Pharmacosomes are the 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.

1. Mr. Sagar Kishor Savale
[Department of Pharmaceutics]
avengersagar16@gmail.com
2015-2016
Department of Pharmacy (Pharmaceutics) | Sagar savale

2. CONTENTS
 Introduction
 Importance
 Formulation
 Evaluation
 Applications
 Conclusion
 References
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3. INTRODUCTION
 Pharmacosomes are the 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 better biopharmaceutical properties to the drug, resulting in
improved bioavailability.
 Pharmacosomes have been prepared for various non-steroidal anti-inflammatory 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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4. Pharmacosome
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5.  In pharmacosomes, membrane fluidity depends upon the phase transition temperature of
the drug lipid complex, but it does not affect release rate since the drug is covalently
bound.
 The drug is released from pharmacosome by hydrolysis (including enzymatic).
 The physicochemical stability of the pharmacosome depends upon the physicochemical
properties of the drug-lipid complex.
 Following absorption, their degradation velocity into active drug molecule depends to a
great extent on the size and functional groups of drug molecule, the chain length of the
lipids, and the spacer.
 They can be given orally, topically, extra-or intravascularly.
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6. IMPORTANCE
 Pharamcosomes have some importance in escaping the tedious steps of removing the free
unentrapped drug from the formulation
 Pharmacosomes provide an efficient method for delivery of drug directly to the site of
infection, leading to reduction of drug toxicity with no adverse effects and also reduces the
cost of therapy by improved bioavailability of medication, especially in case of poorly
soluble drugs.
 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.
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7.  There is no need of following the tedious, time-consuming step for removing the
free, unentrapped drug from the formulation.
 Since the drug is covalently linked, loss due to leakage of drug, does not take place.
 No problem of drug incorporation
 Encaptured volume and drug-bilayer interactions do not influence entrapment
efficiency, in case of pharmacosomes.
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8. 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 (with or
without egg lecithin) 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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9. EVALUATION OF PHARMACOSOMES
 Solubility
 Drug content
 Entrapment efficiency
 Dissolution study
 Scanning electron microscopy (SEM)
 Differential scanning calorimetry (DSC)
 X-ray powder diffraction (XRPD)
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10. APPLICATIONS
 The approach has successfully improved the therapeutic performance of various
drugs i.e. pindolol maleate, bupranolol hydrochloride, taxol, acyclovir, etc.
 The phase transition temperature of pharmacosomes in the vesicular and Micellar
state could have significant influence on their interaction with membranes.
 Pharmacosomes can interact with bimembranes enabling a better transfer of active
ingredient. This interaction leads to change in phase transition temperature of
bimembranes thereby improving the membrane fluidity leading to enhance
permeations.
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11.  Amphiphilic Prodrug
 Pharmacosomes of Aceclophenac
 Pharmacosomes of Diclophenac
 Pharmacosomes of Didnosine
 Pharmacosomes of Acyclovir
APPLICATIONS
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12. REFERENCES
 Y. Jin et al., "Self-Assembled Drug Delivery Systems-Properties and In Vitro –In Vivo Behaviour of Acyclovir Self-
Assembled Nanoparticles (san)," Int. J. Pharm. 309 (1–2), 199–207 (2006).
 P. Goyal et al., "Liposomal Drug Delivery Systems: Clinical Applications," Acta Pharm. 55, 1–25 (2005).
 H.A. Lieberman, M.M. Rieger, and G.S. Banker, Pharmaceutical Dosage Forms: Disperse Systems (Informa
Healthcare, London, England, 1998), p. 163.
 S.S. Biju et al., "Vesicular Systems: An Overview," Ind. Jour. Pharm. Sci. 68 (2), 141–153 (2006).
 M.O. Vaizoglu and P.P. Speiser, "Pharmacosomes—A Novel Drug Delivery System," Acta Pharm. Suec. 23, 163–172
(1986).
 A. Singh and R. Jain, "Targeted Vesicular Constructs For Cytoprotection and Treatment of H. Pylori Infections," US
Patent 6576,625 (2003).
 I.P. Kaur and M. Kanwar, "Ocular Preparations: The Formulation Approach," Drug Dev. Ind. Pharm. 28 (5), 473–493
(2002).
 F. Volkering et al., "Influence of Nonionic Surfactants on Bioavailability and
 Biodegradation of Polycyclic Aromatic Hydrocarbons," App. Environ. Micro. 61 (5), 1699–170 (1995).
 A. Steve, "Lipophilic Drug Derivatives for Use in Liposomes," US Patent 5534499 (1996).
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