Unit APPLIED PHARMACEUTICAL CHEMISTRY AND DRUG DELIVERY AND TARGETING
- Course
- Chemistry and technology of drugs
- Study-unit Code
- 65102613
- Location
- PERUGIA
- Curriculum
- In all curricula
- Teacher
- Maurizio Ricci
- CFU
- 13
- Course Regulation
- Coorte 2018
- Offered
- 2022/23
- Type of study-unit
- Obbligatorio (Required)
- Type of learning activities
- Attività formativa integrata
APPLIED PHARMACEUTICAL CHEMISTRY
| Code | 65004407 |
|---|---|
| Location | PERUGIA |
| CFU | 7 |
| Teacher | Maurizio Ricci |
| Teachers |
|
| Hours |
|
| Learning activities | Caratterizzante |
| Area | Discipline chimiche, farmaceutiche e tecnologiche |
| Academic discipline | CHIM/09 |
| Type of study-unit | Obbligatorio (Required) |
| Language of instruction | Italian |
| Contents | Biopharmaceutics and bioavailability; Physical and chemical stability of medicaments; Polymers; Drug Delivery Systems. |
| Reference texts | P. Colombo et al., Principi e Tecnologie Farmaceutiche, casa Editrice Ambrosiana, Milano A.T. Florence, D. Attwood, Le basi chimico-fisiche della tecnologia farmaceutica, EdiSES Remington’s Pharmaceutical Sciences Michael E. Aulton, Tecnologie Farmaceutiche Progettazione e allestimento dei medicinali. Edra Editore Argomenti di Tecnologia Farmaceutica (R. Calcinari Edizioni LINT, Trieste) Appunti delle lezioni e slides |
| Educational objectives | The purpose of the course is to provide students with the knowledge of the issues regarding the path of the drug from therapeutic idea to its registration, for their inclusion in research and pharmaceutical industry. In this multidisciplinary experience, particular importance is either the preformulation studies in the development of the drug and its goals such as bioavailability, stability and security, or the new methods and theoretical and practical approaches to modulate drug release from the formulation. Knowledge/understanding: The student will acquire the knowledge and methods that will enable him to study and think critically and independently the problems in the field of pharmaceutical technology with particular reference to the preformulation and industrial development of conventional and modified release dosage forms. Applying knowledge/understanding: The course provides the basis for the development of judgment and choice of the best technological approaches to the preparation of innovative pharmaceutical forms and conventional ones, with respect to the characteristics of the active ingredients and therapeutic purposes |
| Prerequisites | n order to understand and know how to apply most of the techniques described during the course, the student should possess sound knowledge of mathematics, physical chemistry, physiology, pharmacology, general and organic chemistry as well as the concepts in polymer chemistry. The course foresees, as a prerequisite, to have taken the Physics and Physical Chemistry examinations and it is advisable to have also taken the exams of Technology-Socio-economy, and pharmaceutical legislation, as well as Implantations of pharmaceutical industry. This is an essential pre-requisite for the student to be able to understand the benefits of innovative pharmaceutical forms and to have a better and broader vision of the organization of a pharmaceutical company and the process of research and development. Moreover, since this course, inevitably, involves aspects belonging to several disciplines, the student should have a good overview of the disciplines followed in previous years in order to make fast connections needed to follow the course with profit. |
| Teaching methods | Frontal lessons with help of projections on the screen and possibly the board. Each lesson begins with a brief summary of the concepts covered in the lessons immediately preceding and ends with a brief discussion in the classroom as assessment. Direct involvement of the students to the issues covered in them trying to develop an approach not only reactive but also proactive to the submitted problems. Some practical demonstrations in the classroom will be used to better set some concepts covered in theory. The slides used in class ar |
| Other information | Supplementary teaching activities as provided by teaching plan |
| Learning verification modality | The exam consists of a oral test, inherent the entire program, taking care to subject the student to at least two questions for each module of the course: 1. A question aimed at ascertaining the level of knowledge and understanding achieved by students on the theoretical and methodological implications listed in the program; this type of question will also test the student communication skills and his autonomy in the organization of the exposure of the theoretical topics, necessary to address any exposure of its search results in various contexts, from academia to industry; 2. A question of logic that aims to understand whether the student is able to make those correlations necessary to develop a specific project formulation based on the type of drug and therapeutic needs. This second type of evaluation is sometimes carried out showing the student publications concerning the topic on which readies the discussion. This is crucial to help the student to address a "case study" in a rational and constructive way while it forces him to apply all the knowledge acquired in previous teachings. Moreover, the student get used to a type of interview that some pharmaceutical industries use in the selection of candidates. |
