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School of Medicine
CHEMISTRY AND PHARMACEUTICAL TECHNIQUES
Course unit
TECHNOLOGY OF TARGETING AND CONTROLLED RELEASE OF DRUGS
MEP3052593, A.A. 2018/19

Information concerning the students who enrolled in A.Y. 2014/15

Information on the course unit
Degree course 5 years single cycle degree in
CHEMISTRY AND PHARMACEUTICAL TECHNIQUES
FA1733, Degree course structure A.Y. 2009/10, A.Y. 2018/19
N0
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Number of ECTS credits allocated 6.0
Type of assessment Mark
Course unit English denomination TECHNOLOGY OF TARGETING AND CONTROLLED RELEASE OF DRUGS
Department of reference Department of Pharmaceutical and Pharmacological Sciences
E-Learning website https://elearning.unipd.it/dsf/course/view.php?idnumber=2018-FA1733-000ZZ-2014-MEP3052593-N0
Mandatory attendance
Language of instruction English
Branch PADOVA
Single Course unit The Course unit CANNOT be attended under the option Single Course unit attendance
Optional Course unit The Course unit can be chosen as Optional Course unit

Lecturers
Teacher in charge STEFANO SALMASO CHIM/09

ECTS: details
Type Scientific-Disciplinary Sector Credits allocated
Core courses CHIM/09 Applied Technological Pharmaceutics 6.0

Course unit organization
Period First semester
Year 5th Year
Teaching method frontal

Type of hours Credits Teaching
hours
Hours of
Individual study
Shifts
Laboratory 2.0 30 20.0 No turn
Lecture 4.0 32 68.0 No turn

Calendar
Start of activities 01/10/2018
End of activities 18/01/2019

Examination board
Board From To Members of the board
6 Commissione a.a. 2018/19 01/12/2018 30/09/2019 SALMASO STEFANO (Presidente)
CALICETI PAOLO (Membro Effettivo)
MORPURGO MARGHERITA (Supplente)
PASUT GIANFRANCO (Supplente)

Syllabus
Prerequisites: Students are required to possess the basic concepts and terminology regarding organic chemistry, organic synthesis, pharmaceutical technology and drug formulation, conventional pharmaceutical dosage forms. The students should pay special attention to physics related to dosage forms and the aspects that dictate the physico-chemical stability, the dissolution behavior, the absorption mechanisms of drugs. It is relevant to understand the main features and advantages offered by the most common synthetic and natural polymers used for drug formulation. Knowledge of the basics of human anatomy and physiology of biological barriers (cell membranes, mucosa, skin and intestinal epithelium architecture etc.) is mandatory.
The students already should have knowledge about the basic concepts of pharmacology (pharmacokinetics, pharmacodynamics) and the terms used in the pharmaceutical technology.
It is required that the students comprehend spoken and written English to understand the slides shown during the lectures, the papers and scientific textbooks to which the teacher refers. The slides used by the teacher and the lectures are provided only in English.
Target skills and knowledge: The student will be guided to learn the therapeutic relevance of controlled drug delivery strategies to ameliorate the biopharmaceutical properties of marketed and new drugs, the most diffused strategies to control the release of drugs from matrices and micro- and nano-carriers, the relevance of designing pharmaceutical dosage form for controlled drug delivery according to scientific principles. At the end of the course the student is aware that, by controlling peculiar features of the delivery system and by using adequate formulation strategies, the rate of drug absorption can be controlled, which allows, ultimately, for the delivery of drugs to the target tissues and reduce their side effects. The student will learn the properties and formulation strategies of the most common dispersed and colloidal systems for the delivery of drugs.
The student learns which polymers and excipients may be employed for the preparation of dispersed systems and which features are required to each component to play its activity. The student will be guided through the last generation of commercialized and “under-development” nanotechnological platforms employed for the delivery of drugs. The student will learn the required features of nanoparticulate systems for the delivery and the controlled release of drugs. The students will understand the major techniques to perform the physical and pharmaceutical characterization of these systems. The student is exposed to the innovative dosage forms for the drug administration via unconventional routes that guarantees improved absorption (transdermal, transmucosal). The student will learn when it is desired to use controlled release systems to ensure delivery and therapeutic effect of chemically instable drugs.
Examination methods: The exam is oral. The teacher reserves the possibility to perform the exam in written mode.
The exam includes a scientific report of the student concerning the practical laboratory experiences performed during the course. The report structure is the same of a scientific paper (Abstract, introduction, material and methods, results, discussion) and the student has to write down this report together with the other students of the bench group.
The exam is also made up of at least 3 open questions regarding the topics covered during the lectures.
The exam is only in English.
The exam sections are scheduled within the appropriate official examination sessions. Extraordinary exam sections can be scheduled at the discretion of the teacher.
The student who does not pass the exam may recur to the closest exam section after a period of at least three weeks.
Assessment criteria: The exam aims to assess the knowledge gained by the candidate according to the scopes of the course and its content. The professor will evaluate of the student possesses:
-knowledge about the features that affect drug release profile from a colloidal delivery system
-knowledge of colloidal carriers and the requirements to generate performing nanotechnological systems
- capacity to identify the critical points in the formulations of delicate drugs
-knowledge of polymers, excipients, and their role in the preparation of innovative systems for the delivery of drugs
-knowledge of the properties and advantages offered by alternative routes of administration, and the formulation requirements to exploit such routes for drug controlled release.

