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<p>Many hydrophobic anticancer drugs are severely limited in their clinical utility due to their extremely low aqueous solubility. Herein, we propose a facile supramolecular solubilization strategy by introducing a small aromatic molecule bearing hydrophilic groups to enhance drug solubility, achieving stabilization through π-π stacking and complementary non-covalent interactions. Dopamine (DA), a catecholamine neurotransmitter with hydrophilic functional groups, was selected as a model scaffold to assemble with hydrophobic drugs. Experimental results demonstrated that the aqueous solubility of 7-ethyl-10-hydroxycamptothecin (SN38) was enhanced by 33.5-fold upon complexation with DA. Furthermore, compared with the free drug, the DA-SN38 complex not only retained the intrinsic pharmacological efficacy of SN38 but also further enhanced its cytotoxicity against cancer cells. This work highlights a generalizable approach for improving the formulation of poorly soluble aromatic drugs through supramolecular assembly with biocompatible small molecules, providing a promising new paradigm for pharmaceutical research and development.</p>

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Enhancing aqueous solubility of hydrophobic drugs via dopamine-mediated π-π interaction

  • 期刊论文

  • 发表日期：

    2026年1月20日

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  • Xiaodong Wen,
  • He Zhou,
  • Liping Wang,
  • Feng Zhang,
  • Xinmin Zhao,
  • Ruisong Xu,
  • Feng Gao,
  • Wenjian Guo

摘要

Many hydrophobic anticancer drugs are severely limited in their clinical utility due to their extremely low aqueous solubility. Herein, we propose a facile supramolecular solubilization strategy by introducing a small aromatic molecule bearing hydrophilic groups to enhance drug solubility, achieving stabilization through π-π stacking and complementary non-covalent interactions. Dopamine (DA), a catecholamine neurotransmitter with hydrophilic functional groups, was selected as a model scaffold to assemble with hydrophobic drugs. Experimental results demonstrated that the aqueous solubility of 7-ethyl-10-hydroxycamptothecin (SN38) was enhanced by 33.5-fold upon complexation with DA. Furthermore, compared with the free drug, the DA-SN38 complex not only retained the intrinsic pharmacological efficacy of SN38 but also further enhanced its cytotoxicity against cancer cells. This work highlights a generalizable approach for improving the formulation of poorly soluble aromatic drugs through supramolecular assembly with biocompatible small molecules, providing a promising new paradigm for pharmaceutical research and development.