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By Tushar Chavan
M Pharmacy 2018-2019
K.Y.D.S.C.T.College of Pharmacy, Sakegaon
NMU, Jalgaon [MH]
Email: tusharchavantsc@gmail.com
Updated April 30, 2019
INTRODUCTION
• Polyphenolics and terpenes are ubiquitous in plants, but their poor solubility
and hydrolytical instability in water and organic solvents at physiological pH
values make them very poorly absorbed both orally and topically.
• Bioavailability can be improved by using new delivery systems which can
enhance the rate and the extent of solubilization into aqueous intestinal fluids
and the capacity to cross bio membranes.
• It is claimed that phytosome increases absorption of "conventional herbal
extracts" or isolated active principles both topically as well as orally.
• Polyphenolics exhibit a marked affinity for phospholipids via hydrogen
bondings and dipolar interactions with the charged phosphates groups of
phospholipids.
• By complexing the polyphenolic phytoconstituents in a definite ratio with
phosphatidylcholine, Indena has developed a new series of non-covalent
supramolecular adducts named “Phytosome®”.
PHYTOSOME
• A phytosome is a complex of a natural active ingredient and a phospholipid -
mostly lecithin
• Phytosomes are novel drug delivery system containing hydrophilic bioactive
phytoconstituents of herbs surround and bound by phospholipids.
PREPARATION OF PHYTOSOME
Phospholipid Dissolved in organic solvent containing drug/extract Hydration
Solution of phospholipid in organic solvent with drug/extract Drying / Solvent
Evaporation Formation of thin film Formation of phytosomal suspension
Different additives used in the formulations of Phytosomes:
1. Phospholipids: Soya phosphatidyl choline, Egg phosphatidyl choline, Dipalmityl
phosphatidyl choline, Distearyl phosphatidyl choline, Phosphotidylcholine ,
Phosphotidylethanolamine, Phosphotidylserine.
2. Aprotic solvent: Dioxane, acetone, methylene chloride
3. Non solvent: n-hexane and non-solvent i.e. aliphatic hydrocarbon
4. Alcohol: Ethanol, Methanol
1) Antisolvent precipitation technique
Drug + Soya Lecitin Reflux With 20ml Dichloromethane At 60ºc For 2 Hr.
Concentrate Mixture To 5-10ml Add Hexane 20ml Filter The Ppt Formed Dry
,Crush And Pass Through #100
2) Rotary evaporation technique
Drug And Soya Lecithin Dissolved In 30 ml Of Tetrahydrofuran Stirring For 3
Hours At A Temperature Not Exceeding 40ºc Thin Film Is Formed Add n-Hexane
With Stirring Precipitate Obtained Dry And Pass Through Mesh Phytosomes
Formed
3) Solvent evaporation method
Drug and Soya Lecithin Refluxed With 20 ml of Acetone at a Temperature 50 -
60ºc for 2 hrs. Concentrated Mixture to 5-10 ml Obtain the Precipitate Filter
and Collect Phytosomes Obtained

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Phytosome, preaparation

  • 1. By Tushar Chavan M Pharmacy 2018-2019 K.Y.D.S.C.T.College of Pharmacy, Sakegaon NMU, Jalgaon [MH] Email: tusharchavantsc@gmail.com Updated April 30, 2019 INTRODUCTION • Polyphenolics and terpenes are ubiquitous in plants, but their poor solubility and hydrolytical instability in water and organic solvents at physiological pH values make them very poorly absorbed both orally and topically. • Bioavailability can be improved by using new delivery systems which can enhance the rate and the extent of solubilization into aqueous intestinal fluids and the capacity to cross bio membranes. • It is claimed that phytosome increases absorption of "conventional herbal extracts" or isolated active principles both topically as well as orally. • Polyphenolics exhibit a marked affinity for phospholipids via hydrogen bondings and dipolar interactions with the charged phosphates groups of phospholipids. • By complexing the polyphenolic phytoconstituents in a definite ratio with phosphatidylcholine, Indena has developed a new series of non-covalent supramolecular adducts named “Phytosome®”. PHYTOSOME • A phytosome is a complex of a natural active ingredient and a phospholipid - mostly lecithin • Phytosomes are novel drug delivery system containing hydrophilic bioactive phytoconstituents of herbs surround and bound by phospholipids.
  • 2. PREPARATION OF PHYTOSOME Phospholipid Dissolved in organic solvent containing drug/extract Hydration Solution of phospholipid in organic solvent with drug/extract Drying / Solvent Evaporation Formation of thin film Formation of phytosomal suspension Different additives used in the formulations of Phytosomes: 1. Phospholipids: Soya phosphatidyl choline, Egg phosphatidyl choline, Dipalmityl phosphatidyl choline, Distearyl phosphatidyl choline, Phosphotidylcholine , Phosphotidylethanolamine, Phosphotidylserine. 2. Aprotic solvent: Dioxane, acetone, methylene chloride 3. Non solvent: n-hexane and non-solvent i.e. aliphatic hydrocarbon 4. Alcohol: Ethanol, Methanol 1) Antisolvent precipitation technique Drug + Soya Lecitin Reflux With 20ml Dichloromethane At 60ºc For 2 Hr. Concentrate Mixture To 5-10ml Add Hexane 20ml Filter The Ppt Formed Dry ,Crush And Pass Through #100 2) Rotary evaporation technique Drug And Soya Lecithin Dissolved In 30 ml Of Tetrahydrofuran Stirring For 3 Hours At A Temperature Not Exceeding 40ºc Thin Film Is Formed Add n-Hexane With Stirring Precipitate Obtained Dry And Pass Through Mesh Phytosomes Formed 3) Solvent evaporation method Drug and Soya Lecithin Refluxed With 20 ml of Acetone at a Temperature 50 - 60ºc for 2 hrs. Concentrated Mixture to 5-10 ml Obtain the Precipitate Filter and Collect Phytosomes Obtained