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<p>Conventional anticancer therapies are often limited due to poor pharmacokinetics, systemic toxicity, and low bioavailability. Nanostructured lipid carriers (NLCs) have emerged as promising platforms to enhance drug delivery efficiency and therapeutic outcomes. This study aimed to further evaluate the abiraterone acetate (AA)-loaded NLCs (AANLCs) for in vivo anticancer efficacy. AANLCs were prepared using cholesterol solid lipid, almond oil liquid lipid, surfactant tween 80, solvent mix of acetone and ethanol by solvent diffusion-evaporation method. The fabricated AANLCs was tested for in vivo anticancer against MCF7 tumor-bearing rabbit model and further assessed for mean survival time, percentage increase in life span, tumor volume and weight, cell viability (%), biochemical and hematological parameters, tissue distribution study, and pharmacokinetic in comparison with pure AA in tumor induced New Zealand White rabbits. In vivo assessments demonstrated that AANLCs significantly reduced tumor volume (3.30 ± 0.23 cm<sup>3</sup>) and weight (5.37 ± 0.41&#xa0;g), enhanced cytotoxicity (92.36%), and improved survival outcomes (49.66 days), compared to the free drug administered as suspension (0.25%w/v Na-CMC) (42 days). Pharmacokinetic studies revealed prolonged half-life, delayed T<sub>max</sub>, increased AUC, and improved mean residence time, indicating sustained drug release and enhanced bioavailability. Moreover, the bio-distribution studies showed enhanced accumulation in vital organs such as liver (45.47 ± 0.23&#xa0;µg/mL<b>)</b>, kidney (49.88 ± 0.95&#xa0;µg/mL<b>)</b>, and breast tissues (44.26 ± 0.44&#xa0;µg/mL), with increase in AUC (44.26 ± 0.44&#xa0;µg/mL) and relative targeting efficiency in the breast tissue (3.10 ± 0.63 rE). These findings suggest that fabricated AANLCs offer a superior, targeted delivery system for AA, with potential for improved safety and efficacy in hormone-sensitive breast cancer therapy.</p> Graphical Abstract <p></p>

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Pharmacokinetic Profiling and in Vivo Anticancer Evaluation of Abiraterone Acetate Loaded Nanostructured Lipid Carriers

  • 期刊论文

  • 发表日期：

    2026年2月24日

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  • Shivappa N. Nagoba,
  • Avinash B. Swami,
  • Anant N. Deshpande,
  • Anbhule Sachin Jalindar,
  • Sachin S. Mali,
  • Sudarshan Singh

摘要

Conventional anticancer therapies are often limited due to poor pharmacokinetics, systemic toxicity, and low bioavailability. Nanostructured lipid carriers (NLCs) have emerged as promising platforms to enhance drug delivery efficiency and therapeutic outcomes. This study aimed to further evaluate the abiraterone acetate (AA)-loaded NLCs (AANLCs) for in vivo anticancer efficacy. AANLCs were prepared using cholesterol solid lipid, almond oil liquid lipid, surfactant tween 80, solvent mix of acetone and ethanol by solvent diffusion-evaporation method. The fabricated AANLCs was tested for in vivo anticancer against MCF7 tumor-bearing rabbit model and further assessed for mean survival time, percentage increase in life span, tumor volume and weight, cell viability (%), biochemical and hematological parameters, tissue distribution study, and pharmacokinetic in comparison with pure AA in tumor induced New Zealand White rabbits. In vivo assessments demonstrated that AANLCs significantly reduced tumor volume (3.30 ± 0.23 cm3) and weight (5.37 ± 0.41 g), enhanced cytotoxicity (92.36%), and improved survival outcomes (49.66 days), compared to the free drug administered as suspension (0.25%w/v Na-CMC) (42 days). Pharmacokinetic studies revealed prolonged half-life, delayed Tmax, increased AUC, and improved mean residence time, indicating sustained drug release and enhanced bioavailability. Moreover, the bio-distribution studies showed enhanced accumulation in vital organs such as liver (45.47 ± 0.23 µg/mL), kidney (49.88 ± 0.95 µg/mL), and breast tissues (44.26 ± 0.44 µg/mL), with increase in AUC (44.26 ± 0.44 µg/mL) and relative targeting efficiency in the breast tissue (3.10 ± 0.63 rE). These findings suggest that fabricated AANLCs offer a superior, targeted delivery system for AA, with potential for improved safety and efficacy in hormone-sensitive breast cancer therapy.

Graphical Abstract