Chemistry: Contibutions to Clinical Therapeutics By Jaume Veciana

1. “NANOMEDICINA. La Última Frontera”
Chemistry: Contributions to
Clinical Therapeutics
Jaume Veciana
vecianaj@icmab.es
www.expoquimia.com

2. Nanomedicine
20th Century
Research based on the discovery of new
molecular entities (APIs)
Analgesics Antibiotics Cancer treatment
Keys: chemical synthesis, molecular and bioactivity
characterization

4. Nanomedicine
Drug therapies based in targeted/controlled
drug delivery systems
Drug
(therapeutic action)
Polymeric capsule
(pharmacological features)
Nanocarrier
Drug Delivery System
Increasing the therapeutic efficiency of drugs….

9. Nanomedicine
Ideal Nanocarriers as Drug Delivery Systems (DDS)
Multifunctional nanobjects
Components Functions
Container
Protector
Targeting
Magnetic particle Diagnosis
Drug Therapy
Preparation of drug delivery systems at the nanoscale with scale-up
methods
P. Couvreur et al., Pharm. Res., 2006, 23, 1417-1450.

10. Nanomedicine
Novel Drug Delivery Systems
Nanoparticles Polymeric-drug Vescicles
Nanosuspensions conjugates Liposomes

11. New Methods to Prepare Particulate Drug Delivery Systems
Using compressed CO2 as a green solvent
 Non-toxic
 Non-flammable
 Cheap
 Easy separated from products
 Enabling to control particles
 Scale-up methods
J.J. Watkins et al., Science 2004, J.D. Holmes et al. Chem. Eur. J. 2003

12. New Methods to Prepare Particulate Drug Delivery Systems
Using compressed CO2 as a green solvent
Vescicles
Liposomes
Polymeric-drug
conjugates
Nanoparticles
Nanosuspensions
DELOS-family processes

15. Processing of a drug for bronquial asthma
Salmenterol xinafoate (SX) Drug for inhalatory asthma treatment
OH
NH2+
HO
HO O
OH
CO2
-
Bioavailable
12 Non-bioavailable
% Volume
8
4
0
0.1 1 10 100
Particle Size (µm)

18. Processing of an antibiotic for resistent infections
Gentamicine loaded in bioadhesive nanostructured polymer as
microparticles
2,5 µm
Oral Delivery
E. Elizondo et al, Pharm. Res., 2011, 28, 309-321

21. Integration of Bioactive Principles into Nanovesicles
Integration on surface &
inside of the nanovesicles
Compressed
CO2
Integration Encapsulation

22. Integration of Bioactive Principles into Nanovesicles
Cholesterol CTAB
CO2
small molecules
Bioactive macromolecules
Spin-off at PRUAB:

23. Scaling-up the DELOS methodology
6 mL system 300 mL system 2000 mL system
25mL 1250mL 8300mL
X 50 X6
E. Elizondo, Doctoral Thesis, 2010

24. Scaling-up the DELOS methodology
E. Elizondo, Doctoral Thesis, 2010

25. Nanomedicine Acknowledgments
Co-workers:
Dr. Nora Ventosa, Dr. Santi Sala, Dr. Maria Muntó, Dr. Mary Cano, Dr. Elisa
Elizondo, Alba Cordoba, Ingrid Cabrera, Dr. Miquel Gimeno, Daniel Villanueva,
Dr. Evelyn Moreno, Dr. Imma Ratera, Dr. César Diez-Gil, Witold Tatkiewicz
Financial support:
Collaborations:
• Prof. Marcel Besnard (LPCM-CNRS, France)
• Dr. Cristina Patiño (CNB-CSIC, Madrid)
• Dr. Jordi Esquena (CID-CSIC, Barcelona)
• Dr. Sylvane Lesieur (CNRS, France)
• Prof. Antoni Villaverde (UAB)
• Dr. Simó Schwartz (Hospital Vall D´Hebrón)
• Dr. Maria Blanco (U. Navarra)
• Dr. Maria Parajo (IBEC, Barcelona)
• Prof. Joel Bernstein (Israel)
• Dr. Dimitrios Stamou (Denmark)
• Dr. Eduardo Martínez Díaz, (CIGB, Cuba)

26. Acknowledgements
Molecular Nanoscience Acknowledgments
Thank you for your attention.......