<p>Allicin, an organosulfur compound derived from garlic, exhibits effective cellular activities, but its administration is often hindered by poor bioavailability and relative instability. To address these limitations, Soluplus-based polymeric micelles were engineered to encapsulate allicin and evaluated for their chemosensitizing or chemoprotective capacity with doxorubicin. The micelles displayed uniform spherical nanoparticles (~ 74&#xa0;nm, PDI ~ 0.21) with nearly complete encapsulation efficiency. Compared with free allicin, micellar formulations showed markedly reduced release (~ 16% vs. ~50%) at physiological temperature, indicating improved drug retention. Stability assessments revealed particle size and zeta potential were time-dependent but unaffected by temperature. FTIR confirmed successful encapsulation, while thermogravimetric analysis demonstrated thermal stability up to 250–300&#xa0;°C. In vitro, treatment with the allicin-Soluplus micelles prior to doxorubicin treatment exhibited a cell-model-dependent modulation of doxorubicin response. A partial protective metabolic response was observed in myocardial cells H9C2 and colorectal adenocarcinoma CACO2 cells. An opposite effect was observed on prostate adenocarcinoma DU145 cells, in which allicin exhibited a chemosensitizing effect with doxorubicin. These preliminary in vitro findings highlight Soluplus micelles as a promising delivery platform to stabilize allicin and potentiate its therapeutic effect in oncotherapy.</p>

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Allicin-loaded soluplus polymeric micelles differentially modulate doxorubicin response in adenocarcinoma and myocardial cell models

  • Khaldoun J. Al-Hadid,
  • Walhan Alshaer,
  • Baidaa AlQuaissi,
  • Bayan Ziad Al-Momany,
  • Nowar Alsarayreh,
  • Dana A. Alqudah,
  • Tasneem Alsheleh

摘要

Allicin, an organosulfur compound derived from garlic, exhibits effective cellular activities, but its administration is often hindered by poor bioavailability and relative instability. To address these limitations, Soluplus-based polymeric micelles were engineered to encapsulate allicin and evaluated for their chemosensitizing or chemoprotective capacity with doxorubicin. The micelles displayed uniform spherical nanoparticles (~ 74 nm, PDI ~ 0.21) with nearly complete encapsulation efficiency. Compared with free allicin, micellar formulations showed markedly reduced release (~ 16% vs. ~50%) at physiological temperature, indicating improved drug retention. Stability assessments revealed particle size and zeta potential were time-dependent but unaffected by temperature. FTIR confirmed successful encapsulation, while thermogravimetric analysis demonstrated thermal stability up to 250–300 °C. In vitro, treatment with the allicin-Soluplus micelles prior to doxorubicin treatment exhibited a cell-model-dependent modulation of doxorubicin response. A partial protective metabolic response was observed in myocardial cells H9C2 and colorectal adenocarcinoma CACO2 cells. An opposite effect was observed on prostate adenocarcinoma DU145 cells, in which allicin exhibited a chemosensitizing effect with doxorubicin. These preliminary in vitro findings highlight Soluplus micelles as a promising delivery platform to stabilize allicin and potentiate its therapeutic effect in oncotherapy.