Development and Characterization of New Cannabidiol-Loaded Polycaprolactone Nanoparticles for Increased Bioavailability

Abstract

The potential therapeutic applications of herbal cannabidiol (CBD) extend to various health conditions such as multiple sclerosis, cancer, insomnia, and anxiety. However, the practical use of CBD for medicinal purposes is hindered by its high lipophilicity, bioavailability and dosing. To overcome this, CBD was encapsulated in the biodegradable and biocompatible polymer polycaprolactone (PCL) ensuring prolonged release. Ultrasonication and oil-in-water emulsion were employed to fabricate PCL nanoparticles (NPs), and at optimal conditions, different amounts of CBD were encapsulated within PCL NPs. Morphological and physicochemical characteristics of the nanoparticles were evaluated via FE-SEM, STEM, zeta sizer, HPLC, FT-IR and DSC analyses. The blank and CBD-loaded NPs exhibited mean particle diameters in between 207.5 nm and 227.7 nm with charges ranging −23.37 and −9.40 mV. The stabilities of the NPs were evaluated for 4-day period and NPs are found to be stable in terms of size and zeta potential. Release kinetics of CBD-loaded NPs were found to fit Zero-order kinetic model at pH 1.2 and Higuchi kinetic model at pH 7.4. The internalization of NPs into fibroblast cells was depicted using fluorescence microscopy. The effect of CBD and NPs-4 on the proliferation of the fibroblast and breast cancer cells were demonstrated. The results clearly indicate that the NP formulation reduced the toxic effects of CBD on both cell types. The findings suggest the potential application of innovative NPs as carriers for sustained release of CBD to be used in new formulations.