Scholarlink

<p>Owing to faulty DNA damage repair system, triple negative breast cancer (TNBC) exhibits high susceptibility towards DNA damaging drugs such as platinum compounds e.g., oxaliplatin. Nevertheless, the clinical utility of oxaliplatin (OXA) has been constrained due to chemoresistance and chronic toxicities. Hence, to confer systemic inertness, tumor specific delivery, and multifaceted action, a octahedral OXA-CBL prodrug was synthesized using chlorambucil (CBL) as an axial ligand. The combination of OXA and CBL exhibited synergistic anti-cancer action in TNBC cell lines. Further, to potentiate the cellular internalization, targeting efficiency, and in-vivo performance, the synthesized prodrug was loaded into bovine serum albumin nanoparticles (OXA-CBL/BSA-NPs). The prepared nanoparticles had optimal particle size &lt; 200&#xa0;nm and high drug loading (∼ 5.863 ± 0.16%). As relative to free conjugate, the nanoparticles exhibited amplified cellular internalization and reduced the IC<sub>50</sub> in 4T1 (∼ 1.38-fold) and MDA-MB-231 (∼ 1.43-fold) cell line. The anti-cancer study in 4T1-based TNBC model in BALB/c mice demonstrated significantly higher tumor inhibition rate, and reduced tumor burden in OXA-CBL/BSA-NPs treated group. Toxicity assessment revealed no signs of hepato- and/or renal toxicity. Also, nanoparticles exhibited sufficient compatibility with erythrocytes. Overall, delivery of OXA-CBL via virtue of albumin nanoparticles presents safer and efficacious approach to combat TNBC.</p> Graphical Abstract <p></p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Dual acting oxaliplatin (IV) prodrug loaded albumin nanoparticles for safer synergistic anticancer action against triple negative breast cancer

  • 期刊论文

  • 发表日期：

    2025年3月11日

查看全文
  • Kshitija Abhang,
  • Sayali Dighe,
  • Oly Katari,
  • Vivek Yadav,
  • Sanyog Jain

摘要

Owing to faulty DNA damage repair system, triple negative breast cancer (TNBC) exhibits high susceptibility towards DNA damaging drugs such as platinum compounds e.g., oxaliplatin. Nevertheless, the clinical utility of oxaliplatin (OXA) has been constrained due to chemoresistance and chronic toxicities. Hence, to confer systemic inertness, tumor specific delivery, and multifaceted action, a octahedral OXA-CBL prodrug was synthesized using chlorambucil (CBL) as an axial ligand. The combination of OXA and CBL exhibited synergistic anti-cancer action in TNBC cell lines. Further, to potentiate the cellular internalization, targeting efficiency, and in-vivo performance, the synthesized prodrug was loaded into bovine serum albumin nanoparticles (OXA-CBL/BSA-NPs). The prepared nanoparticles had optimal particle size < 200 nm and high drug loading (∼ 5.863 ± 0.16%). As relative to free conjugate, the nanoparticles exhibited amplified cellular internalization and reduced the IC50 in 4T1 (∼ 1.38-fold) and MDA-MB-231 (∼ 1.43-fold) cell line. The anti-cancer study in 4T1-based TNBC model in BALB/c mice demonstrated significantly higher tumor inhibition rate, and reduced tumor burden in OXA-CBL/BSA-NPs treated group. Toxicity assessment revealed no signs of hepato- and/or renal toxicity. Also, nanoparticles exhibited sufficient compatibility with erythrocytes. Overall, delivery of OXA-CBL via virtue of albumin nanoparticles presents safer and efficacious approach to combat TNBC.

Graphical Abstract