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Papers of the Week


Papers: 10 Jun 2023 - 16 Jun 2023

RESEARCH TYPE:
Basic Science


Animal Studies, In Silico Studies, Molecular/Cellular, Pharmacology/Drug Development

PAIN TYPE:
Cancer Pain, Psychological/Comorbidities


2023 May 31


Molecules


37298941


28


11

Antinociceptive Effect of a p-Cymene/β-Cyclodextrin Inclusion Complex in a Murine Cancer Pain Model: Characterization Aided through a Docking Study.

Authors

Santos WBR, Pina LTS, de Oliveira MA, Santos LABO, Batista MVA, Trindade GGG, Duarte MC, Almeida JRGS, Quintans-Júnior LJ, Quintans JSS, Serafini MR, Coutinho HDM, Kowalska G, Baj T, Kowalski R, Guimarães AG

Abstract

Pain is one of the most prevalent and difficult to manage symptoms in cancer patients, and conventional drugs present a range of adverse reactions. The development of β-cyclodextrins (β-CD) complexes has been used to avoid physicochemical and pharmacological limitations due to the lipophilicity of compounds such as p-Cymene (PC), a monoterpene with antinociceptive effects. Our aim was to obtain, characterize, and measure the effect of the complex of p-cymene and β-cyclodextrin (PC/β-CD) in a cancer pain model. Initially, molecular docking was performed to predict the viability of complex formation. Afterward, PC/β-CD was obtained by slurry complexation, characterized by HPLC and NMR. Finally, PC/β-CD was tested in a Sarcoma 180 (S180)-induced pain model. Molecular docking indicated that the occurrence of interaction between PC and β-CD is favorable. PC/β-CD showed complexation efficiency of 82.61%, and NMR demonstrated PC complexation in the β-CD cavity. In the S180 cancer pain model, PC/β-CD significantly reduced the mechanical hyperalgesia, spontaneous nociception, and nociception induced by non-noxious palpation at the doses tested ( < 0.05) when compared to vehicle differently from free PC ( > 0.05). Therefore, the complexation of PC in β-CD was shown to improve the pharmacological effect of the drug as well as reducing the required dose.