Aquasomes , M.PHARM.F.Y

1. AQUASOMES
Presented By:
Rida Sharif
06

2. 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 spherical in shape with 60–300 nm particles size.
 Aquasomes are utilized for targeted drug delivery to achieve specific
therapeutic effects, and are biocompatible, biodegradable, and stable.
 Aquasomes are first discovered by Nir Kossovsky in 1995.

3. INTRODUCTION :
 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.

4. INTRODUCTION :
 Aquasomes made of calcium phosphate or ceramic diamond coated with a
polyhydroxyl oligomeric film that function as nanoparticulate carrier systems.
It is a biomaterial used in nano biopharmaceutics.
 The pharmacologically active molecule can be incorporated by following
methods like co-polymerization, diffusion or adsorption to carbohydrate
surface of pre-formed nanoparticles.
 As these are solid or glossy particles dispersed in aqueous environment,they
exhibit the physical properties of colloids and their mechanism of action is
controlled by their surface chemistry.
 Aquasomes delivers their contents through a combination of special targeting
molecular shielding and slow & sustained release process.
 Their intended route of administration is parenteral. Some researchers have
extended the route of administration from parenteral to oral.

5. PROPERTIES :
1. Aquasomes water like properties provides a platform for preserving the
conformational Integrity and bio chemical stability of bio-actives.
2. Aquasomes due to their size and structure stability, avoid clearance by
reticuloendothelial system or degradation by other environmental challenges.
3. 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.
4. Protect the drug/antigen/protein from harsh pH condition & enzymatic
degradation.

6. PRINCIPLE OF SELF ASSEMBLY:
 Self assembly implies that the constituent parts of some final product
assume spontaneously prescribed structural orientations in two or three
dimensional space.
 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.

7. 1. Interactions 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.

8. 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.

9. 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.

10. COMPOSITION OF AQUASOMES :
1. Core material : Ceramic and polymers are most widely used core materials.
Polymers such as albumin, gelatin or acrylate are used. Ceramic such as
diamond particles, brushite (calcium phosphate) and tin oxide are used.
2. Coating material : Coating materials commonly used are cellobiose,
pyridoxal 5 phosphate, sucrose, trehalose, chitosan, citrate etc. Carbohydrate
plays important role act as natural stabilizer, its stabilization efficiency has
been reported. Beginning with preformed carbon ceramic nanoparticle and
self assembled calcium phosphate dihydrate particles (colloidal precipitation)
to which glassy carbohydrate are then allowed to adsorb as a nanometer thick
surface coating a molecular carrier is formed.
3. Bioactive : They have the property of interacting with film via non covalent
and ionic interactions

11. OBJECTIVES OF AQUASOMES :
1. Enhanced Stability: Aquasomes aim to stabilize pharmaceutical compounds
vulnerable to degradation in water-based environments.
2. Increased Bioavailability: They improve drug absorption and distribution in the
body, enhancing therapeutic efficacy.
3. Controlled Drug Delivery: Aquasomes offer precise control over the release of
drugs, allowing for targeted and sustained delivery.
4. Improved Solubility: They enhance the solubility of poorly soluble drugs, aiding in
their dispersion in aqueous solutions.
5. Targeted Delivery: Aquasomes can be engineered to deliver drugs to specific tissues
or cells, reducing side effects and improving treatment outcomes.
6. Aquasomes protect bio-actives.
7. Aquasomes maintains molecular confirmation and optimum pharmacological activity.

12. Method Of PREPARATION :
 The method of preparation of aquasomes involves three steps.
 The general procedure consists of Formation of an inorganic core, followed by Coating
of the core with polyhydroxy oligomer, and finally loading of the drug of choice to this
assembly.
 By using the principle of self-assembly, the aquasomes are prepared in three steps i.e.,
1. Preparation of core.
2. Coating of core.
3. Immobilization of drug molecule.

