91061 - Pharmaceutics II

Learning outcomes

Quality and technical evaluation of raw materials for the pharmaceutical use. Types of medicines, development strategies and regulatory activities, ICH and EMA guidelines related to the development and quality of a medicine. Biopharmaceutics, Bioavailability and delivery, pharmaceutical preformulation. Formulation technologies and industrial development for liquid / semi-solid pharmaceutical forms, aerosol. Mono-multi-particulate solid pharmaceutical forms, “fast release” formulations and “taste masking”. Solid oral dosage forms with modified release, dissolution test in formulation of a medicinal product. Paediatric and geriatric medicines Drug delivery and drug targeting, micro and nano - particle systems, liposomes, microemulsions, nanosuspensions, transdermal systems, bio / mucus-adhesive formulations. “gene-delivery” system. Studies on stability of medicines, pharmaceutical packaging, plastic materials and "leachables & extractables" studies.

Course contents

Module 1 – ADVANCED DRUG DELIVERY AND NANOTECHNOLOGY (Prof. Paolo Blasi, 6 CFU)

Drug Delivery e del Drug Targeting: rational - Brief introduction on the terminology (medicinal products, conventional and modified release formulation) and on biopharmaceutics. Micrometrics and nanometrics carriers in drug delivery and targeting. The dimensions of objects at the micro and nano scale. Possible routes of administration of for micro- and nanocarriers.

Materials employed in the development of modified release formulations. Monolitic and core-shell systems: structure, release kinetics and pros and cons. Modified release formulations for oral use (geomatrix, osmotic pumps, push-pull), ophthalmic formulations (ocusert e lacrisert) e Transdermal drug delivery systems: matrix type, reservoir and drug-in-adhesive.

Pharmaceutical microtechnologies - Pharmaceutical relevant microparticles and microcapsules: definitions, structures, and possible applications. Application of microparticles in the pharmaceutical field: materials, preparation methods and possible administration routes. Micrometric carriers prepared by lactic and glycolic acid polymers and co-polymers: production methods, structure, degradation and drug release. Examples of marketed medicinal products containing PLA/PLGA microparticles.

Pharmaceutical nanotechnologies and nanomedicine - Brief historical perspective on the evolution of pharmaceutical nanotechnology. The concept of drug targeting: EPR effect, passive and active targeting. General characteristics of pharmaceutical relevant nanocarriers: micelles, liposomes, dendrimers, metallic/metal oxide nanoparticles, lipid and polymer nanoparticles.

Liposomes: definition and classification. Phospholipid: structure, and thermotropic behaviour of phospholipid membranes. Liposomes in drug delivery and targeting. Main characteristics, production methods and loading of commercially available liposomal anthracycline formulations (Doxil^®/CAELYX^®, Myocet^® e DaunoXome^®).

Nanoparticles (NPs) in the drug targeting scenario. Polymeric NPs: definitions, polymer characteristics, structure and morphology, drug release modalities. Lipid nanoparticles. Lipid and methods to prepare lipid nanoparticles. Drug loading and release. mRNA delivery through lipid nanoparticles: the case of COVID-19 vaccines.

Medical devices: definition and legislation. The Regulation 2017/745. Medical device classification and re-classification of existing products. The borderline products and the new rules on borderline product identification. Medical devices sold in community pharmacies.

Module 2 - ADVANCED DRUG DELIVERY AND NANOTECHNOLOGY - Lab experiences (Dott.ssa Serena Bertoni) (2 CFU)

The practical exercises will focus on the preparation of conventional and advanced drug delivery systems (capsules, granules, tablets, emulsions, gels) and the application of the technological controls (uniformity of weight, dimensional analysis using sieves, angle of repose, hardness tester, friabilometer, disintegration and dissolution studies, pH and viscosity measurements) according to the Italian and European Pharmacopoeia. The practical excercises will also regard the development of innovative pharmaceutical forms, e.g. microparticles, by using different techniques.

Readings/Bibliography

P. Colombo et al., Principi di Tecnologia Farmaceutica, II Ed. CEA, 2015.

E. Aulton, et al., Tecnologie Farmaceutiche, EDRA, 2015.

J. Swarbrick, J.C. Boylan, Encyclopedia of Pharmaceutical Technology, Dekker, 1999-2005

R.C. Rowe et al., Handbook of pharmaceutical excipients, 6th ed. Pharmaceutical Press, 2009.

Lesson's notes.

Slides presented during the course can not be considered as a substitute of the reference texts suggested above.

Teaching methods

Lectures (module 1, 48 hours) and practical experience in the Galenic laboratory (module 2, 30 hours).

As concerns the teaching methods of this course unit, all students must attend Module 1, 2 [https://www.unibo.it/en/services-and-opportunities/health-and-assistance/health-and-safety/online-course-on-health-and-safety-in-study-and-internship-areas] online, while Module 3 on health and safety is to be attended in class. Information about Module 3 attendance schedule is available on the website of your degree programme.

Assessment methods

Oral exam on the content of the modues 1 and 2.

Teaching tools

Power Point presentations for the Module 1 and laboratory notes for the Module 2 (available in the University repository).

Office hours

See the website of Paolo Blasi

See the website of Serena Bertoni