Ateneo - UPO

The course aims to introduce the main strategies and technologies used to optimize the targeted delivery of anticancer drugs, with particular focus on micro- and nano-particulate delivery systems. Students will acquire fundamental theoretical knowledge on the structures, mechanisms, technologies, and applications of advanced drug delivery systems. It begins with the study of microcapsules and microspheres, examining their internal structure, classification criteria, and pharmaceutical applications, especially in controlled release and active ingredient protection. The course then explores drug targeting mechanisms, distinguishing between passive targeting (based on the anatomical and pathological features of tumor tissue), active targeting (mediated by specific interactions between the carrier and biological target), and physical targeting (based on the use of external stimuli such as heat, ultrasound, or magnetic fields). Considerable attention is devoted to the evolution of multiparticulate carriers through first, second, and third-generation systems, each marked by increasing sophistication in recognizing and responding to the tumor microenvironment. The course also covers preparation technologies for micro- and nano-particulate systems, including emulsification, spray drying, coacervation, nanoprecipitation, and controlled synthesis. A central section of the course focuses on nanostructured systems, such as nanoparticles used in drug targeting, imaging, and theranostics. It discusses the properties and pharmaceutical uses of solid lipid nanoparticles, polymeric micelles, and liposomes, including their advantages, limitations, and surface modification strategies. Finally, the course presents the main advanced nanocarriers, including dendrimers, polymersomes, SPIO magnetic nanoparticles, gold nanoparticles, quantum dots, and ceramic and carbon-based nanoparticles. For each type, students will analyze physicochemical characteristics, potential applications in cancer treatment, and prospects for integrated therapeutic and diagnostic use.

Paolo Caliceti, Tecnologia farmaceutica, 2025, CEA Casa Editrice Ambrosiana. Aulton ME, Taylor K.M.G. Tecnologie farmaceutiche, 2015 EDRA LSWR. Farmacopea Ufficiale Italiana edizione vigente. Farmacopea Europea edizione vigente.

At the end of the course, students will be able to: Knowledge and understanding Grasp the theoretical principles and fundamental technologies behind the design of drug delivery and targeting systems for anticancer therapies, including microcapsules, microspheres, nanoparticles, and nanostructured systems. Applying knowledge and understanding Use acquired concepts to critically analyze the features, mechanisms, and potential of various drug delivery platforms, particularly those used in oncology. Making judgments Independently evaluate targeting strategies (passive, active, physical) and production techniques, recognizing the strengths and limitations of different approaches. Communication skills Communicate effectively using appropriate scientific and technical language to describe and discuss the characteristics and implications of advanced drug targeting systems. Learning skills Build upon course knowledge to pursue deeper insights, enabling engagement with more advanced studies and innovations in nanomedicine and oncological pharmaceutical technology.

To enroll in the course, the student must be familiar with the content covered in the first-year courses. Access to the final exam is subject to meeting the prerequisite requirements specified in the Academic Regulations

The course will be delivered primarily through lectures. Several seminars could be held by professionals working in the pharmaceutical industry, who will illustrate the practical application of the theoretical concepts presented. On certain occasions, students will be invited to respond collectively to questions on previously covered topics and to retrieve supplementary educational material from the official websites of AIFA, EMA, and FDA.

Students with physical disabilities, Learning Disabilities or Special Education Needs can request specific services and tools via the Staff Sviluppo e Coordinamento Carriere e Servizi alle Studentesse e agli Studenti, consulting the University webpage: https://www.uniupo.it/en/services/services-students-physical-or-learning-disabilities Students with disabilities, learning disabilities or special education needs, once they have contacted the University Staff, can refer to the tutor in charge of the course to define the examination modalities, concerning academic aspects.

The exam will be conducted in written and/or oral form. To achieve a final grade, students must demonstrate both a solid understanding and the ability to apply the fundamental concepts covered in the course. Evaluation, expressed on a scale of thirty, will take into account their theoretical and practical comprehension of the topics, their ability to think independently and connect different aspects of the subject, their communication skills and correct use of technical language, and their overall learning capacity.

The course introduces the principles of drug delivery and targeting in cancer therapy, illustrating the evolution of controlled drug release and site-specific drug delivery from conventional dosage forms to modern drug delivery systems. It examines the biological and pharmacological rationale of Paul Ehrlich's "magic bullet" concept, the principles of controlled drug release, the mechanisms governing drug accumulation at the target site, and passive, active, and physical targeting strategies, with particular emphasis on first-, second-, and third-generation drug delivery systems.
The course then focuses on microparticulate systems for anticancer drug delivery. The structural and functional characteristics of microcapsules and microspheres, drug encapsulation and release mechanisms, and their therapeutic applications are discussed. The main preparation techniques for microparticulate systems are also presented, including coacervation, phase separation, emulsion solvent evaporation and extraction, interfacial polymerization, complexation, spray technologies, and fluid-bed processes, highlighting their advantages, limitations, and pharmaceutical applications.
The second part of the course is devoted to nanoparticulate systems and drug targeting strategies. Following an introduction to nanomedicine for cancer therapy and the evolution of nanoscale drug delivery systems, the course examines passive, active, and physical targeting mechanisms, the physicochemical properties governing nanoparticle interactions with biological systems, and the principles underlying the design of nanocarriers. The major classes of nanoparticles used in cancer therapy are presented, including bio-inspired, polymeric, lipid-based, inorganic, and hybrid systems, discussing their structural characteristics, functional properties, and potential biomedical applications. The course also introduces the principles of theranostics and the main therapeutic approaches based on nanotechnology, including photothermal, photodynamic, and magnetothermal therapies.
The course concludes with an introduction to PEGylation and bioconjugation as strategies for modifying the pharmacokinetic and pharmacodynamic properties of therapeutic proteins and drug delivery systems. The rationale for PEGylation, its effects on bioavailability, stability, and immunogenicity, and the basic principles of bioconjugation applied to advanced drug delivery systems are also discussed.

By the end of the course, students will have acquired a solid understanding of micro- and nanoparticulate systems used for the delivery of anticancer drugs, including their structure, classification, and applications. They will be able to apply theoretical knowledge to critically analyze drug targeting and release strategies, including passive, active, and physically triggered delivery mechanisms. Students will demonstrate the ability to independently evaluate the potential of different delivery systems by considering their technological, functional, and therapeutic aspects in the context of oncology. They will also develop effective scientific communication skills, enabling them to clearly and accurately describe the characteristics of nanocarriers and related technologies using appropriate technical terminology. Finally, students will acquire the learning skills necessary to independently explore future developments in nanomedicine and pharmaceutical technology, fostering lifelong learning and interdisciplinary competence.