Chemistry: Contributions to Clinical Therapeutics. Drug therapies based in targeted/controlled drug delivery systems.

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

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

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

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

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

11. 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
New Methods to Prepare Particulate Drug Delivery Systems

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

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

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

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

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

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

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

25. 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)
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

26. Thank you for your attention.......
Acknowledgements AcknowledgmentsMolecular Nanoscience