The headline to this article was the subject line of an email we at LifeScience Krakow sent to Professor Henry Chesbrough when we were investigating new ways to bring together innovators and entrepreneurs. Mr Chesbrough coined the phrase “open innovation” and it’s an idea that’s been at the heart of everything we do.
In fact, all the cluster initiatives at LifeScience Krakow aim to connect and support the development of innovation of different origins and applications. The scope of the “quality of life” science competencies and the resources available within the ecosystem at Krakow is the main competitive advantage we offer to the international community.
I recently caught up with some of the scientists currently thriving within LifeScience Krakow to demonstrate exactly what is on offer and how world-class research is flourishing in our cluster.
First, I spoke to Maciej Szaleniec and Piotr Warszynski from Jerzy Haber Institute of Catalysis and Surface Chemistry PAS about their latest developments related to steroids and nanocarriers for medical applications, and the role of the research institute in the development value chain.
Q: You apply the key competence of the ICSC, which is the synthesis of fine chemicals applied to a novel therapeutics and drug delivery systems, tell us more about this work.
Maciej Szaleniec: Steroids are ubiquitous in nature and play important roles as membrane components, hormones, vitamin D and bile salts. As a result many drugs responsible for hormonal regulation or immunological response contain steroid structural motif. The ability to modify steroids and sterols chemical structure in a regioselective manner is essential in the development of new drugs of this class or modifying characteristics of the existing ones. It also provides access to alternate, more economical and environmentally friendly synthetic pathway.
Piotr Warszynski: Novel therapeutics and drug delivery systems belong to the one of the main disciplines of nanomedicine as described by the European Science Foundation (ESF). Nanoscale drug delivery systems are a sub-class of advanced drug delivery systems that consists of drug carriers with the sizes mostly below 200 nm. However, in numerous studies, the maximum uptake by the cells occurs for nanovehicles with about 100 nm in the diameter. Therefore, they may be the most suitable candidates to be used as nanocarriers for medical applications.
Q: What it is exactly that you do in ICSC in relation to the aforementioned technologies?
MS: We study the biocatalysts that enable regioselective oxidation of sterols and steroids. The enzymes under study originate from the facultative anaerobic bacteria, which is able to grow on cholesterol as a sole carbon source also under anaerobic conditions. As a result the bacteria employs a range of biocatalytic techniques for cholesterol modification. Some of these methods are highly interesting due to their potential application in synthesis of biologically active molecules. Currently, two enzymatic systems are under study and extensive development, and both have reached an application-ready stage.
The first one enables precise introduction of the OH group into the alkyl side chain of the cholesterol or its derivatives. In contrast to widely known cytochroms P450 the reaction catalysed by the enzyme is highly regioselective, which results with only one type of the product. This method allows synthesis of activated form of vitamin D3 or 25-hydroxylated cholesterol, it’s a potential anti-cancer or anti-viral agent.
The second method allows regioselective oxidative dehydrogenation of ketosterols or ketosteroids (e.g. androsteron to boldion). The enzyme enables introduction of a double bond into the ring A of the steroid ring system which changes pharmacological characteristics of steroid drugs. Most of these compounds are used to stimulate musculature growth and introduction of the additional unsaturated bond is associated with decrease of the reported side effects of these drugs.
PW: The research activities are concentrated in the direction of two medical applications, nanoncariers for the treatment of neurodegenerative diseases and cancer. A successful prevention and an effective treatment of the central nervous system disorders such as Alzheimer’s disease, Parkinson’s disease represent a major challenge of contemporary medicine. Unfortunately, despite the remarkable progress in the development of new neuroprotective substances, their effectiveness is still very limited because they do not penetrate the blood-brain-barrier (BBB). Together with partners from the NanoNeucar consortium we concentrate our efforts on developing various methodologies of encapsulation of neuroprotectants, adjusted to their physicochemical properties, for formation of nanocarriers with the size in the range (10 – 150 nm) for targeted delivery to brain. We attempt to elaborate the mechanisms of internalisation of nanocarriers of different structure and architecture of the “in-vitro” “in-vivo” models of BBB. If the synthesised nanonarriers appear to be effective, the “in-vivo” experiments in mice models are planned. The first results concerning the neuroprotective action of encapsulated components are promising and we hope that nanocarriers will be used in future for therapies of stroke and neurodegenerative diseases.
