Bioavailability

Reaching the desired in vivo exposures for the growing number of lipophilic drug candidates is one of the well-known challenges facing scientists in the pharmaceutical industry today

Bioavailability solutions

Approaches for improving solubility, enhancing dissolution rates, and raising the oral bioavailability of poorly soluble molecules have been developed with Losan’s formulation expertise for both clinical and preclinical studies.

How Losan Pharma Solves Bioavailability Challenges

What We Do

Using different platform technologies over the years, Losan has acquired in-depth experience on how to successfully improve oral bioavailability:

Nano technology

One of the most suitable technologies for improving the solubility of poorly soluble compounds is to reduce the particle size to the nano size range, which increases the effective surface area. This results in much higher dissolution rates and an oversaturation effect that leads to higher bioavailability and lower required dosages. It also helps to reduce any food or adverse effects.
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Hot melt extrusion

Another approach is to use HME to form a solid drug dispersion with hydrophilic polymers. The drug is molecularly dispersed and has a lower thermodynamic barrier for dissolution. Solid dispersions are an effective formulation technique to improve solubility, dissolution rate and therefore the bioavailability of water-insoluble drugs for oral delivery. In addition, amorphous solid dispersion (ASD) can accelerate a project by offering flexible dose escalation and excipient acceptance for toxicology studies, as well as providing adequate preclinical and clinical exposure.
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Mesoporous silica materials

Another new and interesting approach in Losan’s portfolio of solid dispersions is silica amorphous loading (drug loading onto inert porous silica materials). Two processes are possible: a dry extrusion/milling step, or a solvent based set-up, where API particles are removed from an organic solution and loaded onto the pores providing large surface areas for drug adsorption. With this technology, amorphous drug loading up to 40% is possible and contributes to improving the bioavailability of poorly water-soluble drugs.
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Spray drying technology

Spray drying is a well-established manufacturing technique which can be used to formulate amorphous solid dispersions by fast solvent evaporation that leads to a rapid transformation of solution to a solid state.
Besides evaporation kinetics, various process parameters that influence physical and chemical characteristics are important to obtain a stable amorphous structure of the API.
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Pharmaceutical manufacturing


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