Preparation and characterization of Δ⁹-tetrahydrocannabinol-loaded biodegradable polymeric microparticles and their antitumoral efficacy on cancer cell lines

Abstract

Cannabinoids present an interesting therapeutic potential as antiemetics, appetite stimulants in debilitating diseases (cancer, AIDS and multiple sclerosis), analgesics, and in the treatment of multiple sclerosis and cancer, among other conditions. However, despite their high clinical potential, only few dosage forms are available to date. In this paper, the development of Δ(9)-tetrahydrocannabinol (THC) biodegradable microspheres as an alternative delivery system for cannabinoid parenteral administration is proposed. Tetrahydrocannabinol was encapsulated into biodegradable microspheres by the oil-in-water (o/w) emulsion solvent evaporation method. Several formulations were prepared using different drug:polymer ratios. The influence of antioxidant (α-tocopherol acetate) concentration on the release of THC from the microparticles was studied. Elevated process yield and entrapment efficiencies were achieved. The in vitro drug release studies showed that the encapsulated drug was released over a two week period. As THC has shown therapeutic potential as anticancer drug, the efficacy of the microspheres was tested on different cancer cell lines. Interestingly, the microspheres were able to inhibit cancer cell proliferation during the nine-day study period. All the above results suggest that the use of biodegradable microspheres would be a suitable alternative delivery system for THC administration.

New hydrazonoindolin-2-ones: Synthesis, exploration of the possible anti-proliferative mechanism of action and encapsulation into PLGA microspheres

“…These results indicate the efficiency of the preparation method and optimization of the preparation parameters such as the concentration and viscosity of the polymer solution. The obtained results are consistent with the previously reported studies for different drugs [40][41][42].…”

Anti-Cancer Potential of Cannabinoids, Terpenes, and Flavonoids Present in Cannabis

“…THC biodegradable microspheres were developed for an alternative cannabinoid delivery system than the usual oral route. The THC microspheres were able to inhibit cell proliferation of multiple cancers, including Caco-2 colon cancer cells, over a 9 day period [90].…”

Anti-carcinogenic activity of anandamide on human glioma in vitro and in vivo

“…Currently, there is a burgeoning interest in the study of the therapeutic effects of cannabinoids in different cancer types. It was demonstrated that cannabinoids and their derivatives exert anti-proliferative, pro-apoptotic, anti-migratory and anti-invasive actions in a wide spectrum of cancer cells in culture ( 3 – 5 ). δ9-Tetrahydrocannabinol, a cannabinoid, was reported to induce apoptosis in glioma cells through modulating the activity of the sphingomyelin cycle ( 6 ).…”