Filip Kiekens professor

Research Filip Kiekens

Research team

Expertise

research into conventional dosage forms and drug delivery systems research into products with Probiotic (Formulations and production techniques) research into dosage forms and drug delivery systems for poorly watersoluble active compounds

Cyber-physical system for personalized intranasal drug delivery. 01/05/2023 - 30/04/2024

Abstract

The upper nasal space is a unique drug delivery environment and has long been underutilized. Nose-to-brain delivery of therapeutic agents for neurodegenerative disorders does not have the same limitations as other existing administration methods. However, intranasal drug delivery has its own set of challenges because of the nasal shape's heterogeneous character and dynamics. This large morphological variation demands a person-specific approach that enables live sampling of the nasal structure and subsequently uses it during administration of the therapeutic agent. This project is the first and important step in the creation an efficacious intranasal drug delivery solution: designing and building the portable device able to capture the three-dimensional nasal shape in a non-invasive manner.

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    Project type(s)

    • Research Project

    Entomovectoring of lactic acid bacteria to control Botrytis cinerea on strawberries. 01/11/2022 - 31/10/2024

    Abstract

    The phytopathogenic fungus, Botrytis cinerea, is the most common reason for fruit rejection in small fruit crops such as the strawberry plant. To get rid of this fungus, chemical fungicides are still the most popular worldwide. Due to increased resistance, growing environmental awareness, continued consumer demand for fewer pesticide residues and more stringent policies in many countries, more and more research is being devoted to sustainable alternatives fitting within the framework of integrated pest management. Within this project, biocontrol using lactic acid bacteria is studied as an alternative. Lactic acid bacteria are well known for their protective properties within food applications, but their role on the plant and their potential as a biocontrol organism on the phyllosphere have only been investigated to a limited extent. To avoid inconsistent field performance, a common problem in biocontrol, candidates will be screened for their potential to survive and grow on the phyllosphere. We will focus on the entomovectoring system as the approach to applying these potential biocontrol agents. In this system, a vector, Bombus terrestris, will disseminate an optimized formulation of lactic acid bacteria directly to the strawberry flowers. In this way, pollination and crop protection are done at the same time and efficient delivery towards the target location is guaranteed.

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    • Research Project

    OPTIMISE: Advanced biOreactors and Processing equipmenT for culturIng beneficial MIcrobeS to higher yiElds. 01/05/2020 - 30/04/2024

    Abstract

    Beneficial microbes have a plethora of biomedical, environmental and engineering applications. Currently, many fundamental and more applied R&D projects are slowed down by the need for advanced equipment for the upscaling and processing of the microbial cultures. Here, a research consortium of bio-engineers, civil engineers, biologists and pharmaceutical engineers was built to jointly advance the applications and research of beneficial microbes at UAntwerpen. This consortium aims to manage joint equipment and expertise. The core of the equipment is a 100 l pilot bioreactor suited for bacteria, yeasts and algae. It is fully computer controlled and monitored, and equipped with a steam-in-place (SIP) unit. The system is equipped with several sensors and valves allowing automated control of important parameters (e.g. pH, dissolved oxygen, conductivity, turbidity, …). The whole system is GMP- compatible and in pharmaceutical- grade steel. A 10 l bioreactor is foreseen for optimizing culturing conditions. The reactors are complemented with an incubator-shaker for the growth of inocula and postprocessing equipment to professionally process the biomass. The post-processing equipment mainly consists of a large scale, low- to- high speed cooled centrifuge and a pilot spray dryer for final processing for extended shelf life of the biomass and work up of the biomass towards its final application.

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    • Research Project

    Versatile X-ray powder diffraction platform for materials science. 01/01/2020 - 31/12/2021

    Abstract

    The proposal concerns versatile instrumentation for determining crystallinity, unit cell size and structure of organic, metal-organic and inorganic materials. Several groups at UAntwerp have a pressing need for fast, reliable, X-ray diffraction data, at low angles to determine large unit cells, and preferably in 2D to determine sample homogeneity. The envisaged machine has a Cu K alpha source, horizontal sample platform (Bragg-Brentano geometry), capability for measuring down to low angles (theta = 0.5°), and a fast and sensitive 2D solid state area detector. It will be used for materials research and characterization in inorganic porous materials (zeolites, templated silicas and titanias), metal organic materials (crystalline metal-organic frameworks), organic materials (fatty acids, PUR building blocks) and identification and characterisation of pigments for study and conservation of old masters' paintings. In addition, through the use of the PDF (probability density punction), the machine can generate experimental information through x-ray scatterineg on average short-range order in non-crystalline materials such as glasses and amorphous powders.