The student is expected to show that he/she has learned the critical issues in the preparation of advanced systems for the delivery of drugs. The laboratory report will challenge the student to show that he/she has acquired the knowledge to manipulate, prepare and characterize novel platforms for the controlled release of drugs. Particular remark will be given to the student's ability to integrate and correlate critically the theoric concepts provided during the lectures with the practical experience in teaching laboratory.
Course unit contents: 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.
Planned learning activities and teaching methods: The learning activity takes place in 32 hours of lectures and 30 hours of practical laboratory. The teacher will lecture using slides in English only. Slides have been prepared using information from textbooks and from recent scientific publications.
Students will learn the relevance of the design of a pharmaceutical formulation for drug controlled release to ensure the performance and biopharmaceutical behavior of the final product. The course aims at guiding students to understand why, once the drug features are known from pre-formulation studies and the route of administration has been chosen, it is crucial to endow the delivery system with defined features that ensure that the biopharmaceutical behavior, site-specific drug delivery and controlled release take place according to a robust design. The formulation features are dictated by the materials and excipients used, the process of production, the size, the morphology, the surface properties, the environmental responsiveness of the carrier.
Students will be guided through the main colloidal systems and “smart” systems available on the market (or under development) for the administration of drugs. Students will be exposed extensively to all the issues related to colloidal systems, the physico-chemical characterization techniques, the most performing materials and polymers conventionally used to prepare drug nanocarriers, how to ensure their stability and performance and how to choose components with technological role.
Through the learning activities, the students will acquire the necessary knowledge to play an active role in the field of pharmaceutical formulations for the design, set up and development of innovative drug delivery systems of the future. The knowledge acquired along this course will be relevant both for accademic and industrial carrier.
Teaching activities in the practical laboratory will take place through the teacher’s step-by-step description of the procedures to prepare the controlled release formulations described in the “Contents” chapter. Students will be guided to acquire the ability to independently organize the preparation of those carriers based on a written tutorial and will be exposed to the strategies to prepare and characterize few nanotechnological systems for drug delivery. Team cooperation is mandatory in the practical laboratory which will stimulate the ability of students to share information, coordinate tasks, act alternatively as leaders and under guidance of a group leader.
Additional notes about suggested reading: The students can study the course content using the slides presented during the lectures.
Information about the topics presented during the in classroom lectures can also be (in part) found on the textbooks provided below. Students can refer to those textbooks to support their study activity.
Textbooks (and optional supplementary readings)
  • Juergen Siepmann, Ronald A. Siegel, Michael J. Rathbone Editors, Fundamentals and Applications of Controlled Release Drug Delivery. New York: Springer, 2012. Cerca nel catalogo
  • Wise, Donald L. Editor, Handbook of Pharmaceutical Controlled Release Technology. New York: Marcel Dekker Inc, 2000. Cerca nel catalogo
  • Melgardt M. de Villiers, Pornanong Aramwit, Glen S. Kwon Editors, Nanotechnology in Drug Delivery. New York: Springer, 2009. Cerca nel catalogo
  • Xiaoling Li, Ph.D. Bhaskara R. Jasti, Ph.D. Editors, Design of Controlled Release Drug Delivery Systems. New York: McGraw-Hill, 2006. Cerca nel catalogo

Innovative teaching methods: Teaching and learning strategies
  • Lecturing
  • Laboratory
  • Problem based learning
  • Working in group
  • Questioning
  • Problem solving
  • Flipped classroom
  • Work-integrated learning
  • Loading of files and pages (web pages, Moodle, ...)

Innovative teaching methods: Software or applications used
  • Moodle (files, quizzes, workshops, ...)

Sustainable Development Goals (SDGs)
Good Health and Well-Being Quality Education Industry, Innovation and Infrastructure