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PHARMACOSOMES :AN EMERGING VESICULAR DRUG
DELIVERY SYSTEM
Chandrakanta Misra. Mir Irfan Soyel, Dr. Bankim Chandra Nandy
Bengal College of Pharmaceutical Sciences & Research, B.R.B Sarani, Bdhannagar, Durgapur-713212, West Bengal.
Email:misra361@gmail.com
Drug salt was converted into the acid form to provide an activeDrug salt was converted into the acid form to provide an active
hydrogen sitefor complexation.hydrogen sitefor complexation.
Drug acid was prepared by acidification of an aqueous solutionof drugDrug acid was prepared by acidification of an aqueous solutionof drug
salt, extraction into chloroform, and subsequent recrystallization.salt, extraction into chloroform, and subsequent recrystallization.
Drug -PC co Drug salt was converted into the acid form to provide anDrug -PC co Drug salt was converted into the acid form to provide an
active hydrogen siteactive hydrogen site
mplex was prepared by associating drug acid with anmplex was prepared by associating drug acid with an
equimolarconcentration of PC.equimolarconcentration of PC.
The equimolar concentration of PC and drug acid were placed in aThe equimolar concentration of PC and drug acid were placed in a
100-mL round bottom flask and dissolved in dichloromethane.100-mL round bottom flask and dissolved in dichloromethane.
The solvent was evaporated under vacuum at 40°C in a rotaryThe solvent was evaporated under vacuum at 40°C in a rotary
vacuum evaporator.vacuum evaporator.
The pharmacosomes were collected as the dried residue and placedThe pharmacosomes were collected as the dried residue and placed
in a vacuum desiccator overnight and then subjected toin a vacuum desiccator overnight and then subjected to
characterization.characterization.
INTRODUCTION PREPARATION
IMPORTANCE
FORMULATION
CONCLUSIONS
Vesicular systems have been realized as extremely usefulcarrierVesicular systems have been realized as extremely usefulcarrier
systems in various scientific domains. Over the years, vesicularsystems in various scientific domains. Over the years, vesicular
systems have been investigated as a major drug delivery system, duesystems have been investigated as a major drug delivery system, due
to their flexibility to be tailored for varied desirable purposes. In spiteto their flexibility to be tailored for varied desirable purposes. In spite
of certain drawbacks, the vesicular delivery systems still play anof certain drawbacks, the vesicular delivery systems still play an
important role in the selective targeting, and the controlled delivery ofimportant role in the selective targeting, and the controlled delivery of
various drugsvarious drugs..
APPLICATION
 The approach has successfully improved the therapeutic performanceThe approach has successfully improved the therapeutic performance
of various drugs i.e. pindolol maleate, bupranolol hydrochloride, taxol,of various drugs i.e. pindolol maleate, bupranolol hydrochloride, taxol,
acyclovir, etc.acyclovir, etc.
 The phase transition temperature of pharmacosomes in the vesicularThe phase transition temperature of pharmacosomes in the vesicular
and Micellar state could have significant influence on their interactionand Micellar state could have significant influence on their interaction
with membranes.with membranes.
 Pharmacosomes can interact with bimembranes enabling a betterPharmacosomes can interact with bimembranes enabling a better
transfer of active ingredient. This interaction leads to change in phasetransfer of active ingredient. This interaction leads to change in phase
transition temperature of bimembranes thereby improving thetransition temperature of bimembranes thereby improving the
membrane fluidity leading to enhance permeations.membrane fluidity leading to enhance permeations.
REFERENCE
 P. Goyal et al., "Liposomal Drug Delivery Systems: ClinicalP. Goyal et al., "Liposomal Drug Delivery Systems: Clinical
Applications,"Applications," Acta Pharm.Acta Pharm. 55,55, 1–25 (2005).1–25 (2005).
 S.S. Biju et al., "Vesicular Systems: An Overview,"S.S. Biju et al., "Vesicular Systems: An Overview," Ind. Jour. Pharm.Ind. Jour. Pharm.
Sci.Sci. 68 (2), 141–153 (2006).68 (2), 141–153 (2006).
 M.O. Vaizoglu and P.P. Speiser, "Pharmacosomes—A Novel DrugM.O. Vaizoglu and P.P. Speiser, "Pharmacosomes—A Novel Drug
Delivery System,"Delivery System," Acta Pharm. Suec.Acta Pharm. Suec. 23,23, 163–172 (1986).163–172 (1986).