    Researcher(s)

    Research team(s)

    • Intelligence in PRocesses, Advanced Catalysts and Solvents (iPRACS)

    Project type(s)

    • Research Project

    Drug delivery systems and in vivo efficacy of the serine protease inhibitor UAMC-00050 in a preclinical model for irritable bowel syndrome. 01/10/2018 - 30/09/2019

    Abstract

    The serine protease inhibitor UAMC-00050, previously shown efficacious in 2 preclinical IBS models after systemic administration, will be formulated for oral and rectal administration. The drug delivery systems will be tested in the rat IBS model for dose determination, efficacy, time of administration and serum concentrations, a crucial step towards further valorization of the compound.

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    • Research Project

    In vivo POC of potential respiratory probiotic strains (REINSPIRE). 01/01/2018 - 31/12/2018

    Abstract

    Probiotics are defined as live microorganisms which, when applied inadequate amounts, confer a health benefit to the host (FAO/WHO, 2001). These microbes are generally applied in the gastrointestinal tract via fermented food products or capsules. In previous research, we isolated bacterial strains with potential probiotic properties for the upper respiratory tract based on in vitro laboratory tests and genome sequencing. Here, we want to deliver the POC that – at least one of - these strains has also interesting properties in vivo, i.e. that this strain is able to –temporarily- colonize the upper respiratory tract of healthy volunteers after oral and nasal application.

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    • Research Project

    Research in formulation of poorly watersoluble active compounds in PLGA Nanoparticles using spray-drying technology. 01/10/2017 - 30/09/2021

    Abstract

    The poor water-solubility of new active pharmaceutical ingredients (API) is a true challenge for formulation experts. Before an API can reach the systemic circulation and reach the target site of action, orally-taken drugs need to dissolve first in the gastrointestinal fluids. The use of organic solvents in high-throughput screening of new API's, as well as the structure-activity related research, often results in candidate-molecules with an extreme lipophilicity and high molecular weight and consequently a poor water-solubility. In this project, different formulation technologies will be screened to increase the bio-availability of these API's. This project focusses on an innovative technology, the spray-drying of nanoparticles (NP's), in comparison with 3 more conventional formulation approaches (cyclodextrine-complexes, amorphous systems and PolyLactic-co-Glycolic Acid (PLGA)-nanoparticles). Embeded in the Antwerp Drug Discovery Network of the UA, the Laboratory of Pharmaceutical Technology (LPTB) is well situated to bridge the Medicinal Chemistry research activities with the LMPH in vivo-modeling expertise. This allows the evaluation of the full potential of new medicinal compounds in an in vitro and in vivo setting. Last year, the applicants' laboratory supported several other UA labs requesting formulation assistance with their poorly water-soluble compounds.

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      • Research Project

      Formulation and processing of probiotic bacteria in a solid oral dosage form for pharyngeal delivery. 01/01/2017 - 02/11/2020

      Abstract

      Respiratory infections know a high morbidity. Nowadays, patients are treated with over-thecounter products such as decongestives and expectorants. There is also an overuse of antibiotics, which leads to antibiotic resistance. Therefore, a new therapy, based on microbiomemanipulation, is imposed. This research will focus on the improvements for this new therapeutic strategy. The human body consists of many microorganisms lives in symbiosis with each other, resulting in beneficial effects for both. Pathogens can disturb this symbiosis. The homeostasis can be restored by probiotic formulations. They will reinforce the innate immunity. It is the aim of this research to develop a solid oral dosage form for the pharyngeal delivery of probiotic bacteria, which can prevent and treat respiratory infections. Mechanical stress during compression can damage the bacteria, which can result in therapy failure. The aim of this research is to protect the bacteria by choosing the correct formulation and process parameters. This research will be combined with detailed microbiological analysis. The stability of the formulation will be investigated by stability tests. Finally, the efficacy and safety of the formulation will be determined by in vitro tests. Successful results can lead to clinical studies on humans and to new businesses. This can result in a medical and economical progress..

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        Project type(s)

        • Research Project

        Implementation of a state of the art reference center for pharmaceutical and pharmacological studies in Cuba to support the use of natural product formulations composed of indigenous phytomedicinal and nutraceutical molecules. 13/03/2016 - 31/12/2019

        Abstract

        The project aims to establish a multidisciplinary reference platform at CIDEM with improved capacity (infrastructure+ know-how/training) in natural drug research and development, which integrates preparation of plant extracts, extraction and purification, analytical and structural characterization, molecular pharmacological evaluation and design and evaluation of appropriate systems of drug delivery, which allows pharmaceutical and pharmacological studies of phytomedicinal and nutraceutical products according to international standards, to stimulate the use of natural products in the National System of Health (NSH) in Cuba.

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          Project type(s)

          • Research Project

          ProCure : Defining the future of probiotics for upper respiratory tract diseases. 01/01/2016 - 31/12/2019

          Abstract

          This project aims to explore probiotic microbial approaches that can efficiently reduce the incidence and symptoms of diseases of the upper respiratory tract (URT). Hereto, we will set up an enabling platform to (1) select innovative probiotic strains for this original human body niche of probiotic application, (2) develop innovative processes for the formulation, upscaling and application of these probiotic strains and (3) develop innovative services based on cellular, more complex polymicrobial model systems and microbiome analyses of the URT to monitor the impact of probiotics, food and pharmaceutical compounds on the microbiota of the URT.

