Anti-Tumor Efficiency of Perillylalcohol/β-Cyclodextrin Inclusion Complexes in a Sarcoma S180-Induced Mice Model

Area of Science:

• Pharmacology
• Materials Science
• Oncology

Background:

• Low solubility and high volatility of perillyl alcohol (POH) limit its bioavailability and therapeutic potential.
• Perillyl alcohol is a monoterpene with promising anticancer properties.

Purpose of the Study:

• To enhance the anticancer activity of perillyl alcohol by complexing it with beta-cyclodextrin (β-CD).
• To evaluate the efficacy of the POH/β-CD complex in a sarcoma S180-induced mice model.

Main Methods:

• Complexation of POH with β-CD using three different approaches.
• Molecular docking, thermal analysis, and FTIR spectroscopy to characterize the complexes.
• In vitro cytotoxicity testing on L929 fibroblasts and in vivo efficacy studies in mice.

Main Results:

• Molecular docking indicated a 1:1 molar ratio for POH-β-CD complexation via hydrogen bonding.
• Complexation confirmed by thermal analysis and FTIR, showing POH enclosed in β-CD cavity with reduced particle size.
• POH/β-CD showed no cytotoxicity to L929 fibroblasts and achieved ~60% tumor growth inhibition in mice.
• Reduced Ki67 antigen expression indicated decreased cell proliferation and tumor growth.

Conclusions:

• Complexation with β-CD effectively addresses POH's volatility and solubility issues.
• The POH/β-CD complex demonstrates enhanced antitumor efficacy and reduced tumor cell proliferation.
• This formulation represents a promising strategy for improving perillyl alcohol's use as a chemotherapeutic agent.