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<p>A nano-sized drug carrier possesses several advantages, including adjustable drug encapsulation and release properties, reduced drug toxicity and improved drug stability. Carboxymethyl chitosan (CMCh) inherits the advantages of chitosan and water solubility of carboxymethyl groups. Amphiphilic CMCh can form nano-sized self-aggregates, which have important potential applications in oil-soluble drug delivery. In this study, two types of amphiphilic CMCh, <i>N</i>-stearic-<i>O</i>-carboxymethyl chitosan (SA-CMCh) and <i>N</i>-lauric-<i>O</i>-carboxymethyl chitosan (LA-CMCh), were synthesized, which exhibited pH-responsive properties. The optimum reaction conditions were determined by assessing the maximum degree of substitution (DS), and the molecular structures were confirmed through Fouriertransform infrared spectroscopy (FTIR), proton nuclear magnetic resonance (<sup>1</sup>H NMR), and X-ray diffraction (XRD). The physicochemical properties of SA-CMCh and LA-CMCh, including thermal stability, aggregation behavior, antibacterial activity against <i>S. aureus</i>and <i>E. coli</i>, and in vitrocytotoxicity, were comprehensively evaluated and compared. SA-CMCh and LA-CMCh self-assembled into nanoparticles with diameters ranging from 285 to 723&#xa0;nm, depending on DS and alkyl chain length. The critical aggregation concentrations were inversely proportional to the DS. These nano-sized self-aggregates were utilized to encapsulate curcumin, allowing for an assessment of their potential as drug carriers. Notably, SA-CMCh aggregates exhibited an initially rapid release of curcumin, followed by a sustained release over 800&#xa0;m under intestinal pH conditions (6.86) and physiological temperature (37 ºC), with a maximum release rate of 41.73%. These results highlight SA-CMCh<sub>6.8%</sub> as a superior carrier for oral oil-soluble drugs due to its pH-responsive release profile.</p> Graphical abstract <p></p>

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Synthesis, characterization, and applications of amphiphilic chitosan derivatives for oral drug delivery: focus on curcumin encapsulation and pH-responsive release

  • 期刊论文

  • 发表日期：

    2025年9月6日

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  • Xianghui Liu,
  • Qirui Zhou,
  • Yan Li,
  • Xiaodeng Yang,
  • Guohong Li,
  • Mojtaba Koosha,
  • Ling Wang,
  • Zhongfu Dong,
  • Jing Dong

摘要

A nano-sized drug carrier possesses several advantages, including adjustable drug encapsulation and release properties, reduced drug toxicity and improved drug stability. Carboxymethyl chitosan (CMCh) inherits the advantages of chitosan and water solubility of carboxymethyl groups. Amphiphilic CMCh can form nano-sized self-aggregates, which have important potential applications in oil-soluble drug delivery. In this study, two types of amphiphilic CMCh, N-stearic-O-carboxymethyl chitosan (SA-CMCh) and N-lauric-O-carboxymethyl chitosan (LA-CMCh), were synthesized, which exhibited pH-responsive properties. The optimum reaction conditions were determined by assessing the maximum degree of substitution (DS), and the molecular structures were confirmed through Fouriertransform infrared spectroscopy (FTIR), proton nuclear magnetic resonance (1H NMR), and X-ray diffraction (XRD). The physicochemical properties of SA-CMCh and LA-CMCh, including thermal stability, aggregation behavior, antibacterial activity against S. aureusand E. coli, and in vitrocytotoxicity, were comprehensively evaluated and compared. SA-CMCh and LA-CMCh self-assembled into nanoparticles with diameters ranging from 285 to 723 nm, depending on DS and alkyl chain length. The critical aggregation concentrations were inversely proportional to the DS. These nano-sized self-aggregates were utilized to encapsulate curcumin, allowing for an assessment of their potential as drug carriers. Notably, SA-CMCh aggregates exhibited an initially rapid release of curcumin, followed by a sustained release over 800 m under intestinal pH conditions (6.86) and physiological temperature (37 ºC), with a maximum release rate of 41.73%. These results highlight SA-CMCh6.8% as a superior carrier for oral oil-soluble drugs due to its pH-responsive release profile.

Graphical abstract