Three layered self assembled structures, containing the particle core composed of nanocrystalline calcium phosphate or ceramic diamond, and is covered by a polyhydroxyl oligomeric film to which biochemically active molecules are adsorbed.

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

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CONTENT
 Introduction
 Preparation
 Properties
 Characterization
 Application

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AQUASOME
 Three layered self assembled structures, containing the particle core composed of nanocrystalline calcium
phosphate or ceramic diamond, and is covered by a polyhydroxyl oligomeric film to which biochemically
active molecules are adsorbed .
 Aquasomes are spherical 60-300nm particles used for drug and antigen delivery.
 It was first developed by NIR KOSSOVSKY.

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Aquasomes are called as “ bodies of water ’’
1] Their water like properties.
2] Protect and preserve fragile biological molecules.
3] This property of maintaining conformational integrity as well as high degree of surface exposure
and in targeting of bio-active molecules like peptide and protein hormones, antigens and genes to
specific sites.
 The carbohydrate stabilize nanoparticle of ceramic are known as “Aquasomes “

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MECHANISM
1] Aquasomes protect bio-actives.
 Carbohydrate coating prevents destructive denaturing interaction between drug and solid
carriers.
2] Aquasomes maintains molecular conformation and thus shows optimum pharmacological activity.

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PREPARATION OF AQUASOME
 PREPARATION OF THE CORE
 Fabrication of the ceramic core by colloidal precipitation and sonication.
 CARBOHYDRATE COATING
 Coating by carbohydrate on the surface of ceramic cores.
 Addition of polyhydroxyl oligomer , sonication and then lyophilization.
 Coating material used are cellobiose, citrate, sucrose and trehalose.

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It involves 3 steps
 Step I - Formation of an inorganic core.
 Step II - Coating of the core with polyhydroxyl oligomer.
 Step III - Loading of the drug of choice to this assembly.

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IMMOBILIZATION OF DRUG
 The surface modified nano-crystalline cores provide the solid phase for the
subsequent non-denaturing self- assembly biochemically active molecules.

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PROPERTIES
 Aquasomes due to their size and structure stability, avoid clearance by reticuloendothelial system or by other
environmental challenges.
 Biodegradation of ceramic in-vivo achieved by monocytes and multicellular cells called osteoclast.
 Aquasomes possess large size and active surface hence can be efficiently loaded.
 Aquasomes deliver contents through combination of specific targeting, molecular shielding, and slow sustained release
process.
 Aquasomes water like properties provides a platform for preserving the conformational integrity and biochemical
stability of bio-actives.

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Characterization
 Structural analysis,
 Particle size and morphology.
 Transmission electron microscopy
 Scanning electron microscopy.
 X-ray powder diffractometry

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Application
 Aquasomes as red blood cell substitutes , haemoglobin immobilized on oligomer surface because release
of oxygen by haemoglobin is conformationally sensitive.
 Aquasomes used as vaccines for delivery of viral antigen i.e Epstein-barr and Immune deficiency virus.
 Aquasomes used for successful targetted intracellular gene therapy.
 Aquasomes for pharmaceutical delivery i.e insulin.
 Aquasomes also used for delivery of enzymes like DNAase and pigment/ dyes.

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Aquasomes for Gene Therapy

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Protein/ Surface
Macromolecule
Use Rationale
Active drug e.g. Insulin Pharmaceuticals Drug activity is conformationally specific
Polypeptide e.g. DNase Enzymes Activity fluctuates with molecular conformation
Antigenic envelope proteins
including EBV & HIV
Vaccines To be effective protective antibodies, the objective of vaccine
therapy must be triggered by conformationally target molecules
Genetic material Gene therapy Targeted intracellular delivery
Application

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References
 Vyas S.P and Khar R.K (2004), Targetted & controlled Drug Delivery,CBS Publisher & Distributor , New Delhi, 28-30.
 Kossovsky N. Gelman A., Sponsler E.D and Millet D. (1991), Nano-crystalline Epstein-Bar Vims decoys, Appl. Biomater, 2: 251-259.
 Dunitz J.D (1994), The entropic cost of bound water in crystals and biomolecules, Science,264-270.
 Cevc G., Drug delivery across the skin. Exp. Opin invest Drugs 1997:1887-1973
 Bhatia A., Kumar R., Tamoxifen in Topical liposomes, development and Characterization and in-vitro evaluation, j pharm Sci; 20047(2), 252-259.
 Jain. N. K. “Advances in controlled drug delivery system”; 317-328.
 www.pharmainfonet.com/aquasomes.

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