Novel Technology for the Preparation of Nanoparticles to Increase the Solubility and Bioavailability of Hydrophobic Molecules

It is estimated that 70–90% of drug candidates at the development stage are hydrophobic, with poor water solubility. Examples of hydrophobic drug candidates include quercetin, cannabidiol (CBD), tetrahydrocannabinol (THC), retinoic acid, tocotrienols, and ivermectin. This physical property can limit the development of these molecules for new drug use, and may be associated with low bioavailability, reduced therapeutic effects, and increased dosage that could cause un-wanted adverse effects. Background: In previous work, we developed a novel Facilitated Self-assembling Technology (FAST for short) with several specific practical methods. The major advantage of FAST is that the hydrophobic compound is not engineered nor encapsulated, and there is no addition of lipid, surfactant, or metal component. The nanoparticles prepared using this technology are highly hydrophilic and stable. This nanotechnology would allow many drug candidates to be developed with increased solubility and bioavailability in their own nanoparticle form. Objectives: The purpose of the current study is to use three practical methods of FAST to prepare water nanosuspensions of several known poorly soluble drug candidates. Methods: ZetaView nanoparticle tracking analysis and electron microscopy imaging. Results: The results demonstrate that this novel nanotechnology is able to generate stable and water-soluble nano-particles of these compounds, which could be used in new drug development or reformulate and improve the solubility and bioavailability of currently used drugs.