020Phytosomes prepared by pratik sonar MPH10
17
• Wound healing: Ethanolic extract of wrightia arborea
leaves and its phytosomes.the phytosome exhibited
about 90.40%healing while the ethanolic extract alone
could heal only 65.63%of the wound.
• Transdermal application: the phytosomal colpex of
saponins and plant extracts (panax ginseng M)more
active in protection against UV radiation.
27-05-2020Phytosomes prepared by Pratik sonar MPH10
18
Conclusion:
Phytosomes forms a bridge between the conventional
delivery system and novel delivery system. Phytosomes
exhibit better pharmacokinetic and pharmacodynamic
profile than conventional herbal extracts. Phytosomes is
used to increase the solubility as well as permeability of
the phytoconstituents present in part of the plant.
27-05-2020Phytosomes prepared by Pratik sonar MPH10
19
References:
1. R. P. Singh, H. V. Gangadharappa, K. Mruthunjaya; Phytosome Novel Herbal
Drug Delivery System : A Review, International Research Journal Of
Pharmacy; 2016, Vol 7, Issue 6.
2. Amith Kumar B, Prasanna Habbu, Thimmasetty, Lakshman, Prabha Hullatti,
Ravi Kumar S, Phytosomes as Novel Drug Delivery System for Herbal
Medicine –A Review; Systematic Reviews in Pharmacy, Jan-Dec, 2017, Vol 8,
Issue 1, 5-7.
3. M. Sravanthi and J. Shiva Krishna, PHYTOSOMES: A Novel Drug Delivery
For Herbal Extracts – A Review; International journal of Pharmaceutical
science and research; 2013, Vol. 4, Issue 3, 949-959.
4. Chivte Prajkta, Pardhi Vinal, Joshi Vineeta, Ajitha Rani R; A REVIEW ON
THERAPEUTIC APPLICATIONS OF PHYTOSOMES; Journal of Drug
Delivery and Therapeutics2017; 7(5):17-21
5. Josef kareparamban,a pravin novel revolution in herbal drugs ,IJRPC
2012,2(2)
27-05-2020
Phytosomes prepared by Pratik sonar MPH10
20
Thank
you
27-05-2020Phytosomes prepared by Pratik sonar MPH10
21

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Phytosomes

  • 1. H. R. Patel Institute of Pharmaceutical Education and Research, Shirpur Presented By: Pratik Anil Sonar M. Pharm 1st year (Dept. of P’ceutics) Guided By : Dr. P. K. Deshmukh (Dept. of P’ceutics) “Phytosomes” 27-05-2020Phytosomes prepared by Pratik sonar MPH10 1
  • 2. Content: 1. Introduction 2. Structure of phytosomes 3. Strength of phytosomes 4. Advantages 5. Disadvantages 6. Method of preparation 7. Evaluation parameter 8. Application 9. Conclusion 10.References 27-05-2020Phytosomes prepared by Pratik sonar MPH10 2
  • 3. Introduction[1] • The term “phyto” suggests that plant whereas “somes” suggests that cellular or cell like structure. 27-05-2020Phytosomes prepared by Pratik sonar MPH10 3
  • 4. Introduction cont… • The Phytosome technology, developed by Indena S.P.A. of Italy. • Phytosome is a patented technology (U.S. Patent). • better absorbed and produces better results. • Phytosomes are more bioavailable. • Phytosome is novel drug delivery system is a that combines hydrophilic bioactive phytoconstituents of herbal extracts and bound by phospholipids. (e.g. soybean phospholipids ,lecithin) 27-05-2020Phytosomes prepared by pratik sonar MPH10 4
  • 5. Structure of phytosomes • PC (Phosphatidylcholine) is a bifunctional compound. Specifically the choline head (hydrophilic) binds to these compounds while the phosphatidyl portion (lipophilic) comprising the body and tail which then envelopes the choline bound material and forms phyto- phospholipid complex. • Phosphatidyl-choline - phospholipid • Phosphatidyl moiety - lipophilic • Choline moiety - Hydrophilic 27-05-2020Phytosomes prepared by pratik sonar MPH10 5
  • 6. Strength of phytosomes[2] • Strength of phytosomes Phytosomes show better stability as chemical bond is formed between phospholipid molecule and phytoconstituent(s). • Dose of phytoconstituents is reduced due to more bioavailability of the phytoconstituents in the complex form. Duration of action is increased. • Phytoconstituents complex with phospholipids are more stable in gastric sections and resist the action of gut bacteria. Enhanced permeability of phytoconstituents across the biological membranes. • Absorption of lipid insoluble polar phytoconstituents through different routes shows better absorption, hence shows significantly higher therapeutic effects. • Phoshatidylcholine used in the formation of phytosomes, besides acting as a carrier also possess several therapeutic properties, hence gives the synergistic effect when particular substance is given. • Drug entrapment is not a problem with phytosome as the complex is biodegradable. 27-05-2020Phytosomes prepared by Pratik sonar MPH10 6
  • 7. Advantages of Phytosomes[2] 1. Better bioavailability. 2. Reduced dose. 3. Enhanced absorption of herbal constituents. 4. Better stability profile. 5. Greater therapeutics benefit. 27-05-2020Phytosomes prepared by Pratik sonar MPH10 7
  • 8. Disadvantages of phytosomes[2] 1. Phytoconstituent from phytosomes are rapidly eliminated. 27-05-2020Phytosomes prepared by Pratik sonar MPH10 8
  • 9. Method of preparation of phytosomes[1] 1. Solvent evaporation methods 2. Rotary evaporation technique 3. Anti-solvent Precipitation Technique 27-05-2020Phytosomes prepared by Pratik sonar MPH10 9
  • 10. 1)Solvent evaporation methods 27-05-2020Phytosomes prepared by pratik sonar MPH10 10 Drug, polymer and Phospholipids Take in RBF Reflux with specific solvent at temp 50-60ºC Mixture may be conc.To 5-10ml to get ppt Filtered and collected Stored in amber colored glass bottle at RT.