 Y. Jin et al., "Self-Assembled Drug Delivery Systems-Properties andY. Jin et al., "Self-Assembled Drug Delivery Systems-Properties and
In VitroIn Vitro ––In VivoIn Vivo Behaviour of Acyclovir Self-AssembledBehaviour of Acyclovir Self-Assembled
Nanoparticles (san),"Nanoparticles (san)," Int. J. Pharm.Int. J. Pharm. 309309 (1–2), 199–207 (2006).(1–2), 199–207 (2006).
 Pharmacosomes are the colloidal dispersions of drugs covalentlyPharmacosomes are the colloidal dispersions of drugs covalently
bound to lipids, and may exist as ultrafine vesicular, micellar, orbound to lipids, and may exist as ultrafine vesicular, micellar, or
hexagonal aggregates, depending on the chemical structure ofhexagonal aggregates, depending on the chemical structure of
drug-lipid complex.drug-lipid complex.
 Pharmacosomes are amphiphilic phospholipid complexes of drugsPharmacosomes are amphiphilic phospholipid complexes of drugs
bearing active hydrogen that bind to phospholipids.bearing active hydrogen that bind to phospholipids.
 Pharmacosomes impart better biopharmaceutical properties to thePharmacosomes impart better biopharmaceutical properties to the
drug, resulting in improved bioavailability.drug, resulting in improved bioavailability.
 Pharmacosomes have been prepared for various non-steroidal anti-Pharmacosomes have been prepared for various non-steroidal anti-
inflammatory drugs, proteins, cardiovascular and antineoplasticinflammatory drugs, proteins, cardiovascular and antineoplastic
drugs.drugs.
 Developing the pharmacosomes of the drugs has been found toDeveloping the pharmacosomes of the drugs has been found to
improve the absorption and minimize the gastrointestinal toxicity.improve the absorption and minimize the gastrointestinal toxicity.
Two methods have been used to prepare vesicles:Two methods have been used to prepare vesicles:
1. The hand-shaking method1. The hand-shaking method
2. The ether-injection method2. The ether-injection method
In the hand-shaking method, the dried film of the drug–lipid complexIn the hand-shaking method, the dried film of the drug–lipid complex
(with or without egg lecithin) is deposited in a round-bottom flask and(with or without egg lecithin) is deposited in a round-bottom flask and
upon hydration with aqueous medium, readily gives a vesicularupon hydration with aqueous medium, readily gives a vesicular
suspension.suspension.
In the ether-injection method, an organic solution of the drug–lipidIn the ether-injection method, an organic solution of the drug–lipid
complex is injected slowly into the hot aqueous medium, wherein thecomplex is injected slowly into the hot aqueous medium, wherein the
vesicles are readily formed.vesicles are readily formed.
Pharamcosomes have some importance in escaping the tedious steps ofPharamcosomes have some importance in escaping the tedious steps of
removing the free unentrapped drug from the formulation.removing the free unentrapped drug from the formulation.
Pharmacosomes provide an efficient method for delivery of drug directlyPharmacosomes provide an efficient method for delivery of drug directly
to the site of infection, leading to reduction of drug toxicity with no adverseto the site of infection, leading to reduction of drug toxicity with no adverse
effects and also reduces the cost of therapy by improved bioavailability ofeffects and also reduces the cost of therapy by improved bioavailability of
medication, especially in case of poorly soluble drugs.medication, especially in case of poorly soluble drugs.
. Pharmacosomes are suitable for incorporating both hydrophilic andPharmacosomes are suitable for incorporating both hydrophilic and
lipophilic drugs.lipophilic drugs.
Entrapment efficiency is not only high but predetermined, because drugEntrapment efficiency is not only high but predetermined, because drug
itself in conjugation with lipids forms vesicles.itself in conjugation with lipids forms vesicles.
There is no need of following the tedious, time-consuming step forThere is no need of following the tedious, time-consuming step for
removing the free, unentrapped drug from the formulation.removing the free, unentrapped drug from the formulation.
Since the drug is covalently linked, loss due to leakage of drug, does notSince the drug is covalently linked, loss due to leakage of drug, does not
take place.take place.
No problem of drug incorporation.No problem of drug incorporation.
Encaptured volume and drug-bilayer interactions do not influenceEncaptured volume and drug-bilayer interactions do not influence
entrapment efficiency, in case of pharmacosomes.entrapment efficiency, in case of pharmacosomes.
Following absorption, their degradation velocity into active drug moleculeFollowing absorption, their degradation velocity into active drug molecule
depends to a great extent on the size and functional groups of drugdepends to a great extent on the size and functional groups of drug
molecule, the chain length of the lipids, and the spacer.molecule, the chain length of the lipids, and the spacer.
