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Objective <p>The objective of this study was to develop and evaluate PEG-2000 coated solid lipid nanoparticles (PEG-Ber-SLN) for encapsulating berberine, aiming to extend its biological half-life and systemic circulation for enhanced breast cancer therapy.</p> Methods <p>PEG-Ber-SLN was formulated and characterized for particle size, zeta potential, entrapment efficiency, morphology, drug release profile, and drug-excipient interaction. Cellular uptake and internalization studies were conducted in AMJ-13 and BT-20 breast cancer cell lines, while cytotoxicity was assessed using the MCF-7 cell line. Pharmacokinetic and biodistribution studies were carried out in rats.</p> Results <p>The PEG-Ber-SLN exhibited a nanometric particle size of 206 ± 8.3&#xa0;nm, a zeta potential of − 24.3 ± 8.5 mV, and an entrapment efficiency of 74 ± 3%. In-vitro release showed 75% drug release over 72&#xa0;h following Higuchi kinetics. Cellular internalization was significantly enhanced. Compared to berberine solution, PEG-Ber-SLN demonstrated increased half-life (t₁/₂), mean residence time (MRT), and reduced clearance. Biodistribution studies showed higher accumulation in breast tissue, indicating effective passive targeting.</p> Conclusions <p>PEG-Ber-SLN represents a promising nanocarrier system to improve berberine’s pharmacokinetic profile and targeting efficacy for breast cancer treatment by enhancing circulation time and site-specific accumulation.</p> Graphical Abstract <p></p>

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Enhancing Pharmacokinetics and Therapeutic Efficacy of Berberine via PEGylated Nanocarriers for Breast Cancer Treatment

  • 期刊论文

  • 发表日期：

    2026年3月25日

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  • Deepa Yadav,
  • Bhupesh C. Semwal,
  • Hitesh Kumar Dewangan,
  • Mohamed Rahamathulla,
  • Syeda Ayesha Farhana,
  • Mohammed Muqtader Ahmed

摘要

Objective

The objective of this study was to develop and evaluate PEG-2000 coated solid lipid nanoparticles (PEG-Ber-SLN) for encapsulating berberine, aiming to extend its biological half-life and systemic circulation for enhanced breast cancer therapy.

Methods

PEG-Ber-SLN was formulated and characterized for particle size, zeta potential, entrapment efficiency, morphology, drug release profile, and drug-excipient interaction. Cellular uptake and internalization studies were conducted in AMJ-13 and BT-20 breast cancer cell lines, while cytotoxicity was assessed using the MCF-7 cell line. Pharmacokinetic and biodistribution studies were carried out in rats.

Results

The PEG-Ber-SLN exhibited a nanometric particle size of 206 ± 8.3 nm, a zeta potential of − 24.3 ± 8.5 mV, and an entrapment efficiency of 74 ± 3%. In-vitro release showed 75% drug release over 72 h following Higuchi kinetics. Cellular internalization was significantly enhanced. Compared to berberine solution, PEG-Ber-SLN demonstrated increased half-life (t₁/₂), mean residence time (MRT), and reduced clearance. Biodistribution studies showed higher accumulation in breast tissue, indicating effective passive targeting.

Conclusions

PEG-Ber-SLN represents a promising nanocarrier system to improve berberine’s pharmacokinetic profile and targeting efficacy for breast cancer treatment by enhancing circulation time and site-specific accumulation.

Graphical Abstract