Drug Transport & Drug Delivery Systems, SDU (5ECTS), fall 2015 recommended reading draft last updated july 8th 2015 Topic Preformulation & Solid state Teacher Annette BauerBrandl Keywords Acid base properties, solubility, solvation, salt selection; partitioning and distribution revisited; Recommended reading Solid state Polymorphism, amorphous state, crystal energy, solid state-limited solubility, crystal engineering, industrial crystallization; Recommended basic knowledge (for repetition!) Aulton’s pharmaceutics. The design and manufacture of medicines 4th Edition. Churchill Livingstone/Elsevier, 2013, chapter 2: pp 126-134 chapter 20: pp 314-324 chapter 23: pp 382-390 Steffansen et al. (eds), Molecular Biopharmaceutics. Pharmaceutical Press 2009. Chapters 2.1 and 2.5 Lecture notes Chemical structure and bioavailability properties of drug candidates Elisabeth Christiansen Predicting the absorption of new structures (Lipinski´s rule of 5); in silico methods; chemical strategies to improve absorption (bio-isosteric replacement, prodrugs); Drug-like properties. Edward H. Kerns and Li Di. Elsevier, 2008 (e-book available at SDU-library) Chapter 5: pp 43-47 Chapter 8.3: pp 92-98 Lecture notes Topic Skin as biological barrier Transdermal delivery Teacher Judith Kuntsche Keywords Models to study skin permeability; transdermal patches Recommended reading In vitro diffusion cells Hanady Akram Bibi Franz cell studies Aulton’s pharmaceutics. The design and manufacture of medicines 4th Edition. Churchill Livingstone/Elsevier, 2013, chapter 39: pp. 683-685. Steffansen et al.(eds), Molecular Biopharmaceutics. Pharmaceutical Press 2009. Chapter 3.2.1 and 3.2.2 (pp 135-141) Calculation of flux and Papp Buccal & mucoadhesive dosage forms Judith Kuntsche Buccal & muco-adhesive dosage forms Topic Intestinal permeability screening Teacher Martin Brandl Preclinical evaluation of carrier-mediated transport Bente Steffansen Keywords Approaches to assess / predict uptake from gastro-intestinal tract, in vitro and in situ; Caco-2, HT-29, PAMPA, PVPA-model Biopharmaceutics classification system Membrane transporters in drug delivery. Methods to characterize transporter-mediated permeability. Preclinical investigation of drug/druginteraction on transporters Aulton’s pharmaceutics. The design and manufacture of medicines 4th Edition. Churchill Livingstone/Elsevier, 2013, chapter 39: pp. 679-683; 685-696. Buccal drug delivery. J.D. Smart. Expert Opin. Drug Del. 2 (2005) 507-517. The basis and underlying mechanisms of mucoadhesion. J.D. Smart. Adv. Drug Del. Rev. 57 (2005) 15561568. Recommended reading Aulton’s pharmaceutics. The design and manufacture of medicines 4th Edition. Churchill Livingstone/Elsevier, 2013, chapter 21: pp. 334-342 & 353-354 Steffansen et al. (eds), Molecular Biopharmaceutics. Pharmaceutical Press 2009. Chapter 3.7 pp 225-239 Steffansen et al., Molecular Biopharmaceutics. Pharmaceutical Press 2009. pp 153-173 & 193223 Nice to know: Maeda K and Sugiyama Y (2013) Transporters biology in drug approval: regulatory aspects, Mol Aspects Med. 34, 711-8 Topic Formulations for poorly soluble drugs Micro- & nanoparticles Teacher Martin Brandl Keywords Formulations for poorly soluble drugs: Nano-crystals, amorphous solid dispersions, S(M/N)EDDS, microemulsions, lipolysis, FaSSiF, FeSSiF, Solubility-/permability-interplay Recommended reading Buckley et al. European Journal of Pharmaceutical Sciences 50 (2013) 8–16 Lecture notes Modified release oral dosage forms Annette BauerBrandl Modified-release oral drug delivery Aulton’s pharmaceutics. The design and manufacture of medicines 4th Edition. Churchill Livingstone/Elsevier, 2013, chapter 31: pp. 550-565. Biopharmacy & pharmacokinetics Carsten Uhd Nielsen Pharmacokinetics; in vitro in vivo correlation Aulton’s pharmaceutics. The design and manufacture of medicines 4th Edition. Churchill Livingstone/Elsevier, 2013, Chapter 21: pp 344-354 chapter 22: pp. 355-366. Clinical aspects of drug transport Kim Brösen The interplay of drug absorption, disposition, metabolism and excretion; examples Brøsen et. Al (eds): Basal og Klinisk Farmakologi, 5. Udgave pp 58-63 Topic Inhalative dosage forms Teacher Martin Brandl Recommended reading Blood-brainbarrier Carsten Uhd Nielsen Keywords Physical and physiological aspects of drug deposition in the airways Pharmacopeial methods Formulations and technologies MDI, DPI, nebulizer BBB, pathways for CNS-drugs and drug delivery to the brain Liposomes Martin Brandl Aulton’s pharmaceutics. The design and manufacture of medicines 4th Edition. Churchill Livingstone/Elsevier, 2013, chapter 37: pp. 634-656. And lecture notes. Begley, D.J. Delivery of therapeutic agents to the central nervous system: The problems and the possibilities (2004) Pharmacology and Therapeutics, 104 (1), pp. 29-45. M. Brandl Liposomes as drug carriers: a technological approach In: Biotechnology Annual Review. M.R. El-Gewely, editor Volume 7: pp 59-85. Elsevier 2001 Lecture notes