  • 11. 2)Rotary evaporation technique 27-05-2020Phytosomes prepared by pratik sonar MPH10 11 Drug, polymer and Phospholipids Dissolve in specific solvent in a rotary spherical bottom flask followed by stirring for 3 hrs. at temp 40ºC. Thin film of sample obtained, in which n- hexane added and stirred continuously by magnetic stirrer Ppt phytosome collected and stored in amber colored glass bottle at RT
  • 12. 3)Anti-solvent Precipitation Technique 27-05-2020Phytosomes prepared by pratik sonar MPH10 12 Drug, polymer and Phospholipids Taken in RBF & reflux with specific solvent at temp. not exceeding 60◦C Mixture can conc. to 5-10 ml Add n-hexane carefully with continuous stirring To get ppt, filtered & collected, stored in vacuum desiccators The dried ppt. crushed in mortar & sieved through #100 meshes The dried ppt, phytosome loaded placed in amber colored bottle at RT
  • 13. Evaluation of Phytosomes[3] • Visualization: Visualization of phytosomes can be achieved using transmission electron microscopy (TEM) and by scanning electron microscopy (SEM). • Vesicle size and zeta potential: The particle size and zeta potential can be determined by dynamic light scattering (DLS) using a computerized inspection system. • Entrapment efficiency: The entrapment efficiency of a drug by phytosomes can be measured by the ultracentrifugation technique . 27-05-2020Phytosomes prepared by Pratik sonar MPH10 13
  • 14. • Transition temperature: The transition temperature of the vesicular lipid systems can be determined by differential scanning calorimeter (DSC). • Surface tension activity measurement: The surface tension activity of the drug in aqueous solution can be measured by the ring method in a Du Nouy ring tensiometer. • Drug content: The amount of drug can quantified by a suitable spectroscopic method. 27-05-2020Phytosomes prepared by pratik sonar MPH10 14
  • 15. • FTIR: The spectroscopic evaluation of the formed complex can be confirmed by FTIR simply by comparing the spectrum of the complex and the individual components. • In vitro and in vivo evaluations: Models of in‐vitro and in‐vivo evaluations are selected on the basis of the expected therapeutic activity of biologically active phytoconstituents present in the phytosomes. • Spectroscopic evaluations: • 1HNMR • 13CNMR 27-05-2020Phytosomes prepared by pratik sonar MPH10 15
  • 16. Application[4] • Enhancing Bioavalability:Evodiamine,a quinoline alkaloid, these pytosomes reduce the first-pass metabolism by passing liver and therefore avoiding the contact of the hepatic metabolism enzymes. • Antioxidant properties: A phytosomal formulation of Quercetin was prepared with higher encapsulation efficiency and physical stability to improve its efficacy in intestinal absorption and its preservation from oxidation in foodstuffs. 27-05-2020Phytosomes prepared by Pratik sonar MPH10 16
  • 17. • Hepato-Protective: Andrographolide(AN) obtained from Andrographis paniculata linn include treatment of hepatic impairment. • Cancer treatment: Silybin (silibum marianum)is a natural polyphenol with antioxidant and anti-cancer properties which bloks estrogen receptor which are over expresses in breast cancer. 27-05-2020Phytosomes prepared by pratik sonar MPH10 17
  • 18. • Wound healing: Ethanolic extract of wrightia arborea leaves and its phytosomes.the phytosome exhibited about 90.40%healing while the ethanolic extract alone could heal only 65.63%of the wound. • Transdermal application: the phytosomal colpex of saponins and plant extracts (panax ginseng M)more active in protection against UV radiation. 27-05-2020Phytosomes prepared by Pratik sonar MPH10 18
  • 19. Conclusion: Phytosomes forms a bridge between the conventional delivery system and novel delivery system. Phytosomes exhibit better pharmacokinetic and pharmacodynamic profile than conventional herbal extracts. Phytosomes is used to increase the solubility as well as permeability of the phytoconstituents present in part of the plant. 27-05-2020Phytosomes prepared by Pratik sonar MPH10 19
  • 20. References: 1. R. P. Singh, H. V. Gangadharappa, K. Mruthunjaya; Phytosome Novel Herbal Drug Delivery System : A Review, International Research Journal Of Pharmacy; 2016, Vol 7, Issue 6. 2. Amith Kumar B, Prasanna Habbu, Thimmasetty, Lakshman, Prabha Hullatti, Ravi Kumar S, Phytosomes as Novel Drug Delivery System for Herbal Medicine –A Review; Systematic Reviews in Pharmacy, Jan-Dec, 2017, Vol 8, Issue 1, 5-7. 3. M. Sravanthi and J. Shiva Krishna, PHYTOSOMES: A Novel Drug Delivery For Herbal Extracts – A Review; International journal of Pharmaceutical science and research; 2013, Vol. 4, Issue 3, 949-959. 4. Chivte Prajkta, Pardhi Vinal, Joshi Vineeta, Ajitha Rani R; A REVIEW ON THERAPEUTIC APPLICATIONS OF PHYTOSOMES; Journal of Drug Delivery and Therapeutics2017; 7(5):17-21 5. Josef kareparamban,a pravin novel revolution in herbal drugs ,IJRPC 2012,2(2) 27-05-2020 Phytosomes prepared by Pratik sonar MPH10 20