ProRelease™

Controlled release microspheres for precise GI targeting

Kuecept Ltd has developed one of the world’s first erosion-based multiparticulate amorphous drug delivery technologies which enables the controlled release of drugs in the GI tract with high precision and reproducibility. In the ProRelease™ system, the drug is homogeneously distributed throughout a GRAS polymer matrix in a stabilised amorphous state to afford improved kinetic solubility, whilst providing precise dissolution control and drug release, something that is dificult  to control with other methods of amorphous dispersion manufacture (e.g. spray drying).

Once administered, these solid microspheres rapidly disperse in the stomach and are eroded by the gastrointestinal fluids in a controlled manner as they pass through the GI tract; the drug release mechanism is particle erosion, effected through water diffusion and polymer hydration / dissolution. The matrix is designed to erode when in contact with biological fluid at a defined pH, but at the same time, it is desirable that water does not diffuse into the matrix until the point of release, thus avoiding drug diffusion out of the microparticles and reducing the effects of luminal enzymatic activity.

By altering the composition of the matrix, three versions of the ProRelease™ technology have been created, namely modified, prolonged and targeted release.

Key benefits:

• Ability to manufacture at small scale (batch sizes of < 100 mg) with high product yields (> 80 %), thereby reducing API requirements during early development stages
• Microparticles exhibit good flow propeties and density (~ 1g/cm³), ideal for manufacture of high dose suspensions for tox programs
• Does not require the use of high processing temperatures or fast solvent removal processes; dispersions are physically stable and do not change during storage
• Does not require the use of expensive processing equipment (i.e. spray drying or hot-melt extrusion), meaning formulation feasibility assessment programs are quick and cost effective.
• Multiple experiments can be set up in parallel which enables us to screen a wide range of stabilising excipients and drug loadings in a short period of time to optimise release kinetics and physical properties
• Options for immediate, modified / delayed and sustained / extended release
• Microparticles form stable suspensions which are ideal for short / medium term preclinical dosing studies or for manufacture of special products (e.g. paediatric / geriatric dosage forms)

The ProRelease™ technology is offered to clients on a fee for service basis. Options are available under license for technology transfer or for development and patent protection of specific drugs or drug classes. Please contact us directly for more information.