MARKETED PRODUCTS
EVALUATION PARAMETERS
 SolubilitySolubility
 Drug contentDrug content
 Entrapment efficiencyEntrapment efficiency
 Dissolution studyDissolution study
 Scanning electron microscopy (SEM)Scanning electron microscopy (SEM)
 Differential scanning calorimetry (DSC)Differential scanning calorimetry (DSC)
 X-ray powder diffraction (XRPD)X-ray powder diffraction (XRPD)
Figure 1 .Mechanism of pharmacosomesFigure 1 .Mechanism of pharmacosomes
Table .1.effects of drug with pharmacosomesTable .1.effects of drug with pharmacosomes
EFFECT OF DRUGS WITH
PHARMACOSOMES
Two prerequisites of pharmacosomesTwo prerequisites of pharmacosomes
Figure 2.Drugs with pharmacosomeFigure 2.Drugs with pharmacosome
Human Iron Dextran is manufactured as low molecular weight IronHuman Iron Dextran is manufactured as low molecular weight Iron
Dextran by Pharmacosmos.Dextran by Pharmacosmos.
Veterinary Iron Dextran is used as iron supplement forVeterinary Iron Dextran is used as iron supplement for
prevention of iron deficiency anemia in pigletsprevention of iron deficiency anemia in piglets
Dextran polymers from Pharmacosmos are manufacturedDextran polymers from Pharmacosmos are manufactured
according to Good Manufacturing Practice (GMP). Ouraccording to Good Manufacturing Practice (GMP). Our
Dextran products include clinical and reagent grade DextranDextran products include clinical and reagent grade Dextran
and GPC Standards for GPC chromatography.and GPC Standards for GPC chromatography.
LIMITATIONS OF
PHARMACOSOMES
·· Synthesis of a compound depends upon itsSynthesis of a compound depends upon its
ampiphilic nature.ampiphilic nature.
· Required surface and bulk interaction of· Required surface and bulk interaction of
lipids with drugs.lipids with drugs.
·· Required covalent bonding to protect theRequired covalent bonding to protect the
leakage of drugs.leakage of drugs.
· Pharmacosomes, on storage, undergo fusion· Pharmacosomes, on storage, undergo fusion
and aggregation, as well chemical hydrolysis.and aggregation, as well chemical hydrolysis.

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pharmacosomes poster

  • 1. PHARMACOSOMES :AN EMERGING VESICULAR DRUG DELIVERY SYSTEM Chandrakanta Misra. Mir Irfan Soyel, Dr. Bankim Chandra Nandy Bengal College of Pharmaceutical Sciences & Research, B.R.B Sarani, Bdhannagar, Durgapur-713212, West Bengal. Email:misra361@gmail.com Drug salt was converted into the acid form to provide an activeDrug salt was converted into the acid form to provide an active hydrogen sitefor complexation.hydrogen sitefor complexation. Drug acid was prepared by acidification of an aqueous solutionof drugDrug acid was prepared by acidification of an aqueous solutionof drug salt, extraction into chloroform, and subsequent recrystallization.salt, extraction into chloroform, and subsequent recrystallization. Drug -PC co Drug salt was converted into the acid form to provide anDrug -PC co Drug salt was converted into the acid form to provide an active hydrogen siteactive hydrogen site mplex was prepared by associating drug acid with anmplex was prepared by associating drug acid with an equimolarconcentration of PC.equimolarconcentration of PC. The equimolar concentration of PC and drug acid were placed in aThe equimolar concentration of PC and drug acid were placed in a 100-mL round bottom flask and dissolved in dichloromethane.100-mL round bottom flask and dissolved in dichloromethane. The solvent was evaporated under vacuum at 40°C in a rotaryThe solvent was evaporated under vacuum at 40°C in a rotary vacuum evaporator.vacuum evaporator. The pharmacosomes were collected as the dried residue and placedThe pharmacosomes were collected as the dried residue and placed in a vacuum desiccator overnight and then subjected toin a vacuum desiccator overnight and then subjected to characterization.characterization. INTRODUCTION PREPARATION IMPORTANCE FORMULATION CONCLUSIONS Vesicular systems have been realized as extremely usefulcarrierVesicular systems have been realized as extremely usefulcarrier systems in various scientific domains. Over the years, vesicularsystems in various scientific domains. Over the years, vesicular systems have been investigated as a major drug delivery system, duesystems have been investigated as a major drug delivery system, due to their flexibility to be tailored for varied desirable purposes. In spiteto their flexibility to be tailored for varied desirable purposes. In spite of certain drawbacks, the vesicular delivery systems still play anof certain drawbacks, the vesicular delivery systems still play an important role in the selective targeting, and the controlled delivery ofimportant role in the selective targeting, and the controlled delivery of various drugsvarious drugs.. APPLICATION  The approach has successfully improved the therapeutic performanceThe approach has successfully improved the therapeutic performance of various drugs i.e. pindolol maleate, bupranolol hydrochloride, taxol,of various drugs i.e. pindolol maleate, bupranolol hydrochloride, taxol, acyclovir, etc.acyclovir, etc.  