Aquasomes evaluation

Aquasomes evaluation

1. AQUASOMES PRESENTED BY, NIMMI ROY 1 ST YEAE MPHARM DEPT OF PHARMACEUTICS SRINIVAS COLLEGE OF PHARMACY 1

2. CONTENTS Introduction Bodies of water Principle Preparation Evaluation Applications References 2

3. DEFINITION Aquasomes can be defined as “ nanoparticulate carrier system with three layered self assembled structure comprising of central solid nanocrystalline core coated with polyhydroxy oligomers onto which biochemically active molecules are absorbed. 3

4. INTRODUCTION Aquasomes are first discovered by NIR KOSSOVSKY. Consists of solid crystalline core , carbohydrate core and active drug. It is spherical in shape and size of 60-30nm. Aquasomes are called as “Bodies of water” and their water property protect and preserve fragile biological molecules. 4

5. BODIES OF WATER Water like properties. Protect and preserve fragile biological molecules. Maintain conformational integrity as well as high degree of surface exposure in targeting of bio-active molecules/ 5

6. PRINCIPLE OF SELF ASSEMBLY Assembly of micromolecule is governed by 3 process. Interaction between charged groups. Hydrogen bonding and dehydration. Structural stability. 6

7. Interaction between charged groups Interaction of charged group such as amino, carbonyl, sulphate, phosphate groupsfacilitate the long range approach of self assembling subunits. Charged groups also play role in stabilizing teritiary structure of folded proteins. Example of ion pairs- carboxylated /phosphate group boundto ionized arginine /lysine side chain of protein. 7

8. Hydrogen bonding and Dehydration effect Hydrogen bond are formed between hydrogen atom attached to an electronegative donor atom and an electronegative or basic acceptor. Hydrogen bond help in base pair matching and stabilization of secondary protein structure. Molecules that form hydrogen bonds are hydrophilicand these molecule confer significant degree of organization to the surronding water molecules. 8

9. 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 amoung hydrophilic side chains promotes stability of compact helical structures. 9

10. PREPARATION Simple and straight forward approach with minimum solvent usuage . No homogenization steps. 3 steps of preparation by using the principle of assembly:- Preparation of the core- Co precipitation Self-precipitation Sonication PAMAM 2.Carbohydrate coating of the core 3.Immobilization of drug molecule 10

11. PREPARATION OF THE CORE Co-precipitation 11

12. Self-precipitation 12

13. Sonication 13

14. PAMAM Carboxilic acid terminated half generation poly( amidoamine )(PAMAM) used. Forms amorphus hydroxyapatite cores with a mixture of calcium phosphate. 14

15. CARBOHYDRATE COATING OF CORE Coating material – Cellulose , citrate , pyrodoxal-5-phosphate , sucrose and trehalose Adsorption method- Lactose coated by adsorption method by direct incubation and by nonsolvent addition. 15

16. IMMOBILIZATION OF DRUG MOLECULE The drug can be loaded by partial adsorption. 16

17. 17 Fig: preparation of aquasomes

18. EVALUATION 18

19. EVALUATION OF CERAMIC CORE Structure analysis- Interpretated by fourier transformed infrared spectroscopy using hydroxypatite powder in the wave no range of 4000-400 cm⁻¹. Phase analysis of core- Cores exposed to Cu K- α radiation in a wide angle X-ray diffractometer . Particle morphology- Determined by using transmission electron microscopy one drop of aqueous dispersion is placed over a 400-mesh carbon-coated copper grid followed by negative staining with phosphotungstic acid and placed at the accelerataing voltage. 19

20. EVALUATION OF SUGAR COATING Colorimetric analysis-( Anthrone method) 20

21. Concanavalin –A-Induced aggregation 21

22. EVALUATION OF DRUG LOADED AQUASOMES Size and shape- Morphological examination- transmission electron microscope. Mean particle size and size distribution-A photon correlation spectroscopy using a Autosizer II C apparatus and SEM. Chemical composition and crystalline structure – X-ray powder diffractometry . Glass transition temperature- Carbohydrates and protein studied by using DSC analyzer. In-process stability studies- Stability and integrity of protein during the formulation of the aquasomes determined by using sodium dodecyl sulfatepolyacrylamide gel electrophoresis(SDS-PAGE) 22

23. In vitro drug release studies- To study the release pattern of drug 23

24. Drug loading efficiency- Ensure the amount of drug which is bound on the surface of aquasomes . Hb loading capacity-( Drabkin’s method) Estimated by the difference between the control sample( HbaA solution)and the free hemoglobin contained in all fractions without nanoparticles . Antigen loading efficiency- 24

25. APPLICATIONS Oxygen carrier For immunotherapy For oral route For immunopotentiation Anti thrombic activity Antigen delivery Delivery of poorly soluble drugs Enzyme delivery Insulin delivery Vaccine delivery 25

26. CONCLUSION Aquasomes appears to be promising carriers for delivery of broad range of conformational sensitive molecule better biological activity as it contain carbohydrate coating over creamic core.Molecular plasticizers,carbohydrates prevent destructive carrier intraction and helps to preserve spatial qualities and the crystalline natural core provide structural stability and overall integrity. This strategy may benificially extended to novel drug delivery of other bioactive molecule. 26

27. REFERENCES Jain N.K. Advances in controlled drug delivery system , 317-328. wani S.U, Yerawar A.N. International journal of pharmacy and technology 2015; 2:1. Gulati monica , Singh sachin . Potential applications of aquasomes for therapeutic delivery of proteins and peptides, www.pharmainfonet .com/ aquasomes . 27

28. 28 THANKING YOU…..