Unit PREFORMULATION AND MODIFIED RELEASE SYSTEMS - DELIVERY AND DIRECTION OF DRUGS
- Course
- Industrial pharmacy
- Study-unit Code
- A003601
- Location
- PERUGIA
- Curriculum
- In all curricula
- Teacher
- Maurizio Ricci
- CFU
- 13
- Course Regulation
- Coorte 2023
- Offered
- 2024/25
- Type of study-unit
- Obbligatorio (Required)
- Type of learning activities
- Attività formativa integrata
PREFORMULATION AND MODIFIED RELEASE SYSTEMS
| Code | A003602 |
|---|---|
| Location | PERUGIA |
| CFU | 7 |
| Teacher | Maurizio Ricci |
| Teachers |
|
| Hours |
|
| Learning activities | Caratterizzante |
| Area | Discipline tecnologiche normative e economico-aziendali |
| Academic discipline | CHIM/09 |
| Type of study-unit | Obbligatorio (Required) |
DRUG DELIVERY AND TARGETING
| Code | 65013306 |
|---|---|
| Location | PERUGIA |
| CFU | 6 |
| Teacher | Aurelie Marie Madeleine Schoubben |
| Teachers |
|
| Hours |
|
| Learning activities | Caratterizzante |
| Area | Discipline tecnologiche normative e economico-aziendali |
| 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 physics with elements of informatics and Physical Chemistry examinations. 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. Laboratory exercises on methods of preparation of micro- and nano-particle carriers and their characterization. The slides used in class are provided to the students as well as papers. |
| Other information | |
| 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: 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. |
| 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. Laboratories: Preparation of MLV liposomes with the Thin Layer Evaporation method using the DPPC. Dimensional analysis of MLVs obtained with the SPOS technique - use of the Accusizer Particle Sizing System instrument, Preparation of albumin nanoparticles with the phase coacervation and thermal crosslinking method, dimensional analysis of albumin NPs prepared with the phase coacervation technique. Preparation of liposomes containing alizarin red dye by the ethanol injection method. Dialysis of liposomes prepared for solvent injection and UV-vis analysis of the dialysate to determine the liposome encapsulation efficiency. Acyclovir loaded oil entrapped calcium alginate beads: ionotropic gelation method. Preparation of Eudragit nanoparticles loaded with acyclovir, dimensional analysis and freezer-drying. In vitro release study of acyclovir from Eudragit nanoparticles and analysis by UV-Vis spectrophotometer to determine the concentration. Preparation of hydrogels with CMC and sodium hyaluronate. |
| Obiettivi Agenda 2030 per lo sviluppo sostenibile | Health and wellness |