The phase transition temperature of pharmacosomes in the vesicularThe phase transition temperature of pharmacosomes in the vesicular and Micellar state could have significant influence on their interactionand Micellar state could have significant influence on their interaction with membranes.with membranes.  Pharmacosomes can interact with bimembranes enabling a betterPharmacosomes can interact with bimembranes enabling a better transfer of active ingredient. This interaction leads to change in phasetransfer of active ingredient. This interaction leads to change in phase transition temperature of bimembranes thereby improving thetransition temperature of bimembranes thereby improving the membrane fluidity leading to enhance permeations.membrane fluidity leading to enhance permeations. REFERENCE  P. Goyal et al., "Liposomal Drug Delivery Systems: ClinicalP. Goyal et al., "Liposomal Drug Delivery Systems: Clinical Applications,"Applications," Acta Pharm.Acta Pharm. 55,55, 1–25 (2005).1–25 (2005).  S.S. Biju et al., "Vesicular Systems: An Overview,"S.S. Biju et al., "Vesicular Systems: An Overview," Ind. Jour. Pharm.Ind. Jour. Pharm. Sci.Sci. 68 (2), 141–153 (2006).68 (2), 141–153 (2006).  M.O. Vaizoglu and P.P. Speiser, "Pharmacosomes—A Novel DrugM.O. Vaizoglu and P.P. Speiser, "Pharmacosomes—A Novel Drug Delivery System,"Delivery System," Acta Pharm. Suec.Acta Pharm. Suec. 23,23, 163–172 (1986).163–172 (1986).  Y. Jin et al., "Self-Assembled Drug Delivery Systems-Properties andY. Jin et al., "Self-Assembled Drug Delivery Systems-Properties and In VitroIn Vitro ––In VivoIn Vivo Behaviour of Acyclovir Self-AssembledBehaviour of Acyclovir Self-Assembled Nanoparticles (san),"Nanoparticles (san)," Int. J. Pharm.Int. J. Pharm. 309309 (1–2), 199–207 (2006).(1–2), 199–207 (2006).  Pharmacosomes are the colloidal dispersions of drugs covalentlyPharmacosomes are the colloidal dispersions of drugs covalently bound to lipids, and may exist as ultrafine vesicular, micellar, orbound to lipids, and may exist as ultrafine vesicular, micellar, or hexagonal aggregates, depending on the chemical structure ofhexagonal aggregates, depending on the chemical structure of drug-lipid complex.drug-lipid complex.  Pharmacosomes are amphiphilic phospholipid complexes of drugsPharmacosomes are amphiphilic phospholipid complexes of drugs bearing active hydrogen that bind to phospholipids.bearing active hydrogen that bind to phospholipids.  Pharmacosomes impart better biopharmaceutical properties to thePharmacosomes impart better biopharmaceutical properties to the drug, resulting in improved bioavailability.drug, resulting in improved bioavailability.  Pharmacosomes have been prepared for various non-steroidal anti-Pharmacosomes have been prepared for various non-steroidal anti- inflammatory drugs, proteins, cardiovascular and antineoplasticinflammatory drugs, proteins, cardiovascular and antineoplastic drugs.drugs.  Developing the pharmacosomes of the drugs has been found toDeveloping the pharmacosomes of the drugs has been found to improve the absorption and minimize the gastrointestinal toxicity.improve the absorption and minimize the gastrointestinal toxicity. Two methods have been used to prepare vesicles:Two methods have been used to prepare vesicles: 1. The hand-shaking method1. The hand-shaking method 2. The ether-injection method2. The ether-injection method In the hand-shaking method, the dried film of the drug–lipid complexIn the hand-shaking method, the dried film of the drug–lipid complex (with or without egg lecithin) is deposited in a round-bottom flask and(with or without egg lecithin) is deposited in a round-bottom flask and upon hydration with aqueous medium, readily gives a vesicularupon hydration with aqueous medium, readily gives a vesicular suspension.suspension. In the ether-injection method, an organic solution of the drug–lipidIn the ether-injection method, an organic solution of the drug–lipid complex is injected slowly into