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AquasomesMr. 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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