Raimar Loebenberg, PhD, Director DDIC

Area of Study / Keywords

ivivc dissolution PBPK biopharmaceutics nanoparticle

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About

Bio

Dr. Löbenberg holds a BSc in pharmacy from the Johannes Gutenberg-University in Mainz, Germany. He received his PhD in pharmaceutics from the Johann Wolfgang Goethe-University in Frankfurt in 1996. He joined the University of Alberta in 2000. 

His research interests are in Biopharmaceutics to predict the oral performance of drugs and botanicals and inhalable nanoparticles to treat lung diseases like cancer or tuberculosis. 

He is founder and director of the Drug Development and Innovation Centre at the University of Alberta. 

He was president of the Canadian Society for Pharmaceutical Sciences 2014 & 2015.

He is member of the United States Pharmacopeia Dietary Supplement Expert Committee. 

He is Vice Chair of the Specialty Committee of Traditional Chinese Medicine in Pharmaceutics of the World Foundation of Chinese Medicine Science. 

He is member of the Health Canada Scientific Advisory Committee on Pharmaceutical Sciences and Clinical Pharmacology.

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Research

Inhalable Nanoparticles for Pulmonary Drug Delivery of Anti-Cancer Drugs: This collaborative research involves experts from Engineering, Medicine, and Pharmacy. The initial publication from this project received the Most Cited Award from the International Journal of Pharmaceutics in 2004. Subsequently, we have published numerous review articles and research papers, delivered invited talks at national and international conferences, and organized workshops and symposia on this subject. We have secured one patent and filed another patent application. In 2011, we published research highlighting the preclinical application and high potential of this delivery platform, demonstrating its superior efficacy in lung cancer treatment compared to other administration routes.

BCS-Based Development of In Vitro/In Vivo Correlations Using Biorelevant Dissolution Techniques and Computer Simulations: This research earned myself the American College of Clinical Pharmacology (ACCP) New Investigator Award in 2001 and has received support from industry partners. It has resulted in numerous publications and presentations at prestigious events, including Merck Frosst's annual research day, Food and Drug Administration (FDA)- American Association of Pharmaceutical Scientists (AAPS) workshops, AAPS annual conferences, the Canadian Society for Pharmaceutical Sciences annual conference, SINDUSFARMA (Brazil) workshops, the Pharmaceutical Technology Society of Korea, AAPS outreach workshops in Africa and Argentina. Currently this work was extended and includes lysosomal trapping and lymphatic uptake and its contribution to bioavailability. Models were developed to predict if a drug or drug formulation can be targeted to the lymphatic system.

Quality by Design and Performance Testing: Our work on this topic has been published in various journals, including the AAPS Journal. We have presented our findings at conferences and workshops in countries such as Brazil, China, South Korea, and Canada, as well as to the USP expert committee on performance testing. Our contributions have even led to changes in the USP specifications for the disintegration test.

Formulation Development and Novel Processes: Our laboratory has published research on various processes and formulation approaches, including process analytical technology. In a project sponsored by the USP, we investigated blending sequences involving an Active Pharmaceutical Ingredient (API) and two excipients. The results revealed that the dissolution properties of specific tablets may change depending on the blending sequences before compression. We developed a microemulsion system for topical delivery of diclofenac sodium. The formulation showed superb pain relieve in 10 out of 11 patients. In another clinical trial over 50% pain relieve was observed within 28 diays of treatment of osthooarthitis knees. The formulation is now commercialized under the Trademark FoamaDermä and sold in Canada and the USA. A monograph was developed and submitted for publication in the USP.

Traditional Chinese Medicine (TCM) and Natural Health Products: The Drug Development and Innovation Centre actively engages in translational research to design and develop modern Natural Health Products. Our research is disseminated through workshops, symposia, and several published manuscripts. The center has also conducted several clinical trials involving dosage forms and developed prototypes for products that are currently commercialized.

