More than 90 % of newly developed Active Pharmaceutical Ingredients (APIs) are poorly soluble. To get the full pharmacological potential of an API, one has to make sure that the drug will be dissolved in an appropriate time period as a prerequisite for its passive or active absorption in the GI tract of the patient.
To improve the solubility as well as the dissolution rate of poorly soluble APIs, one strategy is to reduce the API particle size to nano size. Due to that, the surface area of the API particles is strongly increased which results in a possible oversaturation. However, an increase of the API solubility and the dissolution rate leads to higher bioavailabilities, which may lead to lower therapeutic doses reduced adverse side effects as well as reduced costs.
The probably most important approach to obtain API nanoparticles is wet bead milling of aqueous API suspensions containing suitable additives for particle stabilization.