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Antinociceptive Effect of a p-Cymene/β-Cyclodextrin Inclusion Complex in a Murine Cancer Pain Model: Characterization
Wagner B R Santos1, Lícia T S Pina1, Marlange A de Oliveira2
1Departament of Pharmacy, Federal University of Sergipe, São Cristóvão 49100-000, SE, Brazil.
Molecules (Basel, Switzerland)
|June 10, 2023
Summary
This study shows that complexing p-cymene (PC) with beta-cyclodextrin (β-CD) effectively treats cancer pain. The PC/β-CD complex significantly reduced pain in a mouse model, unlike free PC, improving its therapeutic effects.
Area of Science:
- Pharmacology
- Medicinal Chemistry
- Pain Management
Background:
- Cancer pain is a prevalent and challenging symptom, often inadequately managed by conventional drugs due to adverse reactions.
- p-Cymene (PC), a monoterpene, exhibits antinociceptive properties but faces physicochemical and pharmacological limitations due to its lipophilicity.
- Beta-cyclodextrins (β-CD) are explored to enhance the properties of lipophilic compounds like PC.
Purpose of the Study:
- To create, characterize, and evaluate the efficacy of a p-cymene and β-cyclodextrin complex (PC/β-CD) in a cancer pain model.
- To determine if PC/β-CD complexation improves the antinociceptive effects of p-cymene.
- To assess the effectiveness of PC/β-CD in managing pain associated with Sarcoma 180 (S180) tumors.
Main Methods:
- Molecular docking was employed to predict the feasibility of PC and β-CD complex formation.
- The PC/β-CD complex was synthesized using slurry complexation and characterized by High-Performance Liquid Chromatography (HPLC) and Nuclear Magnetic Resonance (NMR) spectroscopy.
- The antinociceptive effects of PC/β-CD were evaluated in a Sarcoma 180 (S180)-induced cancer pain model in vivo.
Main Results:
- Molecular docking simulations indicated a favorable interaction between PC and β-CD.
- The PC/β-CD complex exhibited a high complexation efficiency of 82.61%, confirmed by NMR spectroscopy showing PC encapsulated within the β-CD cavity.
- In the S180 cancer pain model, PC/β-CD significantly reduced mechanical hyperalgesia and nociception (p < 0.05) at tested doses, unlike free PC (p > 0.05).
Conclusions:
- Complexation of p-cymene (PC) with β-cyclodextrin (β-CD) successfully overcomes the limitations of free PC.
- The PC/β-CD complex demonstrates enhanced pharmacological efficacy in managing cancer pain compared to p-cymene alone.
- This approach offers a promising strategy for improving the therapeutic potential of p-cymene in cancer pain management by reducing the required dose.
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