aquasomes, M.Pharm, 2nd sem

1. BY: SHANU B. SAHU
Lectuer
Sonekar College of Health
Sciences, D.pharm, Bailwada,
Nagpur

2. *
*Introduction
*Properties
*Formulation of aquasomes
*Method of preparation
*Characterization
*Application
*Aquasomes for insulin delivery
*Aquasomes for gene therapy

3. *
Aquasome :
*It is 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 absorbed.

4. *These are spherical 60-300nm particles used
for drug and antigen delivery.
*It was first developed by NIR KOSSOVSKY in
1995.
*Aquasome consist of solid crystalline core,
carbohydrate coat and active drug.
*The solid core provide structural stability, the
carbohydrate act as a natural stabliser protect
against dehydration and stablizes the
biochemically active molecules.
*Aquasomes offer an attractive mode of delivery
for drugs which having the problems such as
route of delivery, physical as well as chemical
stability, poor bio-availability and potent side
effect.

5. *AQUASOMES ARE CALLED “BODIES OF WATER”
*Their water like properties protect and preserve fragile
biological molecules.
*This has property of maintaining confirmational integrity
as well as high degree of surface exposure and in
targeting of bio-active molecules like peptide and protein
hormones, antigens and gene to specific site.
*The carbohydrate stablize nanoparticle of ceramic are
known as “aquasomes”

6. *PROPERTIES:
*Aquasomes water like properties provide a platform for
preserving the confirmational integrity and biochemical
stability of bio-actives.
*Aquasomes due to their size and structural stability,
avoid clearance by other environmental challenges.
*Aquasomes possess large size and active surface hence
can be efficiently loaded with substantial amount of
agents through ionic, non covalent bonds, van der waals
forces and entropic forces as solid particles dispersed in
aqueous environmental, they exhibit physical properties
of colloids.

7. *FORMULATION OF AQUASOMES:
Principal of self assembly of macromolecules:
*These three layered structure are self assembled by non-
covalent bond.
*Principal of “self assembly of macromolecules” is
governed by three physicochemical process i.e.
1. Interaction between charged group.
2. Hydrogen bonding and dehydration effects.
3. Structural activity

8. 1.Interaction between charged group:
*The interaction of charged group facilitates long range approach of
self assembly sub units charge group also plays a role in stablizing
tertiary structure of folded proteins.
2.Hydrogen bonding and dehydration effects:
*Hydrogen bond helps in base pair matching and stablization
secondary protein structure such as alpha helicales and beta sheets.
In case of hydrophilic molecules due the dehydration effect can self
assembled.
3. Structural stability:
Structural stability of protein in biological environment determined by
interaction between charged group and hydrogen bonds largely
external to molecules and by van der waals, largely internal to
molecules experienced by hydrophobic molecules, responsible for
hardness and softness of molecules and maintain of internal secondary
structures provides sufficient softness, allows maintainance of
confirmation during self assembly.

9. *METHOD OF PREPARATION:
*By using principle of self assembly aquasome can be
prepared by three method:
1. Preparation of core
2. Coating of core
3. Immobilization of drug molecules

10. 1. Preparation of core
*This stage mainly depends on the
• selection of material for core
• its physical, chemical properties
*This can be fabricated by
• Sonication
• Colloidal precipitation
• Plasma condensation
*For the core material ceramic material widely used as they are
structurally most material to be known.
*As they are being crystalline their bulk properties is preserved.
*Commonly used ceramic core are diamond and calcium phosphate.
*Example: synthesis of nano crystalline tin oxide core material.

11. Example *Synthesis of nanocrystalline tin oxide
core material
• This can be prepared by
-Direct current reactive
• 3inch diameter of highly purified tin is sputtered in
• High pressure gas mixture of argon and oxygen
• The ultra fine particle form in gas phase are collect
on copper tube at 700K with liquid nitrogen

12. 2.
• Addition of poly hydroxyl oligomer,
• To a dispersion of core in ultra pure water.
• Lyophilization (to promote the absorption of
carbohydrate on the surface of ceramic core)
• Excess of carbohydrate is removed by stir cell
ultrafiltration.
Process
generally
entail

13. 3. Immobilization of drug
* The surface modified nano crystalline core provide the
solid phase for subsequent non-denaturing self assembly
for a broad range of biologically active molecule
* Drug can be loaded by partial adsorption.
* Commonly used coating material
-Cellobiose
-Citrate
-Sucrose
-Pyridoxal-5-phosphate

14. *
Size distribution
• For morphological characteristic and size distribution
analysis
• i.e. scanning electron microscopy(SEM) and
• Transmission electron microscopy(TEM) are generally used.
• Mean particle size and zeta potential of the particle can
also be determine by using photo correlation spectroscopy.
Structural analysis
• FT-IR spectroscopy
• For crystallinity - the prepared ceramic core can be
analyzed for its crystalline and amorphous behavior using
X-ray diffraction

15. *
*Aquasomes are RBCs substitutes, haemoglobin immobilized on
oligomer surface because release of oxygen by haemoglobin is
confirmationally sensitive.
*Aquasomes used as vaccines for delivery of vital antigen
i.e. delivery of Epstein-Barr virus(EBV) and
Human Immune Deficiency Virus(HIV)
*They are used for successful targeted intracellular gene
therapy.
*Delivery of enzymes like, DNAase and pigment dyes.
*As oxygen carrier

16. *
Colloidal
precipitation
and sonication
of solution
• Na2HPO4 and CaCl2
• Prepare calcium phosphate dihydrate core.
• Core further coated with coating material
like cellobiose, citrate, pyridoxal-5-
phosphate, under sonication
• Drug is loaded to these coated nano
particle/aquasome.

17. *