| Extended program | Part A Some principles of pharmacokinetics and "biopharmaceutical" aspects necessary for the understanding of the disposition parameters and choosing the right formulation and route of administration of a drug. Approach to the development of a medicinal product: from the idea to the realization of a therapeutic pharmaceutical product. Preformulation studies in the development of the drug. Physical-chemical properties. Physical principles of pharmaceutics and biopharmaceutics. Solubility, lipophilicity, dissociation constant, logP. Solid state: amorphous and crystal polymorphism. Diffusion and Fick's law; dissolution rate and Noyes Whitney law. Formulation Development Stability of pharmaceutical formulations: chemical decomposition of the active ingredients and kinetic aspects of chemical decomposition in solid phase and in solution; regular tests of stability, accelerated tests of stability: isothermal method of Garret. Colloidal systems: general properties, classification and methods of preparation; DLVO theory and PZ concept in assessing the stability of colloidal dispersions. Part B Polymers in modified release formulations General: definitions and properties, molecular weight, degree of polymerization and crystallinity. Classification of polymers, synthetic and natural polymers of pharmaceutical interest and modified natural polymers. Modified release Systems Logic: release kinetics of the active ingredient; reservoir systems and matrix systems. Classification of modified release systems: controlled systems, diffusion controlled systems, chemically activated systems, solvent activated systems, swellable systems; development of a pharmaceutical form prolonged release. Oral modified release Systems: DIFFUTAB Technology, multiple unit systems, Microcaps Technology, Diffucaps Technology, MiniTabs, orodispersible Systems (OTD - Orally Disintegrating Tablets), Geomatrix, Pennkinetic Technology, elementary osmotic pumps and OROS push-pull, L-Oros, gastroretentive systems. Transdermal patches. Iontophoresis |
DRUG DELIVERY AND TARGETING
| Code | 65013306 |
|---|---|
| Location | PERUGIA |
| CFU | 6 |
| Teacher | Aurelie Marie Madeleine Schoubben |
| Teachers |
|
| Hours |
|
| Learning activities | Caratterizzante |
| Area | Discipline chimiche, farmaceutiche e tecnologiche |
| Academic discipline | CHIM/09 |
| Type of study-unit | Obbligatorio (Required) |
| Language of instruction | Italian |
| Contents | General concepts of DRUG TARGETING and deepening of micro- and nanoparticulated carriers from a structural, formulative and applicative point of view. Methods of analysis of their physical chemical properties. |
| Reference texts | P. Colombo et al., Principi e Tecnologie Farmaceutiche, casa Editrice Ambrosiana, Milano A.T. Florence, D. Attwood, Le basi chimico-fisiche della tecnologia farmaceutica, EdiSES Remington’s Pharmaceutical Sciences Michael E. Aulton, Tecnologie Farmaceutiche Progettazione e allestimento dei medicinali. Edra Editore Argomenti di Tecnologia Farmaceutica (R. Calcinari Edizioni LINT, Trieste) Appunti delle lezioni e slides |
| Educational objectives | The purpose of the course is to provide students with the knowledge of issues related to the concept of site-specific direction of the drugs in order to identify the advantages and limitations offered by the various carriers. In such formative experience multidisciplinary studies are of particular importance preformulation in the development of the drug and its objectives such as bioavailability, stability and safety, and new approaches and approaches theoretical-practical to affect the release and to convey and direct the drugs. Knowledge / Knowledge: Students will acquire those knowledge and skills methodologies that will allow him to study and reason critically and independently in the field of pharmaceutical technology with particular reference to the formulation and to the industrial development of non-traditional and modified release site specific dosage forms. Ability to Know: The course puts the foundation for capacity building evaluation and choice of the best technological approaches to the design of innovative pharmaceutical forms, with respect to the characteristics of active compounds and therapeutic purposes. |
| Prerequisites | In order to understand and know how to apply most of the techniques described during the course, the student should possess sound knowledge of mathematics, physical chemistry, physiology, pharmacology, general and organic chemistry as well as the concepts in polymer chemistry. The course foresees, as a prerequisite, to have taken the Physics and Physical Chemistry examinations and it is advisable to have also taken the exams of Technology-Socio-economy, and pharmaceutical legislation, as well as Implantations of pharmaceutical industry. This is an essential pre-requisite for the student to be able to understand the benefits of innovative pharmaceutical forms and to have a better and broader vision of the organization of a pharmaceutical company and the process of research and development. Moreover, since this course, inevitably, involves aspects belonging to several disciplines, the student should have a good overview of the disciplines followed in previous years in order to make fast connections needed to follow the course with profit. |
| Teaching methods | Frontal lessons with help of projections on the screen and possibly the board. Each lesson begins with a brief summary of the concepts covered in the lessons immediately preceding and ends with a brief discussion in the classroom as assessment. Direct involvement of the students to the issues covered in them trying to develop an approach not only reactive but also proactive to the submitted problems. Some practical demonstrations in the classroom will be used to better set some concepts covered in theory. The slides used in class are provided to the students as well as papers. |
| Other information | Supplementary teaching activities as provided by teaching plan. |
