Antitubercular Activity of 7-Methyljuglone-Loaded Poly-(Lactide Co-Glycolide) Nanoparticles

Area of Science:

• Natural product drug delivery
• Nanomedicine for infectious diseases
• Polymer-based drug carriers

Background:

• Natural products are explored for treating diseases like tuberculosis (TB).
• Poly-(lactide-co-glycolic) acid (PLGA) nanoparticles are investigated as drug delivery systems.
• 7-methyljuglone (7-MJ), a compound from *Euclea natalensis*, was studied.

Purpose of the Study:

• To investigate the use of PLGA nanoparticles loaded with 7-methyljuglone (7-MJ).
• To evaluate the antimycobacterial and cytotoxic effects of 7-MJ and its PLGA nanoparticles.
• To assess the cellular uptake of 7-MJ PLGA nanoparticles.

Main Methods:

• Antimycobacterial activity testing against *Mycobacterium smegmatis* and *Mycobacterium tuberculosis* (drug-susceptible and MDR).
• Cytotoxicity assessment using differentiated U937 cells.
• Engulfment studies to determine nanoparticle uptake by U937 cells.

Main Results:

• 7-MJ demonstrated antimycobacterial activity with MIC values of 1.6 µg/mL and 0.4 µg/mL.
• Free 7-MJ exhibited cytotoxicity (IC50 of 3.25 µg/mL) against U937 cells.
• 7-MJ PLGA nanoparticles showed an 80-fold decrease in cytotoxicity and were taken up by U937 cells.

Conclusions:

• PLGA nanoparticles offer a potential strategy to reduce 7-MJ's cytotoxicity.
• The study suggests improved delivery possibilities for TB therapy using PLGA nanoparticles.
• Nanoparticle formulation enhances the therapeutic potential of natural products.