13. 1. Preparation of core :
 The process of ceramic core preparation depends on the selection of the
materials for core, its physical chemical properties.
 These ceramic cores can be fabricated by
1. colloidal precipitation.
2. Sonication.
3. inverted magnetron sputtering.
4. plasma condensation and other processes.
 For the core material ceramic material widely used, as they are structurally to
be known.
 Commonly used ceramic core are tin oxide, and calcium phosphate.
 Example: synthesis of nanocrystalline tinoxide core material.

14. 2. Coating of core :
 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.
 The processes generally entail the addition of polyhydroxy oligomer to a
dispersion of core in ultra pure water, sonication and then lyophilization to
promote the largely irreversible adsorption of carbohydrate onto the ceramic
core.
 Excess and readily desorbing carbohydrate is removed by stir cell ultra-
filtration.

15. 3. Immobilization of drug molecule :
 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
 The pharmacologically active molecule incorporated carbohydrate surface of
preformed nanoparticles by Co-polymerization, Diffusion, (or) adsorption

16. CHARACTERIZATION OF
AQUASOMES :
 Aquasomes are mainly characterized for structural analyses, particle
size, and morphology these are evaluated by X-ray powder
diffractometry, transmission electron microscopy, and scanning electron
microscopy.
 The morphology and the size distribution were obtained throughimages of
scanning electron microscopy.
 The chemical composition and the crystalline structure of all samples were
obtained through X-ray powder diffractometry.

17. APPLICATION :
1. Aquasomes as red blood cell replacements, with hemoglobin immobilized on the
oligomer surface due to the conformational sensitivity of hemoglobin's oxygen
release. This reduces toxicity, achieving an 80 percent hemoglobin concentration and
delivering blood in a nonlinear fashion similar to normal blood cells.
2. Aquasomes, a five-layered composition consisting of a ceramic Centre,
polyoxyoligomeric film, therapeutic gene section, additional carbohydrate film, and a
targeting layer of conformational conserved viral membrane protein, have been used
for effective targeted intracellular gene therapy.
3. Aquasomes used as vaccines for viral antigen delivery, such as Epstein-Barr and
Immune Deficiency Virus, must be activated by conformationally specific target
molecules in order to elicit proper antibody.
4. Since drug activity is conformationally specific, aquasomes for pharmaceutical
delivery, such as insulin, were created. When compared to i.v. administration,
bioactivity was maintained and activity increased by 60%, with no confirmed
toxicity.

18. CONCLUSION :
 Aquasomes are one of the greatest basic and innovative drug carriers based on the
self-assembly theory. Even when conformationally sensitive drug candidates are
delivered via aquasomes, they display better biological activity.
 This is most likely due to the special carbohydrate coating on the ceramic.
 These formulations have also been found to elicit a stronger immune response,
suggesting that they may be used as an immune adjuvant for proteinaceous
antigens.
 As a result, this method gives pharmaceutical researchers a new ray of hope for
bioactive molecule distribution Still, much more research on Aquasomes is
needed in terms of pharmacokinetics, toxicology, and animal studies to confirm
their efficacy and safety, in addition to determine their clinical utility and
commercialization.

19. REFRENCES :
 A REVIEW ON AQUASOMES: Prashant Popat Jadhav, Dr. Nagesh
Hanmantrao Aloorkar. Department of Pharmaceutics, Satara College of Pharmacy,
International Journal of Creative Research Thoughts (IJCRT).
 AQUASOMES: A NOVEL DRUG CARRIER, Sanjay S. Jain, Pramod S.
Jagtap, Neha M. Dand, Kisan R. Jadhav and Vilasrao J. Kadam, Journal of
Applied Pharmaceutical Science.
 AQUASOMES: A NOVEL NANOPARTICULATE DRUG CARRIER,
Sritoma Banerjee, Kalyan Kumar Sen, Jurnal of Drug Delivery Science and
Technology.
 AQUASOMES: A NOVEL NANOCARRIER FOR DRUG DELIVERY: S.U.
Wani 1., A. N. Yerawar ., available through International Journal of pharmacy and
Technology.
 AQUASOMES: A NOVEL CARRIER FOR DRUG DELIVERY, Vishal
Sutariya and Parth Patel, International Journal of Pharmaceutical Sciences and
Research.

20. THANK
YOU