| Learning verification modality | The exam consists of a oral test, inherent the entire program, taking care to subject the student to at least two questions for each module of the course: 1. A question aimed at ascertaining the level of knowledge and understanding achieved by students on the theoretical and methodological implications listed in the program; this type of question will also test the student communication skills and his autonomy in the organization of the exposure of the theoretical topics, necessary to address any exposure of its search results in various contexts, from academia to industry; 2. A question of logic that aims to understand whether the student is able to make those correlations necessary to develop a specific project formulation based on the type of drug and therapeutic needs. This second type of evaluation is sometimes carried out showing the student publications concerning the topic on which readies the discussion. This is crucial to help the student to address a "case study" in a rational and constructive way while it forces him to apply all the knowledge acquired in previous teachings. Moreover, the student get used to a type of interview that some pharmaceutical industries use in the selection of candidates. |
| Extended program | Introduction to the course: drug targeting rationale. Biological processes involved in the in vivo fate of carriers. Pegylation: mechanism and PEG properties. Drug targeting schemes. Liposomes: definition and composition, the phospholipids: structure, properties, bilayer thermotropic behaviour and importance of the main transition temperature. Influence of the type of phospholipid on the main transition temperature, cholesterol effect on the bilayer fluidity. Liposome classification according to their dimensions and to the number of layers, characteristics of MLV, LUV and SUV, liposome preparation methods: thin layer evaporation and reverse phase evaporation vesicle, the use of extrusion and high pressure homogenization. Liposome loading methods: freeze-thawing and concentration gradient loading.Liposome quality controls, liposome purification methods. Liposome applications: formulation, diagnosis and drug delivery. Liposome administration routes: the oral route. Liposome topical applications: ocular and skin applications. Liposome endovenous application: conventional liposomes, SUV, pegylated liposomes, imunoliposomes, AmBisome, marketed antitumor liposomal formulations. Strategies using hyperthermy and liposomes. Niosomes: composition, advantages with respect to liposome, HLB, critical packing parameter. Niosome preparation methods, niosome applications in cosmetics and as drug carrier (retinoic acid and oestradiol). Polymeric nanoparticles: definition and structures, administration routes: the importance of the oral route and the absorption at the Peyer patches. Polymers used for nanoparticles preparation: biodegradation and bioerosion and its influence on polymeric nanoparticle toxicity. Polymeric nanoparticle preparation methods: frompreformed polymers or monomers. Preparation methods using preformed polymers: water-in-oil method or coacervation for hydrosoluble polymers, oil-in -water emulsion (spontaneous or not) and solvent evaporation method for liposoluble polymers. Preparation methods from monomers: emulsion and solution polymerization (alkyl methacrylate and alkyl cyanoacrylate). Advantages and disadvantages of the different preparation methods and drug loading.Supercritical fluids for the preparation of polymeric particles.Polymeric nanoparticle applications and characterization. SLN introduction: advantages with respect to the other colloidal carriers. Bulk materials used for their preparation and hot and cold high pressure homogenization method used for their production. Use of the probe sonication as alternative solution to the homogenization. SLN: supercooled melts, lipid polymorphism, SLN shape and the gelification problem. Alternative carriers: NLC (nanostructured lipid carriers) e LDC (lipid drug conjugate) to improve drug loading and stability. SLN applications: cutaneous applications for cosmetic use (adhesivity, occlusion and hydration effect, cosmetic active principle delivery, marketed formulations) and pharmaceutical use (strategy that uses NLC instead of SLN, why and how it works). SLN: oral use and lymphatic absorption, parenteral use. Dendrimers: nanoparticulate biomaterial, definition, description, conventional synthesis methods, divergent and convergent synthesis, drug location in the dendrimers (cavity, generation flexibility). New strategies for dendrite synthesis. Dendrimer applications: nanocarrier, nanoscaffold and nanodrug. Dendrimer biocompatibility and toxicity. Colon drug delivery: description and pathologies affecting the colon, the pro-drug strategy to target drug to the colon (azo link, glucosides, amido-aminoacid, cyclodextrins, polymers). The use of pH sensible polymers for drug colon delivery, Eudragit properties and applications. Peptide and protein pulmonary delivery: pulmonary administration potentialities, anatomy and preservation mechanisms of the airways, particle deposition mechanisms and characteristics that particles should possess to reach the lung. Local or systemic therapy: Drug in solution or powder (the use of lactose as carrier). The pharmaceutical technology in the lung delivery: liposomes, large porous particles, biodegradable polymeric particles. Polymeric nanoparticles and solid lipid nanoparticles for brain drug delivery. Anatomy and characteristics of the blood-brain barrier, possible mechanisms od nanoparticle delivery to the brain, Comparison between polymeric and solid lipid nanoparticles used to deliver drug to the brain: preparation methods, degradation and toxicity, surfactant effect, drug loading. Nanocrystals. |