Facilitated Self-Assembling Technology (FAST) for the Preparation of Nanoparticles to Increase the Solubility and Bioavailability of Hydrophobic Molecules

Author(s): Nicolette Frank, Douglas Dickinson, Yutao Liu, Hongfang Yu, Jingwen Cai and Stephen Hsu

Approximately 70–90% of drug candidates at the development stage are hydrophobic. These compounds often exhibit poor water solubility. Examples of hydrophobic drug candidates include quercetin, cannabidiol (CBD), tetrahydrocannabinol (THC), retinoic acid, tocotrienols, paclitaxel, and ivermectin. This physical property can limit the development of hydrophobic molecules for new drug use, and may be associated with low bioavailability, reduced therapeutic effects, and increased dosage that could cause unwanted 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 or 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 including CBD, quercetin and paclitaxel.

Methods: ZetaView nanoparticle tracking analysis was used to characterize nanoparticle suspensions by size distribution and Zeta potential, and electron microscopy imaging was used to examine the shape of the particles.

Results: FAST generated stable nanoparticle suspensions of these compounds, enabling new drug development and improved solubility and bioavailability of existing drugs.