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Chemistry: Contributions to Clinical Therapeutics

Jaume Veciana

vecianaj@icmab.es

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