Aquasomes are nanoparticulate carrier systems that protect and deliver fragile biological molecules like proteins, peptides, and genes. They are self-assembled structures with a solid ceramic core coated with carbohydrates. This seminar discusses the properties, preparation, and characterization of aquasomes. Aquasomes are prepared via a three-step process - ceramic core fabrication, carbohydrate coating, and drug immobilization using self-assembly. They can effectively deliver vaccines, hemoglobin, enzymes, and other drugs while preserving molecular integrity. Some potential applications mentioned include insulin delivery and an oral enzyme delivery system.

1. DAYANANDA SAGAR UNIVERSITY
DEPARTMENT OF PHARMACEUTICS
SEMINAR ON
AQUASOMES
PRESENTED BY SUBMITTED TO
Rajdulari Dr. Wilson
M. PHARMA 2nd sem HOD, Pharmaceutics

2. REFERENCE

3. INTRODUCTION
• Aquasomes are first discovered by Nir Kossovsky IN 1995.
• These are nanoparticulate carrier systems with three layered self assembled
structures
• These comprises of central solid nanocrystalline core coated with polyhydroxy
oligomers onto which biochemically active molecules are adsorbed.

4. • Aquasomes are also called as “bodies of water” and their water like properties
protect and preserve fragile biological molecules.
• This property of maintaining conformational integrity as well as high degree of
surface exposure made it as a successful carrier system for bioactive molecules like
peptide, protein, hormones, antigens and genes to specific sites, that is for targeting.

5. PROPERTIES
• Aquasomes water like properties provides a platform for preserving the
conformational Integrity and bio chemical stability of bio-actives.
• Aquasomes due to their size and structure stability, avoid clearance by
reticuloendothelial system or degradation by other environmental challenges
• Aquasomes possess large size and active surface hence can be efficiently loaded
with substantial amounts of agents through ionic, non covalent bonds, van der
waals forces and entropic forces. As solid particles dispersed in aqueous
environment, they exhibit physical properties of colloids.
• In general these aquasomes are assemblies of simple polymers, complex lipid
mixtures with diameter ranging between 30 to 500 nm.

6. OBJECTIVES
• The main objective of preparing aquasomes is to protect bio-actives.
• Various other carrier system are there like prodrugs and liposomes but they have
disadvantage that they are prone to undergo destructive interactions between
drug and carrier, so in that condition in aquasomes can be termed as a important
carrier.
• In aquasomes carbohydrate coating prevents destructive denaturing interaction
between drug and solid carriers.
• Aquasomes maintains molecular confirmation and optimum pharmacological
activity.

7. MATERIAL USED
• Albumin, gelatin or acrylates are polymers used and diamond particles, brushite,
and tin oxide core are ceramics used in preparation of aquasomes.
• Ceramic materials are mostly used because ceramics are structurally the most
regular materials known for core, being crystalline high degree of order ensures-
 Bulk properties of ceramic will be preserved because any surface modification
will have only limited effect on nature of atoms below surface layer.
The surface will exhibit high level of surface energy that will favor the binding of
polyhydroxy oligomer surface film.
Within a very less time the freshly prepared particles possess good property of
adsorbing molecules

8. METHOD OF PREPARATION OF AQUASOMES
• By using the principle of self assembly, the aquasomes are prepared
in three steps i.e.,
1. preparation of core,
2. coating of core, and
3. immobilization of drug molecule.

9. Principle of self assembly
• In aqueous biological environments , the assembly of macro molecule Is governed by
three process.
(1) Interaction between charged group.
(2) Hydrogen bonding and dehydration effect.
(3) structural stability.
1) Interaction between charged group
• Most of the Biological product are charged due to intrinsic chemical group or absorbed ion from the
biological environment.
• Interaction of charged group such as amino, carbonyl, sulphate, phosphate groups facilitate the long
range approach of self assembling sub units.
• Charged groups also play role in stabilizing tertiary structure of folded proteins.
• Example of ion pairs -carboxylate /phosphate group bound to ionized arginine / lysine side chain of
protein.

10. 2)Hydrogen bonding and dehydration effect.
• Hydrogen bond are formed between hydrogen atom attached to an electronegative donor
atom (Ex oxygen ,Nitrogen,) and an electronegative or basic acceptor (Ex carbonyl oxygen).
• Hydrogen bond help in base pair matching and stabilization of Secondary protein structure.
• Molecule that form hydrogen bonds are hydrophilic and these molecules confer significant
degree of organization to the surrounding water molecules.
3) structural stability.
• The structural stability of Protein in the biological environment is determined by the
interaction between charged groups and hydrogen bond largely external to the molecule and
Vander walls forces largely internal to the molecule.
• Vander walls forces are largely responsible for the hardness or softness of the molecule. The
Vander walls interaction among hydrophilic side chains promotes stability of compact helical
structures.

