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<p>Oral cancer is a prevalent malignancy in developing countries, with treatment hampered by poor drug solubility, low bioavailability, and systemic toxicity of conventional therapies. This study presents a targeted and optimized mesoporous silica nanoparticulate drug delivery system (MSNP) for curcumin to overcome these limitations. Curcumin was encapsulated in functionalized MCM 41 nanoparticles using the solvent evaporation method, with folic acid conjugation enabling tumor-targeting via folate receptors. The formulation was optimized using Box-Behnken Design, considering variables like drug-to-polymer ratio, stirring speed, and time. The optimized nanoparticles exhibited a particle size of 531 ± 7.5&#xa0;nm and an entrapment efficiency of 83.63 ± 0.02%. Characterization using FTIR, SEM, DSC, NMR, and XRD confirmed drug encapsulation and structural integrity. In vitro release showed sustained curcumin release over 24&#xa0;h with Higuchi kinetics. In vivo pharmacokinetic studies in rats showed a twofold increase in AUC (521.23 ± 6.02&#xa0;ng&#xa0;h/mL) and a threefold increase in C<sub>max</sub> (36.32 ± 0.21&#xa0;ng/mL) compared to free curcumin. This nanoparticulate system significantly enhances curcumin’s solubility and bioavailability, offering a promising therapeutic strategy for oral cancer.</p>

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Functionalized Curcumin-Loaded Mesoporous Nanoparticulate Drug Delivery System for Oral Cancer: Formulation Design, Optimization, and In Vitro & In Vivo Evaluation

  • 期刊论文

  • 发表日期：

    2025年7月24日

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  • Priya Patel,
  • Anand Gondhiya,
  • Nasir Vadia,
  • Devesh U. Kapoor,
  • Bhupendra G. Prajapati

摘要

Oral cancer is a prevalent malignancy in developing countries, with treatment hampered by poor drug solubility, low bioavailability, and systemic toxicity of conventional therapies. This study presents a targeted and optimized mesoporous silica nanoparticulate drug delivery system (MSNP) for curcumin to overcome these limitations. Curcumin was encapsulated in functionalized MCM 41 nanoparticles using the solvent evaporation method, with folic acid conjugation enabling tumor-targeting via folate receptors. The formulation was optimized using Box-Behnken Design, considering variables like drug-to-polymer ratio, stirring speed, and time. The optimized nanoparticles exhibited a particle size of 531 ± 7.5 nm and an entrapment efficiency of 83.63 ± 0.02%. Characterization using FTIR, SEM, DSC, NMR, and XRD confirmed drug encapsulation and structural integrity. In vitro release showed sustained curcumin release over 24 h with Higuchi kinetics. In vivo pharmacokinetic studies in rats showed a twofold increase in AUC (521.23 ± 6.02 ng h/mL) and a threefold increase in Cmax (36.32 ± 0.21 ng/mL) compared to free curcumin. This nanoparticulate system significantly enhances curcumin’s solubility and bioavailability, offering a promising therapeutic strategy for oral cancer.