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<p>Glioblastoma remains one of the most aggressive and treatment-resistant brain tumors, necessitating the development of more effective therapeutic strategies. This study aimed to formulate and evaluate <i>Melastomastrum capitatum</i>-loaded chitosan nanoparticles (MC-CSNPs) as a targeted drug delivery system for glioblastoma treatment. MC-CSNPs were successfully prepared using the ionic gelation method and characterized for physicochemical and biological properties. Among the formulations, F3 exhibited optimal performance with the smallest particle size (202.00 ± 1.15&#xa0;nm), highest encapsulation efficiency (89.60 ± 0.41%), and favorable zeta potential (+ 25.02 ± 0.1 mV), indicating good stability. FTIR and XRD analyses confirmed successful encapsulation and reduced crystallinity. SEM revealed rough, porous nanoparticles suitable for enhanced drug loading, while MC-CSNPs exhibited a biphasic, sustained drug release profile, with formulation F3 achieving the highest cumulative release (~ 94.8% at 72&#xa0;h). Drug release followed first-order kinetics, with F3 showing the best fit (R² = 0.989), indicating concentration-dependent and controlled release behavior. Biological evaluations demonstrated that MC-CSNPs significantly reduced brain tumor cell viability (27.60 ± 2.22% at 100&#xa0;µg/mL) compared to the free extract. Enhanced cellular uptake (67.85 ± 3.52%) and apoptosis induction (72.50 ± 4.21%) further confirmed their superior anticancer activity. In vivo studies showed improved body weight gain and increased apoptotic activity in treated groups, with MC-CSNPs outperforming the free extract. Additionally, MC-CSNPs effectively reduced oxidative stress (ROS: 30.12 ± 1.75), restored mitochondrial membrane potential (ΔΨm: 4.45 ± 0.38), and improved antioxidant enzyme activities. Histopathological analysis revealed significant neuroprotection and reduced tumor-induced damage. Overall, MC-CSNPs demonstrated enhanced therapeutic efficacy through improved drug delivery, increased apoptosis, and reduced oxidative stress, highlighting their potential as a promising nanocarrier system for glioblastoma treatment.</p>

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Designing chitosan nanoparticles as a plant-derived drug carrier for brain tumor prevention and treatment

  • 期刊论文

  • 发表日期：

    2026年4月6日

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  • Cletus Anes Ukwubile,
  • Ibrahim Iliya,
  • Nnamdi David Menkiti

摘要

Glioblastoma remains one of the most aggressive and treatment-resistant brain tumors, necessitating the development of more effective therapeutic strategies. This study aimed to formulate and evaluate Melastomastrum capitatum-loaded chitosan nanoparticles (MC-CSNPs) as a targeted drug delivery system for glioblastoma treatment. MC-CSNPs were successfully prepared using the ionic gelation method and characterized for physicochemical and biological properties. Among the formulations, F3 exhibited optimal performance with the smallest particle size (202.00 ± 1.15 nm), highest encapsulation efficiency (89.60 ± 0.41%), and favorable zeta potential (+ 25.02 ± 0.1 mV), indicating good stability. FTIR and XRD analyses confirmed successful encapsulation and reduced crystallinity. SEM revealed rough, porous nanoparticles suitable for enhanced drug loading, while MC-CSNPs exhibited a biphasic, sustained drug release profile, with formulation F3 achieving the highest cumulative release (~ 94.8% at 72 h). Drug release followed first-order kinetics, with F3 showing the best fit (R² = 0.989), indicating concentration-dependent and controlled release behavior. Biological evaluations demonstrated that MC-CSNPs significantly reduced brain tumor cell viability (27.60 ± 2.22% at 100 µg/mL) compared to the free extract. Enhanced cellular uptake (67.85 ± 3.52%) and apoptosis induction (72.50 ± 4.21%) further confirmed their superior anticancer activity. In vivo studies showed improved body weight gain and increased apoptotic activity in treated groups, with MC-CSNPs outperforming the free extract. Additionally, MC-CSNPs effectively reduced oxidative stress (ROS: 30.12 ± 1.75), restored mitochondrial membrane potential (ΔΨm: 4.45 ± 0.38), and improved antioxidant enzyme activities. Histopathological analysis revealed significant neuroprotection and reduced tumor-induced damage. Overall, MC-CSNPs demonstrated enhanced therapeutic efficacy through improved drug delivery, increased apoptosis, and reduced oxidative stress, highlighting their potential as a promising nanocarrier system for glioblastoma treatment.