the hot aqueous medium, wherein thecomplex is injected slowly into the hot aqueous medium, wherein the vesicles are readily formed.vesicles are readily formed. Pharamcosomes have some importance in escaping the tedious steps ofPharamcosomes have some importance in escaping the tedious steps of removing the free unentrapped drug from the formulation.removing the free unentrapped drug from the formulation. Pharmacosomes provide an efficient method for delivery of drug directlyPharmacosomes provide an efficient method for delivery of drug directly to the site of infection, leading to reduction of drug toxicity with no adverseto the site of infection, leading to reduction of drug toxicity with no adverse effects and also reduces the cost of therapy by improved bioavailability ofeffects and also reduces the cost of therapy by improved bioavailability of medication, especially in case of poorly soluble drugs.medication, especially in case of poorly soluble drugs. . Pharmacosomes are suitable for incorporating both hydrophilic andPharmacosomes are suitable for incorporating both hydrophilic and lipophilic drugs.lipophilic drugs. Entrapment efficiency is not only high but predetermined, because drugEntrapment efficiency is not only high but predetermined, because drug itself in conjugation with lipids forms vesicles.itself in conjugation with lipids forms vesicles. There is no need of following the tedious, time-consuming step forThere is no need of following the tedious, time-consuming step for removing the free, unentrapped drug from the formulation.removing the free, unentrapped drug from the formulation. Since the drug is covalently linked, loss due to leakage of drug, does notSince the drug is covalently linked, loss due to leakage of drug, does not take place.take place. No problem of drug incorporation.No problem of drug incorporation. Encaptured volume and drug-bilayer interactions do not influenceEncaptured volume and drug-bilayer interactions do not influence entrapment efficiency, in case of pharmacosomes.entrapment efficiency, in case of pharmacosomes. Following absorption, their degradation velocity into active drug moleculeFollowing absorption, their degradation velocity into active drug molecule depends to a great extent on the size and functional groups of drugdepends to a great extent on the size and functional groups of drug molecule, the chain length of the lipids, and the spacer.molecule, the chain length of the lipids, and the spacer. MARKETED PRODUCTS EVALUATION PARAMETERS  SolubilitySolubility  Drug contentDrug content  Entrapment efficiencyEntrapment efficiency  Dissolution studyDissolution study  Scanning electron microscopy (SEM)Scanning electron microscopy (SEM)  Differential scanning calorimetry (DSC)Differential scanning calorimetry (DSC)  X-ray powder diffraction (XRPD)X-ray powder diffraction (XRPD) Figure 1 .Mechanism of pharmacosomesFigure 1 .Mechanism of pharmacosomes Table .1.effects of drug with pharmacosomesTable .1.effects of drug with pharmacosomes EFFECT OF DRUGS WITH PHARMACOSOMES Two prerequisites of pharmacosomesTwo prerequisites of pharmacosomes Figure 2.Drugs with pharmacosomeFigure 2.Drugs with pharmacosome Human Iron Dextran is manufactured as low molecular weight IronHuman Iron Dextran is manufactured as low molecular weight Iron Dextran by Pharmacosmos.Dextran by Pharmacosmos. Veterinary Iron Dextran is used as iron supplement forVeterinary Iron Dextran is used as iron supplement for prevention of iron deficiency anemia in pigletsprevention of iron deficiency anemia in piglets Dextran polymers from Pharmacosmos are manufacturedDextran polymers from Pharmacosmos are manufactured according to Good Manufacturing Practice (GMP). Ouraccording to Good Manufacturing Practice (GMP). Our Dextran products include clinical and reagent grade DextranDextran products include clinical and reagent grade Dextran and GPC Standards for GPC chromatography.and GPC Standards for GPC chromatography. LIMITATIONS OF PHARMACOSOMES ·· Synthesis of a compound depends upon itsSynthesis of a compound depends upon its ampiphilic nature.ampiphilic nature. · Required surface and bulk interaction of· Required surface and bulk interaction of lipids with drugs.lipids with drugs. ·· Required covalent bonding to protect theRequired covalent bonding to protect the leakage of drugs.leakage of drugs. · Pharmacosomes, on storage, undergo fusion· Pharmacosomes, on storage, undergo fusion and aggregation, as well chemical hydrolysis.and aggregation, as well chemical hydrolysis.