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<p>Abiraterone (ABR) is an antiandrogen medication used for the treatment of prostate cancer. Abiraterone acetate (ABA) was found to be esterase resistant. In vivo rapid deacetylation of ABR results in dynamic suppression of CYP450 C17. The limited bioavailability of ABA due to the poor solubility and permeability poses hurdles towards the dose and dosage regimen required for the treatment of prostate cancer. The present work deals with the preparation of ABA-loaded nano-structured lipid carrier (NLC) by high shear homogenization method and the physiochemical evaluation, i.e., particle size, polydispersity index (PDI), and zeta potential (ZP) by dynamic light scattering (DLS) method, in vitro and in vivo characterization study aiming to prepare a more cytotoxic sustained release nanoparticle. The optimal particle size, PDI, and ZP obtained using DLS were 37.92&#xa0;nm, 0.209–0.499, and -18.3&#xa0;mV, respectively. The in vitro drug release study demonstrated improved traversion of NLC through the dialysis membrane with potential sustained release for 12&#xa0;h. The studies in the oral route demonstrated significant improvement in oral bioavailability. The in vitro cytotoxicity study in DU145 prostate carcinoma cell lines expressed higher cytotoxicity for NLC formulation, which was concentration dependent, with <i>p</i>-value &lt; 0.001 at all concentrations starting from 0.002 to 0.1&#xa0;μg. Hence, the lyophilized NLC of ABA has potential for the treatment of prostate cancer.&#xa0;</p>

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Enhancing Bioavailability of Abiraterone Acetate by Nanostructured Lipid Carriers: In Vivo, In Vitro Characterization and Cytotoxicity Assessment

  • 期刊论文

  • 发表日期：

    2025年9月17日

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  • Ch. Niranjan Patra,
  • Mounik Rout

摘要

Abiraterone (ABR) is an antiandrogen medication used for the treatment of prostate cancer. Abiraterone acetate (ABA) was found to be esterase resistant. In vivo rapid deacetylation of ABR results in dynamic suppression of CYP450 C17. The limited bioavailability of ABA due to the poor solubility and permeability poses hurdles towards the dose and dosage regimen required for the treatment of prostate cancer. The present work deals with the preparation of ABA-loaded nano-structured lipid carrier (NLC) by high shear homogenization method and the physiochemical evaluation, i.e., particle size, polydispersity index (PDI), and zeta potential (ZP) by dynamic light scattering (DLS) method, in vitro and in vivo characterization study aiming to prepare a more cytotoxic sustained release nanoparticle. The optimal particle size, PDI, and ZP obtained using DLS were 37.92 nm, 0.209–0.499, and -18.3 mV, respectively. The in vitro drug release study demonstrated improved traversion of NLC through the dialysis membrane with potential sustained release for 12 h. The studies in the oral route demonstrated significant improvement in oral bioavailability. The in vitro cytotoxicity study in DU145 prostate carcinoma cell lines expressed higher cytotoxicity for NLC formulation, which was concentration dependent, with p-value < 0.001 at all concentrations starting from 0.002 to 0.1 μg. Hence, the lyophilized NLC of ABA has potential for the treatment of prostate cancer.