One of the most recently created delivery systems for bioactive chemicals like peptides, proteins, hormones, antigens, and genes is called an aquasome. Aquasomes have circular 60–300 nm-sized particles. Aquasomes are networks of nanoparticulate carriers rather than pure nanoparticles. They are spherical particles made of calcium phosphate or ceramic diamond coated with a polyhydroxy oligomeric layer. A solid phase nanocrystalline core covered in an oligomeric film that adsorbs biochemically active molecules with or without modification makes up the core of the three layers of self-assembled structures. It frequently serves as an implant preparatory tool.

1. AQUASOMES
SUBMITTED BY-HIMADRI PRIYA GOGOI
ACP22PHCE004
Department of pharmaceutics
Acharya & BM Reddy College of pharmacy
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2. CONTENT
• Introduction
• Properties
• Advantages
• Disadvantages
• Principle of self assembly
• Method of preparation
• Application
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3. INTRODUCTION
• 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.
• Aquasomes are also called as “bodies of water” and their water like properties
protect and preserve fragile biological molecules.
• Aquasomes are one of the most recently developed delivery system for bioactive
molecules like peptide, protein, hormones, antigens and genes to specific sites.
• Aquasomes are spherical in shape with 60–300 nm particles size.
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4. • 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.
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5. PROPERTIES
• Aquasomes have 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, vander
waals forces and entropic forces. As solid particles dispersed in aqueous
environment, they exhibit physical properties of colloids
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6. • In general these aquasomes are assemblies of simple polymers, complex
lipid mixtures with diameter ranging between 30 to 500 nm.
• As these are solid or glassy particles dispersed in an aqueous
environment, they exhibit the physical properties of colloids and their
mechanism of action is controlled by their surface chemistry.
• Aquasomes deliver their contents through a combination of specific
targeting, slow and sustained release process.
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7. ADVANTAGES
• Increase the therapeutic efficacy of pharmaceutically active
ingredients.
• Avoid multiple injection schedule.
• Offer favourable environment for protein.
• Used for various imaging test.
• Act as a vaccine delivery system.
• Novel carrier of enzymes such as DNAses and pigment/dyes
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8. DISADVANTAGES
• It is expensive.
• If the drug is poorly absorbed, may cause burst release in the
body that cause toxicity.
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9. RATIONAL AQUASOME BEHIND DEVELOPMENT
• There are many reasons behind the creation of this novel drug
delivery system, some of which are defined as natural material:
professions such as prodrug, macro molecules, and liposomes that
are meant to have biological limitations.
 The drug delivery mechanism adjusts underlying biophysical limits,
fatigue, and conformational changes.
 There are some inherent structural biophysical limits, which are
identical to sugar.
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10. 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
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11. 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 -carboxylated /phosphate group bound to
ionized arginine / lysine side chain of protein.
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12. 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.
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13. 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.
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14. METHOD FOR PREPARATION
• By using the principle of self assembly Aquasomes can be prepared by
three method
(1) Preparation of core.
(2) coating of core.
(3) Immobilization of drug molecule
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15. 1. PREPARATION OF CORE
• This stage mainly depends on the selection of material for core, -its
physical chemical properties.
• This can be fabricated by the
-Sonication
-Colloidal precipitation.
• For the core material material ceramic material widely used ,as they
are structurally to be known
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16. • Commonly used ceramic core are tin oxide, and calcium phosphate.
Example: synthesis of nanocrystalline tin oxide core material.
• This can be prepared by
-Direct current reactive.
-Magnetron sputtering
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17. • 3 inch diameter target 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 and cool
with liquid nitrogen.
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18. •Synthesis of nano crystal brushite (calcium phosphate
dihydrate)
• This can be prepared by
-colloidal dispersion
-Sonication
-By reaction of disodium hydrogen phosphate and calcium phosphate.
• The commonly feature include
-Crystalline
-They measure b/w 50-150nm. And exhibit clean and reactive surface
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19. 2.CARBOHYDRATE COATING
• The second step involves coating by carbohydrate on the surface of
ceramic cores.
• There are number of processes to enable the carbohydrate (polyhydroxy
oligomers) coating to adsorb epitaxially on to the surface of the Nano
crystalline ceramic cores.
• Process generally entail, Addition of poly hydroxy oligomer, To a
dispersion of core in ultra pure water.
• Lyophilization (to promote the adsorption of carbohydrate on the surface
of ceramic core) Excess of carbohydrate is removed by stir cell
ultrafilteration
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20. 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
biological active molecule.
• Drug can be loaded by partial adsorption.
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21. Characterization of ceramic core:
Size distribution:
• For morphological characterization and size distribution analysis,
Scanning Electron Microscopy (SEM) and Transmission Electron
Microscopy (TEM) are generally used.
• Mean particle size and zeta potential of the particles can also be
determined by using photon correlation spectroscopy
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22. • Structural analysis:
FT-IR spectroscopy can be used for structural analysis. Using the potassium
bromide sample disk method, the core as well as the coated core can be
analyzed by recording their IR spectra in the wave number range 4000-400 cm-
1
• Crystallinity:
The prepared ceramic core can be analyzed for its crystalline or amorphous
behavior using X-ray diffraction. In this technique, the X-ray diffraction pattern
of the sample is compared with the standard diffractogram, based on which the
interpretations are made.
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23. Characterization of coated core
• Carbohydrate coating
• Coating of sugar over the ceramic core can be confirmed by
i. concanavalin A-induced aggregation method (determines the amount of
sugar coated over core)
ii. anthrone method (Determines the residual sugar unbound or residual
sugar remaining after coating).
iii. Furthermore, the adsorption of sugar over the core can also be confirmed
by measurement of zeta potential.
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24. Characterization of drug-loaded aquasomes:
• Drug payload
i. The drug loading can be determined by measuring the drug remaining
in the supernatant liquid after loading which can be estimated by any suitable
method of analysis.
• In vitro drug release studies
i. The in vitro release kinetics of the loaded drug is determined to study
the release pattern of drug from the aquasomes by incubating a known quantity
of drug-loaded aquasomes in a buffer of suitable pH at 37 °C with continuous
stirring.
ii. Samples are withdrawn periodically and centrifuged at high speed for
certain lengths of time. Equal volumes of medium must be replaced after each
withdrawal. The supernatants are then analyzed for the amount of drug released
by any suitable method
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25. Applications of Aquasomes:
• Aquasomes has got a quite versatile application potential as a carrier for
delivery of vaccines, hemoglobin, drugs, dyes, enzymes.
1)Aquasomes used as vaccines for delivery of viral antigen
2) 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.
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26. 3) 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 .
4) Aquasomes are used for oral delivery of acid labile enzyme. Enzyme loaded
aquasome was further protected by encapsulating in alginate gel.
5)They protected structural integrity of enzymes and better therapeutic
efficacy was observed.
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27. REFERENCE
• Dr . K. RAVINDRA REDDY , Dr .B. NARASIMHA RAO, S. FATHIMA K.BHAVYA:
AQUASOME A NOVEL VESICULAR DRUG DELIVERY SYSTEM.
• Sanjay S. Jain, Pramod S. Jagtap, Neha M. Dand, Kisan R. Jadhav and Vilasrao J.
Kadam : AQUASOMES: A NOVEL DRUG CARRIER.
• www. Slideshare.com
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