Medical Cannabis and Psycodelic Drugs: Our laboratory is well-versed in the evaluation of medical cannabis. We have developed analytical assays and extraction methods for major cannabinoids, as well as conducted all the necessary tests mandated by Health Canada, such as pesticide, heavy metal, and residual solvent analysis. Our primary focus revolves around formulating medical cannabis into contemporary dosage forms, offering therapeutic alternatives to smoking. It's worth noting that we hold a Controlled Substance license, enabling us to synthesize Psylocybin, Mescaline, and MDMA. Our laboratory has also pioneered the development of novel molecules designed to enhance the bioavailability of Psilocin, the active form of the prodrug Psilocybin.  We are also licenced to supply the Special Access Program of Health Canada with Pilocybin and MDMA caspules. We have developed new film strip technology for the oral delivery of these substances to provide an improved easy to administer drug delivery system besides the classical dosage forms.

Specialized routes of administration: lysosomal trapping of basic compounds is known for a long time. However, no dissolution method existed to simulate this known fenomen. Basic drugs get entrapped in lysosomes while passing though an eneroocyte because the interna pH of the lysosomes is lower compared to the cytoplasma. This increses the aequous solubility of the basic drug inside the lysosome. Therefore, it takes now longer for the durg to partition out of the lysosome to continues its way to the blood and getting systemically absorbed. Our group has developed a lysosomal dissolution model to simulate this pathway.

Besides the lysosomal pathway there is another not well studied absorption pathway within the cytoplasma of an ernterocyte. The apical membrane of an enterocyte can diffentiate between mid chain and long chain fattyacids. Long chain fatty acids are aborbed intact and can be assembled into chylomicrons in the cytoplasma. Chylomicrons are small lipid rich particles originating in the cytoplasma. The chylomicrons are then excreted into the lymphatic floid outside the enterocytes rather then absorbed into the blood. Drug like molecules can also be packed into the chylomicrons if they have certain physicochemical properties like a Log D at the physicological pH of over 5. However, literature and our in vitro model shows that factors like nature of faty acids, excipients and suractants can highly influence the incorporation of molecules into chylomicrons. Our group has developed the first in vitro dissolution method which can be used to screen drug formualtions in regard to their ability to either increase or block lymphatic uptake of drugs. This is an important because many modern delivery systems for poorly soluble drugs use lipid-based formulations and at this moment it is not known if they promote or inhibit lymphatic uptake. The drug fraction which is lymphtically absorbed is not undergoing first pass metabolism. Therefore, for certain highly metaolized drugs this pathway can significantly increase their overall bioavialablity.

Nasal delivery is gaining attention for the administration of vaccines and other therapeutic moetis like ketamine. The nasal route of administration offers an alternative way to reach the brain without the need to overcome the blood brain barrier. Our group published the first physiologically relevant nasal fluid. We are currently investigating dissolution models to mimic nasal drug delivery. Such methods might be crucial for especially micordosing of psichodelic compounds. The nasal route of administration offers a convenient alternative to the oral route and its potential for brain targeting has to be further investigated.

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Teaching

Undergraduate Lectures: I deliver instruction on pharmaceutical compounding and fundamental principles in pharmaceutics to a cohort of 130 first and second-year undergraduate students. The topics covered for first-year students encompass Pharmacopeial Compounding Standards such as USP Chapter 795, Stability Considerations in Dispensing Practice 1191, Compounding of Powders, Capsules, Suppositories, Solutions, Pharmaceutical Waters, Suppository Bases, Herbal Extraction Processes, Container Materials, and Closures. Second-year students, on the other hand, delve into Sterile Compounding following USP 797 guidelines, Sterilization Methods, Parenteral Dosage Forms, Granulation Processes, Tablets, Film Coating, Quality Control, Pharmaceutical Performance Tests, Biopharmaceutics, Biowaivers, Controlled Release, New Drug Development and the Drug Approval Process, Natural Health Products, and Future Dosage Forms.

Laboratory: The laboratory component takes place two times a week, with each session lasting for 3 hours. First-year students receive practical training in non-sterile liquid, solid, and semi-solid dosage forms. They learn about the production, documentation, and quality control of these forms in licensed public pharmacies. For second-year students, laboratory sessions focus on low-risk manipulations of sterile products, dissolution testing, compounding of complex topical formulations, and biopharmaceutical simulations to close the gap between theroretical knowledge and clinical relevance.

