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Purpose <p>Breast cancer continues to pose a significant global health burden, driving the need for improved therapeutic systems that are both effective and safe. Hesperidin (HSN), a naturally occurring flavonoid, exhibits notable anticancer and antioxidant activities; however, its therapeutic utility is restricted due to inadequate solubility, poor systemic availability, and rapid biotransformation. To address these challenges, the present study focused on the design and optimization of HSN-loaded nanostructured lipid carriers (HSN-NLCs) aimed at enhancing its delivery performance.</p> Methods <p>HSN-NLCs were formulated by high-pressure homogenization method using stearic acid and oleic acid as lipids and tween 80 as a surfactant, optimized via an Ishikawa-guided Quality by Design (QbD) approach using a Box–Behnken design. The formulations were characterized for physicochemical attributes, including particle size (PS), polydispersity index (PDI), zeta potential (ZP), and drug entrapment efficiency (EE), along with solid-state characterization using DSC and PXRD. Functional performance was assessed through <i>in vitro</i> release profiling, antioxidant potential (DPPH assay), cytotoxic activity against MCF-7 breast cancer cells, and in vivo pharmacokinetic studies in Albino Wistar rats.</p> Results <p>The optimized formulation produced nanosized carriers with a PS of 161 ± 1.75&#xa0;nm, surface charge (ZP: − 24.4 ± 1.12 mV), and high drug encapsulation (EE: 92.45 ± 1.6%) with narrow size distribution. Structural analyses indicated successful incorporation of HSN within the lipid matrix with reduced crystallinity. The system demonstrated controlled and sustained drug release under physiological pH conditions (1.2, 5.5, 6.8, and 7.4), improved membrane permeability, significant antioxidant activity, and marked cytotoxic effects in MCF-7 cells. Notably, in vivo studies confirmed an approximately 5-fold increase in oral bioavailability compared to unformulated HSN.</p> Conclusion <p>Overall, this study establishes that nanostructured lipid carrier-based delivery significantly improves the pharmacokinetic and therapeutic profile of HSN. The findings support the potential application of this nanocarrier system as a promising strategy for effective breast cancer management.</p>

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Hesperidin-loaded Nanostructured Lipid Carriers for Mammary Cancer: Optimized Delivery and Pharmacokinetic Enhancement via Quality-by-Design Development

  • 期刊论文

  • 发表日期：

    2026年5月14日

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  • Swati D. Raysing,
  • Nidhi R. Chaudhari,
  • Pankaj J. Jain,
  • Mayur S. Bagul

摘要

Purpose

Breast cancer continues to pose a significant global health burden, driving the need for improved therapeutic systems that are both effective and safe. Hesperidin (HSN), a naturally occurring flavonoid, exhibits notable anticancer and antioxidant activities; however, its therapeutic utility is restricted due to inadequate solubility, poor systemic availability, and rapid biotransformation. To address these challenges, the present study focused on the design and optimization of HSN-loaded nanostructured lipid carriers (HSN-NLCs) aimed at enhancing its delivery performance.

Methods

HSN-NLCs were formulated by high-pressure homogenization method using stearic acid and oleic acid as lipids and tween 80 as a surfactant, optimized via an Ishikawa-guided Quality by Design (QbD) approach using a Box–Behnken design. The formulations were characterized for physicochemical attributes, including particle size (PS), polydispersity index (PDI), zeta potential (ZP), and drug entrapment efficiency (EE), along with solid-state characterization using DSC and PXRD. Functional performance was assessed through in vitro release profiling, antioxidant potential (DPPH assay), cytotoxic activity against MCF-7 breast cancer cells, and in vivo pharmacokinetic studies in Albino Wistar rats.

Results

The optimized formulation produced nanosized carriers with a PS of 161 ± 1.75 nm, surface charge (ZP: − 24.4 ± 1.12 mV), and high drug encapsulation (EE: 92.45 ± 1.6%) with narrow size distribution. Structural analyses indicated successful incorporation of HSN within the lipid matrix with reduced crystallinity. The system demonstrated controlled and sustained drug release under physiological pH conditions (1.2, 5.5, 6.8, and 7.4), improved membrane permeability, significant antioxidant activity, and marked cytotoxic effects in MCF-7 cells. Notably, in vivo studies confirmed an approximately 5-fold increase in oral bioavailability compared to unformulated HSN.

Conclusion

Overall, this study establishes that nanostructured lipid carrier-based delivery significantly improves the pharmacokinetic and therapeutic profile of HSN. The findings support the potential application of this nanocarrier system as a promising strategy for effective breast cancer management.