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Papers of the Week

Papers: 29 Jan 2022 - 4 Feb 2022

Pharmacology/Drug Development

2022 Jan 29

Int J Pharm

Potential Use for Chronic Pain: Poly(Ethylene Glycol)-Poly(Lactic-Co-Glycolic Acid) Nanoparticles Enhance the Effects of Cannabis-Based Terpenes on Calcium Influx in TRPV1-Expressing Cells.


El-Hammadi MM, Small-Howard AL, Jansen C, Fernández-Arévalo M, Turner H, Martín-Banderas L
Int J Pharm. 2022 Jan 29:121524.
PMID: 35104595.


The objective of these in vitro studies was to investigate the impact of the encapsulation of three cannabis-based terpenes, namely β-myrcene (MC), β-caryophyllene (CPh), and nerolidol (NL), on their potential efficacy in pain management. Terpene-encapsulated poly(ethylene glycol)-poly(lactic-co-glycolic acid) nanoparticles (PEG-PLGA NPs) were prepared by an emulsion-solvent evaporation method. The terpene-loaded NPs were examined in HEK293 cells that express the nociceptive transient receptor potential vanilloid-1 (TRPV1), an ion channel involved in pain perception. TRPV1 activation was assessed by monitoring calcium influx kinetics over 1h in cells pre-treated with the fluorescent indicator Fluo-4. In addition, the fluorescence intensity changes induced by the NPs in living cells were also explored by a fluorescence microscope. Furthermore, the cytotoxicity of the terpene-loaded NPs was evaluated by the 3-(4,5-dimethylthiazol-2-yl)-3,5-diphenyl tetrazolium bromide (MTT) proliferation assay. The terpene-loaded NPs had a diameter in the range of 250-350nm and a zeta potential of approximately -20mV. The encapsulation efficiency was 18.5%, 51.3%, and 60.3% for MC, NL, and CPh NPs, respectively. The nano-formulations significantly increased the fluorescence intensity in comparison with free terpenes. Furthermore, combinations of terpene-loaded NPs produced significantly higher calcium responses when compared to combinations of free terpenes. Similar findings were shown by the fluorescence images. In conclusion, the terpene-PLGA NPs can be promising therapeutics for more effective pain management.