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Background <p>The oral route is the most preferred drug delivery method for treating both chronic and acute diseases due to its ease of administration and high patient compliance. However, sesamol (SM), a natural bioactive compound, exhibits promising antioxidant and anticancer activity but suffers from poor water solubility, inconsistent absorption, and low bioavailability, limiting its therapeutic potential. This study aimed to develop SM-loaded hybrid nanoparticles (HNP) composed of a polymer-lipid matrix to enhance bioavailability and therapeutic efficacy for its antioxidant potential and anticancer activity.</p> Method <p>SMHNP were formulated using homogenization and ionotropic gelation techniques and optimized by Box-Behnken design using design expert software. The SMHNP were evaluated through in-vitro and in vivo studies using the albino Wistar rat model.</p> Results <p>The optimized SMHNP formulation (SMHNP13) exhibits a particle size of 177.6 ± 4.7&#xa0;nm, a polydispersity index of 0.179, and a zeta potential of 27.2 mV. Scanning electron microscopy (SEM) confirmed that the particles were spherical and non-aggregated. FTIR and X-ray diffraction (XRD) analyses indicated successful drug encapsulation within the HNP matrix. The SMHNP13 formulation exhibited a sustained drug release profile, with 92.81 ± 3.76% release over 24&#xa0;h, attributed to its nanosize and encapsulation. It displayed 2.45-fold higher ex-vivo intestinal permeation and significantly higher in-vitro antioxidant activity (<i>P</i> &lt; 0.05) at all tested concentrations than pure SM. It also increased cytotoxicity against SK-LU-1 cells (IC50 = 590.23 µM) compared to pure SM (IC50 = 1510.12 µM) and demonstrated a 3.33-fold higher relative bioavailability than pure SM.</p> Conclusion <p>The results indicate that HNP are a promising strategy for enhancing the oral bioavailability and therapeutic potential of sesamol. Further preclinical investigations are needed to confirm their clinical applicability.</p> Graphical Abstract <p></p>

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Development of Sesamol Loaded-Polymer-Lipid Blend Nanoparticles: Statistical Optimization, In-Vitro, and Preclinical Assessment

  • 期刊论文

  • 发表日期：

    2025年6月23日

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  • Ameeduzzafar Zafar,
  • Mohd Yasir,
  • Md Ali Mujtaba,
  • Mohammad Khalid,
  • Dibya Sundar Panda,
  • Lubhan Singh,
  • Omar Awad Alsaidan,
  • Anwarulabedin Mohsin Quazi

摘要

Background

The oral route is the most preferred drug delivery method for treating both chronic and acute diseases due to its ease of administration and high patient compliance. However, sesamol (SM), a natural bioactive compound, exhibits promising antioxidant and anticancer activity but suffers from poor water solubility, inconsistent absorption, and low bioavailability, limiting its therapeutic potential. This study aimed to develop SM-loaded hybrid nanoparticles (HNP) composed of a polymer-lipid matrix to enhance bioavailability and therapeutic efficacy for its antioxidant potential and anticancer activity.

Method

SMHNP were formulated using homogenization and ionotropic gelation techniques and optimized by Box-Behnken design using design expert software. The SMHNP were evaluated through in-vitro and in vivo studies using the albino Wistar rat model.

Results

The optimized SMHNP formulation (SMHNP13) exhibits a particle size of 177.6 ± 4.7 nm, a polydispersity index of 0.179, and a zeta potential of 27.2 mV. Scanning electron microscopy (SEM) confirmed that the particles were spherical and non-aggregated. FTIR and X-ray diffraction (XRD) analyses indicated successful drug encapsulation within the HNP matrix. The SMHNP13 formulation exhibited a sustained drug release profile, with 92.81 ± 3.76% release over 24 h, attributed to its nanosize and encapsulation. It displayed 2.45-fold higher ex-vivo intestinal permeation and significantly higher in-vitro antioxidant activity (P < 0.05) at all tested concentrations than pure SM. It also increased cytotoxicity against SK-LU-1 cells (IC50 = 590.23 µM) compared to pure SM (IC50 = 1510.12 µM) and demonstrated a 3.33-fold higher relative bioavailability than pure SM.

Conclusion

The results indicate that HNP are a promising strategy for enhancing the oral bioavailability and therapeutic potential of sesamol. Further preclinical investigations are needed to confirm their clinical applicability.

Graphical Abstract