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<p>The clinical use of amphotericin B (AmB), a potent antifungal agent, is limited by its poor solubility, aggregation in biological fluids, and severe toxicity. In this study, we developed trimethyl chitosan-based AmB nanoparticles (TMC/AmB NPs) using a mild ionotropic gelation method with tripolyphosphate (TPP) as a cross-linker to overcome these limitations. By optimizing the polymer:drug:cross-linker ratio, we achieved a stable nanoformulation with an average particle size of 202.1&#xa0;nm, high positive surface charge (+ 50.9&#xa0;mV), and an encapsulation efficiency of 79.73%, ensuring colloidal stability and effective drug loading. Spectroscopic analysis (FTIR and UV–Vis) confirmed strong interactions between AmB and TMC, with suppression of the aggregation band (341&#xa0;nm) and stabilization of AmB in its monomeric form, reducing toxicity. TEM images showed uniformly spherical nanoparticles. Wettability studies indicated improved aqueous compatibility (contact angle = 42.56°), while mucoadhesion assays demonstrated 78.44% mucin binding, suggesting prolonged residence at mucosal sites. The nanoparticles also displayed strong electrostatic interaction potential, essential for site-specific delivery in biological environments. Importantly, in vitro drug release studies revealed a sustained release profile over 72&#xa0;h under mildly acidic conditions (pH 5.5), mimicking infected tissue environments, with a controlled release pattern that could minimize side effects and enhance therapeutic efficacy. This work highlights TMC/AmB NPs as a safe, stable, and mucoadhesive delivery system that improves the solubility, bioavailability, and controlled release of AmB, offering a promising strategy for effective antifungal therapy and wound care applications.</p>

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Trimethyl Chitosan-Based Amphotericin B Nanoparticles: Improved Gastrointestinal Stability, Hemocompatibility, Monomeric Stabilization, and Controlled Drug Release

  • 期刊论文

  • 发表日期：

    2025年9月4日

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  • Divya Mathew,
  • Benny Thomas,
  • Sudheep NM,
  • Julit George,
  • Radhakrishnan EK

摘要

The clinical use of amphotericin B (AmB), a potent antifungal agent, is limited by its poor solubility, aggregation in biological fluids, and severe toxicity. In this study, we developed trimethyl chitosan-based AmB nanoparticles (TMC/AmB NPs) using a mild ionotropic gelation method with tripolyphosphate (TPP) as a cross-linker to overcome these limitations. By optimizing the polymer:drug:cross-linker ratio, we achieved a stable nanoformulation with an average particle size of 202.1 nm, high positive surface charge (+ 50.9 mV), and an encapsulation efficiency of 79.73%, ensuring colloidal stability and effective drug loading. Spectroscopic analysis (FTIR and UV–Vis) confirmed strong interactions between AmB and TMC, with suppression of the aggregation band (341 nm) and stabilization of AmB in its monomeric form, reducing toxicity. TEM images showed uniformly spherical nanoparticles. Wettability studies indicated improved aqueous compatibility (contact angle = 42.56°), while mucoadhesion assays demonstrated 78.44% mucin binding, suggesting prolonged residence at mucosal sites. The nanoparticles also displayed strong electrostatic interaction potential, essential for site-specific delivery in biological environments. Importantly, in vitro drug release studies revealed a sustained release profile over 72 h under mildly acidic conditions (pH 5.5), mimicking infected tissue environments, with a controlled release pattern that could minimize side effects and enhance therapeutic efficacy. This work highlights TMC/AmB NPs as a safe, stable, and mucoadhesive delivery system that improves the solubility, bioavailability, and controlled release of AmB, offering a promising strategy for effective antifungal therapy and wound care applications.