Carriers for Drug Delivery Systems (DDS)

Field: Development of new medicine | Nanomaterials

Challenge:

There are a great number of active pharmaceutical ingredients (APIs) showing promising biological effects in (pre)clinical studies, but their chances of clinical use are generally low, which contributes to the high cost of drug development. API failures are usually related to their low bioavailability, stability, selectivity, and the associated deleterious side effects. These drawbacks can be reduced or even eliminated by utilizing side-specific drug carriers. A great deal of work has been done in this field with varying results. For example, drug carrier systems are based on liposomes, polymers, porous silicates, or, more recently studied, porous nanoparticles of metal-organic frameworks (MOFs). The key advantages of MOFs compared to other carrier systems are: 1) large drug loading capacity, 2) control over gradual drug release based on carrier decomposition or slow drug desorption, 3) possibility to fine-tune their composition and thus their properties and 4) possibility of surface modifications enabling additional control over their stability, drug release, targeting, etc. However, the amount of available non-toxic ligands capable of MOF formation is limited.

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Tech overview:

The unique idea is to utilize natural bile acids (BAs) in the preparation of organic ligands for the formation of biohybrid self-assemblies using essential metal salts – Bile Acid-based Metallo-supramolecular NanoParticles (BAM-NPs). BAs’ low toxicity, ability to activate transport mechanisms through biological membranes of the enterohepatic circulation, and convincing preliminary results of BAM-NPs synthesis, toxicity, and transport studies make them strong candidates for use as building blocks of intriguing biocompatible MOFs. BAM-NPs can provide drug protection, maintaining their stability during transport, and a possibility for selective and gradual delivery to tissues and organs of enterohepatic circulation (e.g., aiming at liver, small intestine, colon, gall bladder, or rectum) driven by a natural and highly efficient bile acid transport mechanism. The targeting and drug release can be triggered under specific conditions (e.g., acidic conditions present in cancer cells’ microenvironment, strong reductive environment, light impulse) by tuning the ligand chemical properties, the strength of non-covalent interactions responsible for the formation of BAM-NPs, or by attaching targeting molecules.

Benefits:

In general, the key advantages of steroid ICPs compared to other porous carrier systems are:

Tailorability in terms of composition, size, and shape, thus also their physicochemical properties
Structural reorganization upon changes to external conditions (solvent, pH, temperature, pressure)
Possible control over the gradual release of adsorbed molecules based on slow desorption or carrier decomposition
Low-toxicity, biocompatibility, and targeting
Possibility of surface modifications enabling additional control over their stability, guest release
Lower production cost and sustainability

Applications:

Targeted cancer therapeutics
Combination regimens with other mitotic or transcriptional inhibitors
Patentable novel chemical entities
Platform for further SAR-driven lead optimization

Commercial opportunity (seeking):

We are seeking a partner for technology licensing and its practical implementation.
We are looking for an investment partner to complete the technology development and for the potential establishment of a spin-off company.