Q: In terms of “open innovation”, where are you now in the value chain?
MS: ICSC PAS is able to provide enzymatic preparations which can catalyse the aforementioned reactions and provide a crucial expertise in setting up the reactor systems. Moreover, the overexpression system for the second enzyme has been developed which enables a cheap on-site production of the biocatalysts and its easy affinity-based separation. Also the optimal methods for the downstream processing of the reaction mixture were developed. For both method ICSC PAS has filed patents (Polish Patent applications) this year and the extension of the IP protection to the international markets is envisaged.
PW: Anti-cancer therapy, such as the use of chemotherapeutic agents that efficiently eliminate cancer cells, suffers from a systemic cytotoxicity resulting in serious side-effects. The use of Doxil and Abraxane, two nanoparticle based anticancer drug formulations, have demonstrated that encapsulation of drugs might be a good solution to reduce the toxic effects without losing the therapeutic ones. The nanoemulsion carriers developed at ICSC PAS, with about 100 nm in the diameter containing the anticancer drug, seem the suitable candidates to be used for medical applications as they can penetrate tumour cells by the enhanced permeability and retention properties (EPR effect) that originates from the leaky vasculature of the tumor microenvironment. They have successfully passed the “in-vitro” test, however, much more research needs to be performed before they find application in clinical practice.
Q: These developments demonstrate your capacity to collaborate within drug development projects. Will you be presenting this during BIO-Europe in Munich?
MS: Yes, we will be presenting our research at the BIO Europe meeting, both as presentation and partnering offer. We do hope we can find an industrial partner interested in our discoveries.
The 17th European Congress on Biotechnology
In fact there are other possibilities to get involved in international collaboration. LifeScience Krakow is involved in preparation of the 17th European Congress on Biotechnology (ECB2016) 3-6 July, 2016. Therefore I caught up with Professor Tomasz Twardowski, Chair of ECB2016 Hosting Committee and Chairman of Biotechnology Committee, Polish Academy of Sciences.
Q:How does ECB2016 support scientific development?
Tomasz Twardowski: The main objective of ECB2016, in Krakow, is to develop knowledge of biotechnology with regards to the environment, agriculture, industry and much more. This event will increase Poland’s international position among the scientific research field. The transfer of experimental innovative solutions in several areas to socio-economic environment is critically important for everyday life: health, food, bio-materials, natural resources, biodiversity and many more. We offer the platform for co-operation between academia, industry, economics, and those new to the field.
Q:It seems like it fits the case of ICSC perfectly. How would you describe the event?
TT: In few words I would like to say it bridges academic and industrial expertise in life sciences for the common good.
More than 1000 biotechnologists, from academia and industry, will participate in the congress. It’s the platform for co-operation between Europe, Americas and Asia, as well as the best opportunity to meet leading biotechnologists from around the world. Several leaders of the science world have confirmed their participation, for example, Dr Bob Goldberg and Dr Emmanuelle Charpentier will present plenary lectures. The latest discoveries in science today are of critical value for bio-economy of tomorrow and ECB2016 is the place to learn all about it.
A detailed programme is available at www.ecb2016.com. The European Federation of Biotechnology will organise the 17th Congress under honorary patronage of the President of Polish Academy of Sciences. We have long tradition, 16 congresses in last 30 years, of ground-breaking meetings dedicated to science, industry and covering all the most relevant topics for modern day society.
About the author
Kazimierz Murzyn is Managing Director of the LifeScience Krakow Klaster, Vice Chairman of Global Innovation Network (GIN) Inc. in North Carolina, USA, Member of Biotechnology Committee of Polish Academy of Science, Member of Evaluation Committee of European Business Awards for the Environment.
About LifeScience Krakow
The strategic area of LifeScience Krakow’s activity focuses on products and technologies aimed at improving health and quality of life, and involves related fields of interest from biotechnology and the life sciences, including: drug discovery & research services, medical diagnostics, e-health and telemedicine, advanced- non-drug therapies, cosmetics, food and environment and bioeconomy.