The new high effective antifungal formulations on the basis of fungicides immobilized with the use of polymer carriers
Tech Area / Field
- MED-DRG/Drug Discovery/Medicine
- CHE-POL/Polymer Chemistry/Chemistry
- AGR-FOD/Food & Nutrition/Agriculture
8 Project completed
Senior Project Manager
Mitina L M
INEOS (Organo-Element Compounds), Russia, Moscow
- P.W. Anderson & Partners, Inc., USA, VA, Vienna\nNortheastern University / Bouve College of Health Sciences, USA, MA, Boston
Project summaryThis project is in the field of discovery of substances to be used as new drags and/or drag delivery systems. It is focused on creation of new high-effective biologically active formulations of macromolecular nature to be applied as medical systems and biocides. As the result of the project implementation new polymeric forms of fungicides having improved functional properties compared to low-molecular weight analogs will be developed. Their main advantages should be:
· optimal level of solubility (including water);
· optimal rate of release of active substance;
· relatively low doses of active substances;
· relatively high stability;
Objectives of the project:
· to reveal fundamental principles of correlation between structure of developed macromolecular systems and their property and activity;
· to develop the basis for creation of new effective antifungal preparations for medicine, agriculture, and food industry.
Technical aproach and methodology
As initial low molecular weight fungicides aliphatic carboxylic acids (sorbic, undecenoic), antibiotics (nystatin, amphotericin B) will be used.
Different ways of processes of fungicides immobilization on polymer carriers (via covalent, ionic or H-bond) will be explored. In a number of cases the possibility of fungicides incorporation into polymeric microaggregates and lipid vesicles modified with amphiphilic polymers will be studied.
As the basis for creation of polymeric microaggregates and modifiers for liposome membranes water-soluble amphiphilic polymers of N-vinylpyrrolidone containing long-chain (C17-C18) aliphatic end groups will be used. Radical polymerization in the presence of functional mercaptanes will be used for synthesis of such polymers.
The polymers and co-polymers of N-vinylpyrrolidone, acrylamive, vinyl alcohol will be used as the polymer carriers for fungicides immobilization.
Effect of type of bond between carrier and fungicide, durability of this bond (rate of hydrolysis, constants of polymeric salt dissociation, stability of polymeric complexes), structure of polymer carrier (its molecular weight, content of functional groups which responsible for bonding, change of liophilic-liophobic balance during immobilization, conformation of polymer in solution) on the rate of fungicide release and biological activity will be studied.
Fields of application and perspectives of commercialization
New systems containing fungicides and polymeric carriers for application in medicine (for the surface treatment and injection), protection of food against mycotoxins, seed treatment in agriculture will be developed.
Results and approaches of the project could be of interest for the leading producers of commercial fungicides (Novartis, Jansson-Silag).
Investigation of fungicidal activity of immobilized systems in regard to a number of microorganisms will be accomplished in the Laboratory of toxicology of University of Crete. It is headed by Prof. Tsatsakis, well known specialist in testing of biologically active polymers.