Hydrophobic small molecule drugs and nutraceuticals present obstacles for oral administration. Their poor aqueous solubility and large oil/water partition coefficients often result in poor in vivo bioavailability. Many hemp-derived cannabinoids exist naturally as hydrophobic oils, which are obtained by extraction from plant material. With the recent rise in popularity of cannabinoid containing nutraceutical supplements, there is a need to investigate formulation approaches for enhanced delivery of hydrophobic cannabinoid active ingredients. One approach to improve the oral delivery of hydrophobic actives is nanoparticle encapsulation, where the greater surface area afforded by the nanoparticles, along with the free energy advantage of the amorphous drug core, may enhance the release of the drug. The encapsulation of hemp-derived cannabinoids, many of which exist primarily as liquid oils, poses additional challenges to the formation, solidification, and characterization of these nanoparticles. Here, we investigate the encapsulation of cannabidiol (CBD) as a model. CBD in its amorphous state has a low glass transition temperature and at ambient temperature exists as a nonaqueous liquid. We show that amorphous CBD can be effectively encapsulated into nanoparticles with low polydispersity and high drug loading via Flash NanoPrecipitation, a scalable self-assembly process. Two naturally derived polymers, HPMCAS and lecithin, are employed as amphiphilic particle stabilizers. The resulting nanoparticle suspensions are size stable over time and are thus suitable for further downstream processing. We describe an in-vitro release assay developed for these nanoparticles and show that the nanoencapsulation can enhance the release rate of CBD compared to the CBD starting material.

Nanoencapsulation of cannabidiol via flash nanoprecipitation with naturally derived polymer stabilizers

ACS Spring 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.