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Chemistry: Contributions to Clinical Therapeutics
Jaume Veciana
20th CenturyResearch based on the discovery of new
molecular entities (APIs)
Keys: chemical synthesis, molecular and bioactivity characterization
Analgesics Antibiotics Cancer treatment
Nanomedicine
Drug Delivery System
Drug
Polymeric capsule(pharmacological features)
Nanocarrier
Increasing the therapeutic efficiency of drugs….
(therapeutic action)
NanomedicineDrug therapies based in targeted/controlled
drug delivery systems
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
NanoparticlesNanosuspensions
Nanomedicine
VesciclesLiposomes
Polymeric-drugconjugates
Novel 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
New Methods to Prepare Particulate Drug Delivery Systems
Using compressed CO2 as a green solvent
New Methods to Prepare Particulate Drug Delivery Systems
NanoparticlesNanosuspensions
VesciclesLiposomes
Polymeric-drugconjugates
DELOS-family processes
0.1 1 10 1000
4
8
12
% V
olum
e
Particle Size (µm)
BioavailableNon-bioavailable
Salmenterol xinafoate (SX)
HO
HO
OH
NH2+
O
OH
CO2-
Drug for inhalatory asthma treatment
Processing of a drug for bronquial asthma
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
Compressed CO2
Integration Encapsulation
Integration of Bioactive Principles into Nanovesicles
Integration on surface & inside of the nanovesicles
CO2
Cholesterol CTAB
Bioactive macromoleculesBioactive small molecules
Integration of Bioactive Principles into Nanovesicles
Spin-off at PRUAB:
E. Elizondo, Doctoral Thesis, 2010
Scaling-up the DELOS methodology
6 mL system 300 mL system
X 5025mL 1250mL
2000 mL system
X 68300mL
E. Elizondo, Doctoral Thesis, 2010
Scaling-up the DELOS methodology
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 AcknowledgmentsCo-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
Thank you for your attention.......
Acknowledgements AcknowledgmentsMolecular Nanoscience