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<p>This study aims to overcome the adverse effects of conventional cytotoxic chemotherapy on healthy organs by developing a target-specific approach utilizing Doxorubicin (DOX)-encapsulated liposome conjugated with aptamer which has high binding affinity to the overexpressed Mucin-1 (MUC1) protein in various cancer types. To ensure optimal aptamer selection, we conducted a comprehensive in silico comparison of several MUC1-targeting aptamers, including 5TR1, MA3, S1.6, S2.2, and STRG2. As a results, the S1.6 aptamer was selected as a targeting ligand by comparing the thermodynamic stability, docking score, confidence score, and binding affinity. Also, spectrophotometer, gel electrophoresis, and Dynamic light scattering (DLS) confirm the size, zeta potential, DOX encapsulation rate, stability, and aptamer conjugation of liposomes. In addition, flow cytometry results validate MUC1 expression in MCF7 cells while not in MDA-MB-231 cells, while confocal microscopy confirmed the specific cellular uptake of the lipo-aptamer complex. Consequently, this aptamer-mediated liposomal drug delivery approach shows potential for enhancing the specificity and reducing the side effects of conventional chemotherapy, while the use of in silico methods provides an efficient and cost-effective strategy for screening and optimizing aptamer candidates, simplifying the overall development process. Further in vivo evaluation for therapeutic efficacy and clinical applications is warranted.</p> Graphical Abstract <p></p>

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Aptamer-conjugated liposome system for targeting MUC1-positive cancer: an in silico screening approach

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年1月28日

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  • Md Shakil Ahmed Khan,
  • Jiwoo Park,
  • Somin Lee,
  • Jee-Eun Hwang,
  • Chiwoo Oh,
  • MinKyu Kim,
  • Jeong-Seob Lee,
  • Jongyeong Jeon,
  • Beomjin Park,
  • Shengjun Li,
  • Han Na Jung,
  • Hyung-Jun Im

摘要

This study aims to overcome the adverse effects of conventional cytotoxic chemotherapy on healthy organs by developing a target-specific approach utilizing Doxorubicin (DOX)-encapsulated liposome conjugated with aptamer which has high binding affinity to the overexpressed Mucin-1 (MUC1) protein in various cancer types. To ensure optimal aptamer selection, we conducted a comprehensive in silico comparison of several MUC1-targeting aptamers, including 5TR1, MA3, S1.6, S2.2, and STRG2. As a results, the S1.6 aptamer was selected as a targeting ligand by comparing the thermodynamic stability, docking score, confidence score, and binding affinity. Also, spectrophotometer, gel electrophoresis, and Dynamic light scattering (DLS) confirm the size, zeta potential, DOX encapsulation rate, stability, and aptamer conjugation of liposomes. In addition, flow cytometry results validate MUC1 expression in MCF7 cells while not in MDA-MB-231 cells, while confocal microscopy confirmed the specific cellular uptake of the lipo-aptamer complex. Consequently, this aptamer-mediated liposomal drug delivery approach shows potential for enhancing the specificity and reducing the side effects of conventional chemotherapy, while the use of in silico methods provides an efficient and cost-effective strategy for screening and optimizing aptamer candidates, simplifying the overall development process. Further in vivo evaluation for therapeutic efficacy and clinical applications is warranted.

Graphical Abstract