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          • Research Project

          Research in Formulation and Processing of Probiotics in Buccal Dosage Forms. 01/10/2015 - 31/12/2016

          Abstract

          In case of many nasopharyngeal diseases, such as otitis media, acute and chronic sinusitis and pharyngitis, patients frequently resort to self-medication using over-the-counter products. Often, clinical data is lacking to support the use of decongestive, expectorantia or nasal salt solutions and relapse is frequent. On the other hand, (ab)use of antibiotics is linked with the resistance-issue. Main idea of this project is that local buccal or nasal sprays or lozenges, in which Lactobacillus species are formulated, could enhance the existing therapies. Many nose and throat disease conditions also show a microbial imbalance between enhanced numbers of pathogenic microbes versus decreased number of beneficial macrobiotics. Ultimately, dosage forms containing probiotics might be the preferred upper-airway-therapy over antibiotics-usage. In this project, fundamental formulation and process research will be conducted, to support and in preparation of (pre)clinical studies. The application of spray drying as innovative manufacturing technology for probiotic dosage forms, has many advantages such as excellent control over process parameters and over powder characteristics. The lyophilization-technology is applied as the reference drying technique. The influence of excipients and additives in the formulation will be investigated. They might have a protective effect during the processing, as well as during stability and at moment of reconstitution into the final dosage form. Secondly they will determine the powder particle properties, important for lozenge-formulation. Finally, their effect on adhesion of the formulation to bucal epithelial cells , might be advantageous in terms of local residence time and efficacy . Probiotic cell viability is evaluated in function of the spray drying process parameters. Final goal of this project is a buccal lozenge containing probiotics, having a sufficient efficacy and stability. This project fits perfectly in an on-going IOF-SBO program in collaboration with the UA research lab of Prof. Dr. Sarah Lebeer (Bio-engineering Sciences).

          Researcher(s)

          • Promoter: Kiekens Filip
          • Co-promoter: Claes Ingmar
          • Fellow: Byl Eline

          Research team(s)

            Project type(s)

            • Research Project

            Design of a knowledge platform for the realisation of an extensive and innovative range of probiotics 02/02/2015 - 31/01/2017

            Abstract

            This project represents a formal research agreement between UA and on the other hand the client. UA provides the client research results mentioned in the title of the project under the conditions as stipulated in this contract.

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            Project type(s)

            • Research Project

            Medicinal Chemistry-Drug Discovery (ADDN). 01/01/2015 - 31/12/2020

            Abstract

            This project represents a research contract awarded by the University of Antwerp. The supervisor provides the Antwerp University research mentioned in the title of the project under the conditions stipulated by the university.

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            • Research Project

            Optimization of novel lead compounds for the treatment of African trypanosomiasis using innovative medicinal chemistry and formulation. 01/01/2015 - 31/12/2018

            Abstract

            The main objective of this research project is the lead optimization of the identified triazine series using medicinal chemistry and formulation technologies to increase the in vivo activity against T. brucei by combining enhanced solubility and metabolic stability with enhanced drug delivery.

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            • Research Project

            The influence of probiotic watercontent and wateractivity in spray-dried nasopharyngeal and buccal formulations. 01/02/2014 - 31/12/2014

            Abstract

            This project investigates how the critical formulation and process parameters influence the zeta-potential and the wateractivity in nasal/buccal sprays and lozenges of spray-dried probiotics, in particular with Lactobacillus rhamnosus species. The link between wateractivity, absolute water content and cell viability will be investigated immediately after production and in a stability study.

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              • Research Project

              Creation of a preclinical platform at the UA for testing novel therapeutic approaches against ocular surface diseases. 01/01/2014 - 31/12/2015

              Abstract

              Ocular Surface diseases (OSD) such as dry eye syndrome (DES) show an estimated prevalence between 15 and 29%. The only FDA approved and on subscription dry-eye treatment is cyclosporine 0.05% (Restasis®), but this formulation is not available in the EU. Novel therapies for OSD are therefore needed. The expertise within ADDN fosters a unique opportunity to set up a preclinical platform on OSD leading to an increased collaboration with industrial partners.

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              • Research Project

              Design of a platform for the selection and novel formulation of nasopharyngeal probiotics. 01/12/2013 - 30/11/2015

              Abstract

              Probiotics are primarily known as food additives that can have positive health benefits by improving the microbial balance in the gut. Infections of the throat and nose are also characterized by microbial imbalances. Treatment of these infections with a local spray, tablets or mouthwash of probiotics, in particular with Lactobacillus species, can improve the efficacy of the currently available medication and provide an alternative and novel site of application for probiotics.

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              • Research Project