Obtaining supramolecular systems

Researcher: Ioana-Georgeta Grosu

Keywords: supramolecular systems, inclusion compounds, bioactive substances

Description

Supramolecular systems are new materials of interest for many industrial branches and have particular impact in the pharmaceutical, food supplements, cosmetics, chemical (pesticides) industries.

The incorporation of substances of interest into various carrier matrices, resulting in the formation of supramolecular systems, aims to improve some of their physico-chemical properties, such as solubility, reduction or elimination of undesirable odors, increase physical and chemical stability by protecting against reactions induced by light, heat and moisture. They may also help to stabilize emulsions and suspensions.

In the case of bioactive substances, whether synthetic or natural, the goal is to improve bioavailability, controlled release and transportation to the target, with the aim of reducing adverse effects by lowering the dose required for effective therapy. By implication, significant cost savings can be achieved by identifying optimized formulations.

(Macro)molecules used as carrier matrices: cyclodextrins, dendrimers, metal-organic polymers, zeolites and many others.

Cyclodextrins are cyclic oligosaccharides consisting of 6, 7 or 8 glucose units (cyclodextrin) with a hydrophilic outer surface and a hydrophobic central cavity. The hydrophilic exterior confers enhanced solubility in water, and the hydrophobic cavity constitutes a micro-framework that can accommodate non-polar molecules or parts thereof of appropriate size.

Dendrimers are single-centered nano-sized supramolecules containing three types of structural components: the central unit (core) surrounded repetitively inside by layers of identical and branched units, nodes, determining the generations (G-n, n>1) and peripheral functional groups, which play an important role in the (physico-)chemical properties of the dendrimer.

Their particular properties allow a wide range of applications in combinatorial chemistry, medicine and nanoscience. One important application is the use of dendrimers as drug-delivery systems for the transport of biologically active substances to the site of action, due to the presence of multiple peripheral groups that allow functionalization and controlled release.

Biodegradable metal-organic polymers (BioMOFs) are organic-inorganic hybrid compounds obtained by the coordinative assembly of metal ions and organic ligands. They are of increasing interest for their use as carriers of bioactive substances due to their specific properties: high loading capacity with the active compound, ability to incorporate bulky guest molecules, high stability and non-toxicity.

To obtain supramolecular systems with high yield, we use the following experimental techniques in our laboratory:

  • dry or wet mechanical mixing
  • magnetic stirring in solution/suspension
  • co-evaporation
  • co-precipitation
  • lyophilization
  • atomization

 Applications

Areas of application: R&D, nanomedicine, optimization of industrial processes, obtaining products with increased efficacy

Industries: health and medical sciences industry, pharmaceuticals, cosmetics, food supplements, chemicals (phytosanitary)

 Infrastructure

The preprartion of supramolecular systems is carried out in the Crystallization and Polymorphism Laboratory, equipped with:

  • Zinsser Crissy Light XL small-scale parallel crystallization platform in high-throughput mode, capable of processing 24 experiments simultaneously under temperature controlled conditions. The platform offers the possibility of automatic addition of solvent/solvent mixtures, setting of various temperature regimes ranging from 2÷200°C and horizontal stirring of samples
  • Eyela PPS-5511 large-scale crystallization platform with five synthesis reactors, allowing parallel experiments to be carried out under controlled temperature conditions for each individual reactor
  • The Retsch MM 400 ball mill MM 400 offers the possibility to run two experiments in parallel, with or without added solvent, by setting the mixing frequency and mixing time
  • Memmert HCP10 climatic chamber with temperature (up to 160°C) and humidity control for stability testing
  • System for in situ monitoring of the dissolution rate μDISS Profiler with which four experiments can be performed in parallel, equipped with a spectrometer, and experiments can be performed at a controlled temperature.

Advantages

 The existing facilities allow the realization of services to obtain supramolecular systems

 Specialized staff is able to cover with the highest professionalism all stages of a contractual collaboration, from experimental design, performing experiments to correlation of results with other complementary information

Estimated costs

The total cost of CDI services to obtain supramolecular systems results from:

complexity and number of experiments performed, chemical reagents and solvents required, labor

time of use of the apparatus, consumables and their wear and tear.