PHARM 202 - Pharmaceutics 1

Introduces students to the principles of pharmaceutical dosage forms. This course will focus on factors affecting the physical and chemical behavior of drug products, the rationale underlying their formulation, and compounding techniques of pharmaceutical preparations. (Restricted to Pharmacy students.)

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PHARM 599 - In Silico Drug Development

This course is an introduction into Physiologically Based Biopharmaceutic Modeling (PBBM) and physiologically based pharmacokinetic (PBPK) modeling, relevant to modern drug development and regulatory biowaivers. The core pharmaceutical scientific focus is on understanding basic and advanced physical chemical, biopharmaceutic and pharmacokinetic principles through physiological based modeling approaches. The graduate and undergraduate students will actively engage with contemporary modeling software, concurrently learning both the pharmaceutical foundations and practical operation of the software and how this can be used in further mechanistic drug development and for regulatory applications. An appreciation of in silico drug development is important for both in order to develop a thorough understanding of physicochemical and biopharmaceutical principles and advanced concepts such as: in vitro in vivo correlation, bio-relevant dissolution and disposition phenomena and special populations. Prerequisites: Undergraduate students: Pharm 302 and 315 (pharmaceutics 2 and pharmacokinetics). Graduate students: pharmacy degree (M.Sc., PharmD) or equivalent with exposure to pharmaceutics and pharmacokinetics as undergraduate students or with consent from the faculty.

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Browse more courses taught by Raimar Loebenberg

Malaz Yousef, Chulhun Park, Nadia Bou Chacra, Neal M. Davies, Raimar Löbenberg

AAPS PharmSciTech. 2024 August; 10.1208/s12249-024-02866-y

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Malaz Yousef, Jaime A. Yáñez, Raimar Löbenberg, Neal M. Davies

Biomedicines. 2024 August; 10.3390/biomedicines12081843

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Malaz Yousef, Conor O’Croinin, Tyson S. Le, Chulhun Park, Jieyu Zuo, Nadia Bou Chacra, Neal M. Davies, Raimar Löbenberg

Pharmaceutics. 2024 June; 10.3390/pharmaceutics16060768

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Eakkaluk Wongwad, Kornkanok Ingkaninan, Neti Waranuch, Chulhun Park, Vijay Somayaji, Nat Na-Ek, Raimar Löbenberg

Journal of Drug Delivery Science and Technology. 2024 June; 10.1016/j.jddst.2024.105697

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Luca Maurice Richter, Jozef Al-Gousous, Gabriel Lima Barros de Araujo, Neal M. Davies, Raimar Löbenberg

Journal of Drug Delivery Science and Technology. 2024 February; 10.1016/j.jddst.2023.105305

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Malaz Yousef, Chulhun Park, Mirla Henostroza, Nadia Bou Chacra, Neal M. Davies, Raimar Löbenberg

Pharmaceutics. 2023 October; 10.3390/pharmaceutics15112532

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Chulhun Park, Jieyu Zuo, Myung-Chul Gil, Raimar Löbenberg, Beom-Jin Lee

Pharmaceutics. 2023 October; 10.3390/pharmaceutics15112533

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Daniela Amaral Silva, M. Kenneth Cor, Afaseneh Lavasanifar, Neal M. Davies, Raimar Löbenberg

Pharmacy Education. 2022 May; 10.46542/pe.2022.221.336347

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Braa Hajjar, Jieyu Zuo, Chulhun Park, Shirzad Azarmi, Daniela Amaral Silva, Nádia Araci Bou-Chacra, Raimar Löbenberg

AAPS PharmSciTech. 2022 May; 10.1208/s12249-022-02258-0

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Nicolas van Bavel, Patrick Lai, Raimar Loebenberg, Elmar J Prenner