11. PREPARATION OF CORE
• Calcium phosphate and diamond are the two most commonly used ceramic cores. This method
involves the fabrication of a ceramic core, and the procedure depends upon the materials
selected.
 Synthesis of nanocrystalline tin oxide core ceramic
It can be synthesized by direct current reactive magnetron sputtering. In a high pressure gas mixture
of argon and oxygen, a 3 inches diameter target of high purity tin is sputtered. The ultrafine
particles formed in the gas phase are then collected on copper tubes cooled to 770K with flowing
nitrogen.
Self assembled nanocrystalline brushite (calcium phosphate dihydrate)
These can be prepared by colloidal precipitation and sonication by reacting solution of disodium
hydrogen phosphate and calcium chloride.

12. COATING OF THE CORE
• The commonly used coating materials are cellobiose, citrate, pyridoxal-5-
phosphate and sucrose.
• It is the second step in which ceramic cores are coated with carbohydrate.
• The carbohydrate which we mainly use can be polyhydroxyl oligomer.
• By addition of carbohydrate into an aqueous dispersion of the cores under
sonication the coating is carried out.
• These are then subjected to lyophilization which make an irreversible adsorption
of carbohydrate onto the ceramic surface.
• By centrifugation the unadsorbed carbohydrate are removed.

13. IMMOBILIZATION OF THE MOLECULE
• The loading of drug to the coated particles by adsorption is the last and final
stage for the preparation of aquasomes.
• In this stage a solution of known concentration of drug is prepared in suitable pH
buffer and coated particles are dispersed into it.
• The dispersion is then kept overnight at low temperature which governs drug
loading or lyophilized after some time so as to obtain the drug-loaded
formulation.
• The preparation thus obtained is then characterized using various techniques .

14. CHARACTERIZATION OF AQUASOMES
They are characterized for the structural and morphological properties, particle size distribution and
drug loading capacity.
• Size distribution
Morphological properties and particle size distribution can be characterized by scanning electron
microscopy and transmission electron microscopy. For the measurement of man particle size and
zeta potential of the particle photon correlation spectroscopy is used.
• Structural analysis
• For structural analysis FT-IR spectroscopy is used. In FT-IR Potassium bromide sample disk method
is used, core as well as coated core is analysed by recording their IR spectra in wave number range
4000-400 cm-1.
• Crystallinity
X –ray diffraction is used to determine crystalline or amorphous behavior of ceramic core.

15. CHARACTERIZATION OF COATED CORE
• Carbohydrate coating
For coating of sugar over ceramic core Concanavalin A-induced aggregation method or anthrone
method is used. By the help of zeta potential measurement, absorption of sugar over the core is
recorded.
• Glass transition temperature
The transition from glass to rubber state as a change in temperature upon melting of glass DSC
analyser can be used to analyse.

17. APPLICATIONS OF AQUASOMES
Aquasomes has got a quite versatile application potential as a carrier for delivery of
vaccines, hemoglobin, drugs, dyes, enzymes.
• Aquasomes used as vaccines for delivery of viral antigen
• Aquasomes as red blood cell substitutes can effectively deliver the large, complex labile
molecule, haemoglobin. By incorporating in aquasome carriers, the toxicity of
haemoglobin is reduced, biological activity is preserved, haemoglobin concentration of
80% can be achieved and is reported to deliver oxygen in a non linear manner like natural
red blood cells.
• Aquasomes for pharmaceuticals delivery i.e. insulin, developed because drug activity is
conformationally specific. Bio activity preserved and activity increased to 60% as
compared to i.v. administration and toxicity not reported .
• Aquasomes are used for oral delivery of acid labile enzyme, serratiopeptidase. Enzyme
loaded aquasome was further protected by encapsulating in alginate gel. They protected
structural integrity of enzymes and better therapeutic efficacy was observed .

18. MARKETED PRODUCT
• ACQUASOME body therapy

19. REFERENCE
• INTERNATIONAL JOURNAL OF PHARMACEUTICAL AND CHEMICAL
SCIENCES ISSN: 2277 5005