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A chemistry research group from a Spanish university has developed an invention that refers to the formation of dendrons of carbosilane structure that have in their periphery preferably anionic or cationic groups and in the focal point fatty acids or derivatives of these. License agreement and/or technical cooperation agreement are sought with companies from the sectors of health, biotechnology, pharmaceutics or environment.
The present invention from the Spanish research group provides compounds formed by dendrons of carbosilane structure that are functionalized in their periphery with anionic groups (such as carboxylate, sulfonate or sulfate), which endow the system with a net negative charge, or cationic (such as ammonium), which endow the system with a positive net charge.
These dendrons present a focal point that contains a hydrophobic function, mainly derived from a fatty acid. The fatty acid is linked to the dendron preferably through an ester bond, without dismissing other types of bonds, or even through electrostatic interactions.
Another aspect of the present invention relates to the process for obtaining the compounds.
The patent also includes the preparation of Janus type dendrimers, which are characterized by being formed by two dendritic units that have some distinct structural features.
And finally, the invention includes the ability of the described compounds to form micelles. The principal medium for its formation would be aqueous but micelles can also be formed in solutions containing soluble salts in these media or surfactants.
Its main field of application is in biomedicine, as non-viral transport agents, as drug transporters, to elaborate a drug, as antimicrobial, antiviral or antipyretic agents.
In the environmental sector we also find its application as biocides for water treatment.
Regarding the uses in biomedicine of these compounds and the micelles formed by them, it is worth highlighting: their use as non-viral transport agents for the transfection or internalization of nucleic material within different cell lines in gene therapy processes; use of these compounds as "per se" therapeutic agents, for example as antiviral, antimicrobial or antipyretic agents, or as drug transporters, even for the preparation of a drug of solid or liquid composition. And oral, nasal, topical or parenteral administration.
In their environmental application, they can be used as biocides to prevent the appearance of microorganisms on surfaces or water treatment.
The research group seeks to reach license and/or technical cooperation agreement, with companies in the biomedical, pharmaceutical, biotechnological and environmental sectors.
The main advantage of this innovation is the stability and robustness of the dendritic micelles respecting the conventional polymeric micelles. In addition, the carbosilane scaffold allows good internalization through physiological membranes.
As amphiphilic nanosystems, they allow to be loaded with drugs and therefore used for different biomedical applications, as antimicrobial, anticancer among other, diminishing the doses used without any protective system and therefore reducing side effects. In the case of cationic dendritic dendrons or cationic micelles, they can be used as packing systems for nucleic acids and therefore used as transfection agents for gene therapy. Bringing together both aspects, an important application may consist on the combination of both therapeutic strategies, one able to deliver a specific drug while condensation of DNA can be performed, affording a dual mechanism of action against a concrete disease.
These systems are able to overcome some of the difficulties that certain drugs found, allowing to facilitate their transport, favoring their solubility, increasing their solubility and even acting as transporters to the areas of interest.
- Ease of diffusion of dendrimers through biological barriers, and therefore access to target cells.
- Possibility of encapsulation and transport of drugs or other molecules with biological activity.
- The preparation of these dendrimers as pharmaceutical formula can be very varied, being possible any solid composition (tablets, pills, capsules, granules, etc.) or liquid (gels, solutions, suspensions or emulsions). For oral, nasal, topical or parenteral administration.
The research group seeks to reach license and/or technical cooperation agreement with companies in the biomedical, pharmaceutical, biotechnological and environmental sector.
Two strategies have been developed to carry out this technology to the market:
a) Licensing. This strategy is based on the idea to transfer the technology to a licensee (company) able to easily use and exploit the technology in order to get profits during the license period. For the case of the licensor (group from the university) royalties must be expected.
b) Technical cooperation agreements. Interchange of technical knowledge and skills between the group of research and a company designed to contribute to the balanced and integrated development of the economic resources and productive capacities, as well as the development of the technique. This cooperation must increase the Technological Readiness Level (TRL) from TRL 1 (basic technological research) to TRL 4-5 (technology development) or TRL 5-7 (technology demonstration). The purpose is to get even closer to the market also thinking in future Europe Horizon calls. Therefore, they are looking for pharmaceutical or biotech companies able to proceed with the validation of the technology via drug release studies for in vitro and in vivo experiments.