TECHNOLOGY OF TARGETING AND CONTROLLED RELEASE OF DRUGS

The course provides the knowledge concerning the drug delivery technology and controlled release mostly from nanocarriers and smart matrixes.
An introduction on the pharmaco-economic reasons that motivate the development of alternative formulations of drugs will be provided.
The course starts by discussing the technological determinants dictating the behavior of controlled release systems and continues with the most advanced formulations for the delivery of drugs. In particular, 1. the relevance of having performing systems that guarantee the targeting of drugs to specific sites and 2. the controlled release to reduce administration frequencies and side effects of drugs will be discussed. Mechanisms, parameters and effect of matrix components dictating release rate from matrices, particles, capsules will be discussed. Strategies to control the release of drugs from matrices.
Special attention is paid to colloidal systems in the drug delivery technology. Procedures to prepare and the advantages offered by polymer based micro- and nano-particles for the administration of drugs. Required properties to prepare performing colloidal carriers in term of release profile, stability, biocompatibility with special attention to surface properties and stealth behavior for prolonged blood circulation time and reduced clearance. Impact of nanotoxicity on the performance of colloidal systems for drug delivery. Examples of commercial nanoparticles for the delivery of drugs. Use of metal nanoparticles for diagnostic and therapeutic purposes.
Updated techniques for the characterization of drug nanocarriers and colloidal systems. Size, morphology and zeta potential assessment.
Transdermal and transmucosal routes as non-conventional administration routes of drugs for efficient drug delivery. Features and requirements to formulate a drug for the administration through those routes.
Cyclodextrins as natural carriers for targeted delivery of drugs and controlled release; Macromolecular and colloidal systems based on cyclodextrin. Clinical examples of advanced nanosystems obtained with cyclodextrins.
The students will be involved in a practical laboratory where they will prepare polymeric nanoparticles, polymeric micelles, metal nanoparticles coated with a polymeric shell, cyclodextrin/drug molecular complexes. The preparation of these systems requires that the students exploit their knowledge about stoichiometric dilution of solutions. They will characterize those systems in term of size, physical stability, pharmaceutical behavior by looking at the release profile of the loaded drugs.