Lupeol-loaded PLGA particles conserve anti-topoisomerase activity and decrease the cytotoxicity of lupeol

Area of Science:

• Biomaterials Science
• Nanotechnology
• Pharmacology

Background:

• Lupeol (LP) is a bioactive triterpene with known chemoprotective, anti-inflammatory, and anti-arthritic properties.
• Enhancing the bioavailability and safety of LP is crucial for its therapeutic applications.
• Nanoparticle-based drug delivery systems offer a promising approach to overcome these limitations.

Purpose of the Study:

• To develop and characterize lupeol-loaded polylactic-co-glycolic acid (PLGA) nanoparticles, designated T_LP14.
• To evaluate the biological activity, cytotoxicity, and safety profile of the T_LP14 formulation.
• To assess the potential of T_LP14 as a controlled-release system for lupeol.

Main Methods:

• Lupeol-loaded PLGA nanoparticles (T_LP14) were prepared using the emulsification-evaporation method.
• Nanoparticle characterization included size, polydispersity index (PdI), and encapsulation efficiency.
• Biological activity was assessed via topoisomerase II inhibition assays, in vitro cytotoxicity assays on BEAS-2 and HEPG2 cell lines, and ex vivo studies on peripheral blood mononuclear cells.

Main Results:

• T_LP14 nanoparticles exhibited an average size of 339.8 nm, PdI of 0.240, and 38% encapsulation efficiency.
• Encapsulation did not impair the topoisomerase II inhibitory activity of lupeol.
• T_LP14 showed minimal cytotoxicity in non-tumor cells at concentrations up to 1250 μg/mL and significantly reduced lupeol-induced apoptosis in peripheral blood mononuclear cells.

Conclusions:

• T_LP14 nanoparticles represent a viable controlled-release system for lupeol.
• The formulation enhances lupeol's safety profile by reducing apoptosis.
• T_LP14 holds potential for improved therapeutic outcomes due to preserved activity and enhanced safety.