Cannabinoids and Neuropathic Pain

Brownjohn, Philip W.; Ashton, John C.

doi:10.5772/36889

Cited by 2 publications

(1 citation statement)

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“…This cannabinoid continues to attract special attention in oncology due to its palliative effects and antitumor activity; Δ 9 -THC has been reported to inhibit tumor angiogenesis and cell growth in malignant tissues, leading to cell death 2 – 4 . Unfortunately, this drug presents a major challenge for the design of a suitable pharmaceutical dosage for clinical use, due to its unfavorable physicochemical properties; high instability, oily-resin nature, low solubility in water and low bioavailability, along with psychotropic side effects 5 . In addition, its anticancer effect is frequently subject to resistance mechanisms, some of them strongly related to the actual dose reaching the target site 4 , which is subsequently dependent on the dosage form.…”

Section: Introductionmentioning

confidence: 99%

Receptor-targeted nanoparticles modulate cannabinoid anticancer activity through delayed cell internalization

Durán‐Lobato

Álvarez-Fuentes

Fernández‐Arévalo

et al. 2022

Sci Rep

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AbstractΔ9-tetrahydrocannabinol (Δ9-THC) is known for its antitumor activity and palliative effects. However, its unfavorable physicochemical and biopharmaceutical properties, including low bioavailability, psychotropic side effects and resistance mechanisms associated to dosing make mandatory the development of successful drug delivery systems. In this work, transferring (Tf) surface-modified Δ9-THC-loaded poly(lactide-co-glycolic) nanoparticles (Tf-THC-PLGA NPs) were proposed and evaluated as novel THC-based anticancer therapy. Furthermore, in order to assess the interaction of both the nanocarrier and the loaded drug with cancer cells, a double-fluorescent strategy was applied, including the chemical conjugation of a dye to the nanoparticle polymer along with the encapsulation of either a lipophilic or a hydrophilic dye. Tf-THC PLGA NPs exerted a cell viability decreased down to 17% vs. 88% of plain nanoparticles, while their internalization was significantly slower than plain nanoparticles. Uptake studies in the presence of inhibitors indicated that the nanoparticles were internalized through cholesterol-associated and clathrin-mediated mechanisms. Overall, Tf-modification of PLGA NPs showed to be a highly promising approach for Δ9-THC-based antitumor therapies, potentially maximizing the amount of drug released in a sustained manner at the surface of cells bearing cannabinoid receptors.

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