VEICOLAZIONE E DIREZIONAMENTO DEI FARMACI CON POLIMERI DI INTERESSE FARMACEUTICO

12 CFU - 2° Semester

Teaching Staff

LUCIA MONTENEGRO - Module Modified drug delivery systems and drug targeting - CHIM/09 - 6 CFU
MARIA GRAZIA SARPIETRO - Module POLIMERI DI INTERESSE FARMACEUTICO - CHIM/09 - 6 CFU

Learning Objectives

Modified drug delivery systems and drug targeting
The aim of this course is to provide the student with knowledge and expertise about the strategies exploited in the field of drug-modified release and targeting and their use in biotechnology. In addition, the course focuses on fundamentals of biopharmaceutics and their application to pharmaceutical technology to provide the student with a comprehensive understanding of controlled drug delivery systems.
POLIMERI DI INTERESSE FARMACEUTICO
Provide the fundamental concepts concerning the structure and behavior of polymeric materials and the main tools that allow to relate the characteristics of polymers with their properties; give an overview of the most important synthetic and natural polymeric materials used in the industrial field with an in-depth study of the biomedical and pharmaceutical fields.

Course Structure

Modified drug delivery systems and drug targeting
Prerequisites

Knowledge of organic chemistry and pharmaceutical technology

Teaching methods

Frontal lessons. Should teaching be carried out in mixed mode or remotely, it may be necessary to introduce changes with respect to previous statements, in line with the programme planned and outlined in the syllabus.

Learning Assessment

Learning assessment is performed in the form of written test consisting of 5 open questions. Learning assessment may also be carried out on line, should the conditions require it.
POLIMERI DI INTERESSE FARMACEUTICO
lectures (powerpoint presentation)

Detailed Course Content

Modified drug delivery systems and drug targeting
Administration routes and bioavailability of drugs. Controlled drug delivery systems: classification. Active and passive drug targeting. Fundamentals of controlled drug delivery systems: reservoir systems, osmotic systems, matrix systems, ion exchange systems.

Vesicular controlled delivery systems. Liposomes: advantages and limits, classification, preparation methods, physico-chemical and technological characterization, use in the pharmaceutical field. Ethosomes, transferosomes, niosomes. Technological properties and use in the pharmaceutical field.

Microparticles as controlled delivery systems: advantages and limits. Preparation and characterization methods. Use in the pharmaceutical field.

Nanoparticles as controlled delivery systems: polymeric nanoparticles, solid lipid nanoparticles, nanostructured lipid carriers. Advantages and limits. Physico-chemical and technological characterization. Preparation methods. Use in the pharmaceutical field.

Chemically controlled delivery systems: prodrugs. Advantages and limits, properties and use in the pharmaceutical field.

Molecular inclusion complexes: cyclodextrins. Definition and classification. Preparation methods of cyclodextrin-drug inclusion complexes. Instrumental analyses to characterize inclusion complexes. Use in the pharmaceutical field.

Transdermal delivery systems: advantages and limits, technological properties, use in the pharmaceutical field.

Gene therapy: fundamentals and goals; design and synthesis of oligonucleotide, molecular mechanisms. Biological barriers to gene delivery. DNA and the oligonucleotide delivery: viral and synthetic carriers (liposomes, cationic polymers and lipopolyplexes).
POLIMERI DI INTERESSE FARMACEUTICO
Introduction to polymers. Molecular weights: definitions and methods of determination.

Step-by-step polymerizations: kinetics, degree of advancement, molecular weight distribution. Chain polymerizations: radicals; characteristics, mechanism, kinetics.

Introduction to stereoisomerism in polymers. Stereoregular polymers: isotactic, syndiotactic. Ziegler-Natta polymerizations. Anionic and cationic polymerizations. Polymerization methods.

The solid state in polymers: the amorphous state and the semi-crystalline state; glass transition temperature, crystallization and melting temperatures.

Mechanical properties of polymers.

Viscosity of polymeric solutions. Mark-Houwink-Sakurada equation and calculation of the viscosimetric average molecular weight. Principles of Rheology. Non-Newtonian fluids.

Main synthetic polymers and their applications.

Polysaccharides: general properties. Starch, cellulose, alginates, guar, dextran and other classes of polysaccharides: structures, industrial uses.
Polymeric biomaterials: biofunctionality and biocompatibility, biodegradability, mucoadhesiveness. Applications in the biomedical and pharmaceutical fields.
Devices for the controlled delivery of drugs: matrix, reserve, subcutaneous implants, ocular inserts, transdermal.
Hydrogel: structures, degree of swelling.
Polymers for biomedical and pharmaceutical applications: synthetic (polyolefins, polyesters, polysiloxanes, PEGs) and natural (cellulose and derivatives, other polysaccharides). Polymers for gastro-resistance: polyacrylates (Eudragit).
Microparticles and microencapsulation: interfacial polymerization technique, ion complexation, solvent evaporation technique, spray drying. Applications of microencapsulation in the pharmaceutical, food and cosmetic fields.
Polymeric nanoparticles: definitions, methods of preparation. Nanoparticles as drug carriers. Passive coating and targeting (EPR effect). Functionalization and active targeting.

Polymer chracterization

Textbook Information

Modified drug delivery systems and drug targeting
-COLOMBO P., CATELLANI P.L., GAZZANIGA A., MENEGATTI E., VIDALE E.; Principi di tecnologie Farmaceutiche; Casa Ed. Ambrosiana, Ultima Edizione.

-FLORENCE A.T. AND ATTWOOD D.; Le basi chimico-fisiche della Tecnologia Farmaceutica; Edises, Ultima Edizione.

- AULTON M.E. AND TAYLOR K.M. Tecnologie farmaceutiche. Progettazione e allestimento dei medicinali; Edra, Ultima Edizione
POLIMERI DI INTERESSE FARMACEUTICO
FW Billmeyer Jr - Textbook of polymer science.

AIM (Associazione Italiana di Scienza e Tecnologia delle Macromolecole) Macromolecole Scienza e tecnologia, Pacini editore, Pisa.

Atti del XIX Convegno Scuola AIM Mario Farina su "Polimeri in Medicina", 1997;

slides

Open in PDF format Versione in italiano