This document discusses pharmacosomes, which are colloidal dispersions of drugs covalently bound to lipids. Pharmacosomes can improve drug bioavailability and absorption while minimizing gastrointestinal toxicity. They are prepared using methods like hand shaking or ether injection to form vesicles. Pharmacosomes act by interacting with biomembranes to enhance permeability. They have advantages like high entrapment efficiency and stability. Various drugs have been formulated as pharmacosomes for targeted delivery and improved therapeutic effects.

1. PHARMACOSOMES
PREPARED BY :
SAURABH SHARMA
0001PY18MP14
SCHOOL OF PHARMACEUTICAL SCIENCES
RAJIV GANDHI PROUDYOGIKI VISHWAVIDYALA, BHOPAL
Guided by :
Dr. SUMAN RAMTEKE
(Asst. Prof)

2. CONTENTS
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INTRODUCTION
ADVANTAGE
ACTION OF PHARMACOSOME
COMPONENTS OF PHARMACOSOME
METHODS OF PREPARATION
FORMULATION
APPLICATION
REFERENCES

3. INTRODUCTION
• Pharmacosomes are colloidal dispersions of drugs covalently
bound to lipids, and may exist as ultrafine vesicular, micellar, or
hexagonal aggregates, depending on the chemical structure of
drug-lipid complex.
• Pharmacosomes are amphiphilic phospholipid complexes of
drugs bearing active hydrogen that bind to phospholipids.
• Pharmacosomes impart improved bioavailability.
• As the system is formed by binding the drug (pharmakon) to
carrier (soma), they are termed as pharmacosomes.
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4. • Pharmacosomes have been prepared for various non-steroidal
antiinflammatory drugs, proteins, cardiovascular and
antineoplastic drugs.
• Developing the pharmacosomes of the drugs has been found to
improve the absorption and minimize the gastrointestinal
toxicity.
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5. ADVANTAGE
• Pharmacosomes have importance in escaping the tedious steps of
removing the free unentrapped drug from the formulation.
• Pharmacosomes are suitable for incorporating both hydrophilic and
lipophilic drugs.
• Entrapment efficiency is not only high but predetermined, because
drug itself in conjugation with lipids forms vesicles.
• Since the drug is covalently linked, loss due to leakage of drug, does
not take place.
• Encaptured volume and drug-bilayer interactions do not influence
entrapment efficiency, in case of pharmacosomes.
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6. • They can be given orally, topically, extra-or intravascularly.
• The stability of the pharmacosome depends upon the
physicochemical properties of the drug-lipid complex.
• No problem of drug incorporation.
• Developing the pharmacosomes of the drugs has been found to
improve the absorption and minimize the gastrointestinal toxicity.
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7. ACTION OF PHARMACOSOMES
• Pharmacosomes can act with biomembranes enabling a better
transfer of active ingredient. This interaction leads to change in
phase transition temperature of biomembranes thereby
improving the membrane fluidity leading to enhance
permeation.
• Pharmacosome have greater degree of selectivity for action on
specific target cells.
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8. COMPONENTS OF PHARMACOSOMES
• Drug:
Any drug possessing an active hydrogen atom (-COOH, -OH, -NH2 etc.)
can be esterified to the lipid, with or without spacer chain, resulting in
amphiphilic complexes. These synthesized amphiphilic complexes
(pharmacosome) facilitate membrane, tissue, or cell wall transfer in the
organism. Eg. Rosuvastatin, Etodolac
• Solvent:
An analytical grade organic solvent is required for the preparation of
pharmacosomes. It must be of high purity and volatile in nature. Lipid and
the drug must be dissolved in the selected solvent either simply by its
addition or by refluxing.
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9. • Lipid:
Lipid or lecithin or phosphatidylcholine is the principal
molecular building block of cell membranes. It is miscible both in
water and in an oil/lipid environment and absorbed well orally.
Phospholipids are small lipid molecules in which the glycerol is
bonded only to two fatty acids, instead of three as in triglycerides,
with the remaining site occupied by a phosphate group.
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10. METHODS OF PREPARATION
• Two methods have been used to prepare vesicles:
1. The hand-shaking method
2. The ether-injection method
• In the hand-shaking method, the dried film of the drug–lipid complex
is deposited in a round-bottom flask and upon hydration with
aqueous medium, readily gives a vesicular suspension.
• In the ether-injection method, an organic solution of the drug–lipid
complex is injected slowly into the hot aqueous medium, wherein
the vesicles are readily formed.
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11. 11HAND SHAKING METHOD

12. 12
ETHER INJECTION METHOD

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14. 14

15. CHARATERIZATION OF PHARMACOSOMES
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Characteristics Test or instrument used
Solubility Shake flask method
Drug content spectrophotometrically
Surface morphology Scanning electron microscope
Thermal behaviour DSC
Crystalline state XRD
Dissolution study Dissolution apparatus at 100 rpm at
37 ͦC
Vescicle diameter Freeze fractured microscopy or light
microscope

16. APPLICATION
• Targeted Drug delivery.
• Delivery of Peptide drug.
• Development of Novel ophthalmic DDS.
• Pharmacosomes elicit greater shelf stability.
• The approach has successfully improved the therapeutic
performance of various drugs i.e. pindolol maleate.
• The phase transition temperature of pharmacosomes in the
vesicular and Micellar state could have significant influence
on their interaction with membranes.
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17. REFERENCES
• Vyas .S.P “Theory and practical in novel drug delivery system” First
edition 2009, published by CBS publisher and distributors,
• http://www.thepharmajournal.com/vol3Issue10/Issue_dec_2014/20.
1.pdf
• https://www.tandfonline.com/loi/iedd20
• https://www.hindawi.com/journals/isrn/2013/348186/
• P. Goyal et al., "Liposomal Drug Delivery Systems: Clinical Applications
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18. THANK YOU
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