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Page 1
Development of PristinaTM Aerogel for Targeted and Controlled Release of Cancer Pharmaceuticals
The ATTIA Applied Sciences Inc.TAASI Corporation
Page 2
Schematic of Therapeutic Nanodevice
A) Particle device binds to target cell.
B) Therapeutic agent is released from pore structure of device.
Aerogel Particle
Target Cell
Cell Membrane
Receptor on cell surface
Ligand
“Stealth” Coating
Aerogel Particle
Agent Releasing
Target Cell
Near Cell
Cell Wall
Agent Agent
Receptor
Page 3Page 3
TAASI Project Goals1. Develop very fine particles [less than 2
microns] with 90% porosity of TAASI’s PristinaTM SCM-Aerogel for the storage and subsequent 60 minute controlled release of targeted pharmaceutical agents (melitin).
2. Integrate the chemical “o,o-Bis{3-aminopropyl) polyethylene glycol”, which acts as the “stealth” & anchoring link to the tumor specific EGF (Epidermal Growth Factor Ligand) protein.
3. Gadolinium Oxide, Gd2O3 [gadolinia], to be incorporated into the aerogel to act as a detection tag/identification label.
Page 4
Evaluation Procedures: Aerogel Effectiveness for Targeted/Controlled Release Pharmaceuticals
Routine experiments were outsourced to determine the effectiveness of the TAASI Aerogel particles in the melitin delivery system to targeted Cancer cells.
Aerogel Particle Preparatory Methodso Coupled with EGF (Epidermal Growth Factor Ligand) and
loaded with melitin prior to “seek and destroy” experiment
Model of Cancer Cells: Swiss 3T3 Cellso Expresses high levels of EGF Receptors
Model of Non-Cancer Cells: CHO Cellso Cell concentration was adjusted to equal the Swiss 3T3o No EGF Receptors Present on CHO cells
Page 5Page 5
TAASI Microgel SCM-PEG-Gd Aerogel
Page 6
Size Reduction Methods
1. Micronization, by Sonication, was used to achieve the desired aerogel particle size of 1 to 2 microns.
1. Fractionation, by gravity settling, was use to separate out the desired aerogel particles.
Page 7
TAASI Microgel SCM-Gd Size Distribution: Unsonicated vs. Sonicated
Page 7
Particle size distribution data (Coulter Multisizer) for Sonicated and Unsonicated aerogel particles
Page 8Page 8
TAASI Aerogel Property Results
Material Density g/cc
Porosity %
BET m2/g
SCM-A 0.12 94.77 333.1
2A: SCM-Gd-PEG* 0.26 88.38 -
2D: SCM-Gd (NO PEG) 0.16 92.72 -
Abbreviation Key1.SCM: TAASI Propriety Information2.A: Autoclaved3.Gd: Gadolinium Oxide4.PEG: Polyethylene Glycol
* Used in ‘Seek & Destroy’ Control Release Therapy
Page 9
Melitin Release Comparison:Pristina™ 2A-SCM Aerogel & Aldrich Silica
Page 9
Page 10
Death Loss of CHO & Swiss 3T3 Cells:Raw Data from Flow Cytometry Experiment
Page 10
CHO Cells Swiss 3T3 Cells
Flow Cytometry preformed by Kristie Melnik
1% Dead 97% Dead
Death Loss of Swiss 3T3 and CHO Cells
97
3 1
99
0
20
40
60
80
100
Swiss 3T3 EGFR+ CHO EGFR -
DeadCellsLiveCells
% Live
Page 11
% Dead