Nanomedicine. 2022 May; 10.2217/nnm-2021-0398

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Jieyu Zuo, Chulhun Park, Janice Yu Chen Kung, Nádia Araci Bou-Chacra, Michael Doschak, Raimar Löbenberg

Pharmaceutical Research. 2021 February; 10.1007/s11095-021-03007-x

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Daniela Amaral Silva, Neal M. Davies, Michael R. Doschak, Jozef Al-Gousous, Nadia Bou-Chacra, Raimar Löbenberg

Journal of Controlled Release. 2020 September; 10.1016/j.jconrel.2020.06.031

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Daniela Amaral Silva, Jozef Al-Gousous, Neal M. Davies, Nadia Bou Chacra, Gregory K. Webster, Elke Lipka, Gordon L. Amidon, Raimar Löbenberg

Pharmaceutics. 2020 May; 10.3390/pharmaceutics12050420

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Jieyu Zuo, Wugang Zhang, Hui Jian, Nádia Bou-Chacra, Raimar Löbenberg

Brazilian Journal of Pharmaceutical Sciences. 2020 January; 10.1590/s2175-97902019000417827

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Jieyu Zuo, Hongming He, Zhengyun Zuo, Nádia Bou-Chacra, Raimar Löbenberg

Journal of Pharmacy and Pharmacology. 2018 January; 10.1111/jphp.12840

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Dissolution Technologies. 2015 January; 10.14227/DT220115P17

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AAPS PharmSciTech. 2014 January; 10.1208/s12249-014-0133-8

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BioMed Research International. 2014 January; 10.1155/2014/204925

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AAPS PharmSciTech. 2014 January; 10.1208/s12249-014-0241-5

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Dissolution Technologies. 2013 January; 10.14227/DT200413P6

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Therapeutic Delivery. 2012 January; 10.4155/tde.12.42

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Molecular Pharmaceutics. 2012 January; 10.1021/mp200162b

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AAPS Journal. 2012 January; 10.1208/s12248-012-9350-9

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Dissolution Technologies. 2011 January;

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Journal of Controlled Release. 2011 January; 10.1016/j.jconrel.2010.10.035

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Dissolution Technologies. 2010 January;

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AAPS Journal. 2010 January; 10.1208/s12248-010-9221-1

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AAPS Journal. 2010 January; 10.1208/s12248-010-9202-4

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European Journal of Pharmaceutics and Biopharmaceutics. 2010 January; 10.1016/j.ejpb.2010.05.002

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European Journal of Pharmaceutics and Biopharmaceutics. 2009 January; 10.1016/j.ejpb.2008.10.019

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Pharmaceutical Research. 2008 January; 10.1007/s11095-008-9642-z

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Drug Development and Industrial Pharmacy. 2008 January; 10.1080/03639040802149079

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European Journal of Pharmaceutics and Biopharmaceutics. 2008 January; 10.1016/j.ejpb.2008.01.026

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European Journal of Pharmaceutics and Biopharmaceutics. 2007 January; 10.1016/j.ejpb.2006.10.021

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Thermochimica Acta. 2007 January; 10.1016/j.tca.2007.11.008

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AAPS PharmSciTech. 2007 January; 10.1208/pt0803078

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International Journal of Pharmaceutics. 2007 January; 10.1016/j.ijpharm.2006.10.001

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International Journal of Pharmaceutics. 2007 January; 10.1016/j.ijpharm.2007.08.045

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European Journal of Pharmaceutical Sciences. 2006 January; 10.1016/j.ejps.2006.05.004

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International Journal of Pharmaceutics. 2006 January; 10.1016/j.ijpharm.2006.03.052

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Journal of Pharmacy and Pharmaceutical Sciences. 2006 January;

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International Journal of Pharmaceutics. 2004 January; 10.1016/j.ijpharm.2003.09.041

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Pharmaceutical Research. 2000 January; 10.1023/A:1007529020774

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European Journal of Pharmaceutics and Biopharmaceutics. 2000 January; 10.1016/S0939-6411(00)00091-6

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AIDS Research and Human Retroviruses. 1996 January;

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Proceedings of the Controlled Release Society. 1995 January;

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