Selepe, Cyril TDhlamini, Khanyisile STshweu, Lesego LKwezi, LusisizweRamalapa, Bathabile ERay, Suprakas S2025-02-282025-02-282024-121438-74921439-2054https://doi.org/10.1002/mame.202400283http://hdl.handle.net/10204/14114Betulinic acid (BA) is a promising natural anti-tumor agent renowned for its activity against various tumor cell types. Despite its favorable profile of low cytotoxicity to normal cells, BA’s inherent hydrophobic nature and relatively short systematic half-life impose hurdles for clinical application. This study introduces a strategy to surmount these obstacles by developing a drug delivery system employing poly(lactic-co-glycolic acid) (PLGA)-encapsulated BA nanoparticles (PLGA-BA NPs). Rigorous characterization techniques such as dynamic light scattering (DLS), x-ray diffraction (XRD), and scanning electron microscopy (SEM) analyses are employed to confirm the integrity of the drug within the nanocarriers. The PLGA-BA NPs demonstrated a mean particle size of 196 ± 6.80 nm. XRD analysis demonstrated the amorphous state of the PLGA-BA formulation, a characteristic vital for sustained drug release and enhanced bioavailability. The PLGA-BA NPs exhibited spherical morphology with encapsulation and loading efficiency of 83 ± 9.24% and 7.0 ± 0.4%, respectively, highlighting efficient encapsulation of the drug within the PLGA NPs. In vitro, cytotoxicity assessments demonstrated enhanced anti-proliferative efficacy against breast and lung tumor cells when utilizing PLGA-BA NPs in comparison to free BA. This research underlines the potential of employing the developed PLGA-based nanocarrier to optimize the therapeutic efficacy of BA.FulltextenBetulinic acidTumor cell typesPoly(lactic-co-glycolic acid)PLGAArticleN/A