Antinociceptive effect of a p-cymene/β-cyclodextrin Inclusion complex in a murine cancer pain model: characterization aided through a docking study.
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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 -cyclodextrins ( -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 -cyclodextrin (PC/ -CD) in a cancer pain model. Initially, molecular docking was performed to predict the viability of complex formation. Afterward, PC/ -CD was obtained by slurry complexation, characterized by HPLC and NMR. Finally, PC/ -CD was tested in a Sarcoma 180 (S180)-induced pain model. Molecular docking indicated that the occurrence of interaction between PC and -CD is favorable. PC/ -CD showed complexation efficiency of 82.61%, and NMR demonstrated PC complexation in the -CD cavity. In the S180 cancer pain model, PC/ -CD significantly reduced the mechanical hyperalgesia, spontaneous nociception, and nociception induced by non-noxious palpation at the doses tested (p < 0.05) when compared to vehicle differently from free PC (p > 0.05). Therefore, the complexation of PC in -CD was shown to improve the pharmacological effect of the drug as well as reducing the required dose.
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Rekord utworzony: | 1 czerwca 2023 08:54 |
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Ostatnia aktualizacja: | 27 czerwca 2024 13:57 |