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<p>By enhancing the water solubility of hydrophobic drugs and the stability of easily degradable compounds, nanocarriers such as micellar nanoparticles demonstrate significant potential for optimizing drug formulations, improving efficacy, and reducing side effects associated with conventional therapies, which has attracted considerable attention in the drug delivery field. The advantages of nanoparticles include promoting drug retention in tissues, protecting against enzymatic degradation, enhancing cellular uptake, and enabling highly targeted delivery. Many clinically used drugs exhibit poor water solubility, substantially limiting their absorption and bioavailability. Core–shell micellar nanoparticles formed by the self-assembly of amphiphilic polymers offer distinct advantages for improving drug solubility and stability. Their hydrophobic core (hydrophobic grafted branches) can solubilize hydrophobic drugs, whereas hydrophilic shell (hydrophilic polysaccharide main chain) endows the nanoparticles with “stealth” characteristics (avoiding phagocytosis by mononuclear macrophages), which is beneficial for reducing the non-specific interaction with endogenous substances (such as proteins and enzymes), thereby minimizing immune recognition and prolonging systemic circulation time. Polysaccharides, as natural polymers, are widely studied for drug carrier applications due to their abundance, low cost, non-toxicity, good biocompatibility, degradability, non-immunogenicity and easy cross-linking. However, research on amphiphilic polysaccharide derivatives prepared via chemical modification and their self-assembled nanoparticles remains limited. Therefore, this review details the synthesis of amphiphilic polysaccharide derivatives and methods for fabricating drug-loaded nanoparticles based on amphiphilic polymer self-assembly. We further reveal the characteristics and characterization techniques of these self-assembled nanoparticles as hydrophobic drug delivery systems and outline future research directions. The objective of present study is to provide a theoretical basis for developing polysaccharide-based carriers tailored to therapeutic needs and drug properties, offering valuable insights for advancing natural polysaccharides in drug delivery research.</p>

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Fabrication and characteristics of amphiphilic polysaccharide derivative self-assembled nanoparticles for hydrophobic drug delivery: a review

  • 期刊论文

  • 发表日期：

    2025年9月11日

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  • Jiji Fan,
  • Ting Wu,
  • Yanan Bu,
  • Xiuqiong Chen,
  • Tao Ma,
  • Huiqiong Yan,
  • Qiang Lin

摘要

By enhancing the water solubility of hydrophobic drugs and the stability of easily degradable compounds, nanocarriers such as micellar nanoparticles demonstrate significant potential for optimizing drug formulations, improving efficacy, and reducing side effects associated with conventional therapies, which has attracted considerable attention in the drug delivery field. The advantages of nanoparticles include promoting drug retention in tissues, protecting against enzymatic degradation, enhancing cellular uptake, and enabling highly targeted delivery. Many clinically used drugs exhibit poor water solubility, substantially limiting their absorption and bioavailability. Core–shell micellar nanoparticles formed by the self-assembly of amphiphilic polymers offer distinct advantages for improving drug solubility and stability. Their hydrophobic core (hydrophobic grafted branches) can solubilize hydrophobic drugs, whereas hydrophilic shell (hydrophilic polysaccharide main chain) endows the nanoparticles with “stealth” characteristics (avoiding phagocytosis by mononuclear macrophages), which is beneficial for reducing the non-specific interaction with endogenous substances (such as proteins and enzymes), thereby minimizing immune recognition and prolonging systemic circulation time. Polysaccharides, as natural polymers, are widely studied for drug carrier applications due to their abundance, low cost, non-toxicity, good biocompatibility, degradability, non-immunogenicity and easy cross-linking. However, research on amphiphilic polysaccharide derivatives prepared via chemical modification and their self-assembled nanoparticles remains limited. Therefore, this review details the synthesis of amphiphilic polysaccharide derivatives and methods for fabricating drug-loaded nanoparticles based on amphiphilic polymer self-assembly. We further reveal the characteristics and characterization techniques of these self-assembled nanoparticles as hydrophobic drug delivery systems and outline future research directions. The objective of present study is to provide a theoretical basis for developing polysaccharide-based carriers tailored to therapeutic needs and drug properties, offering valuable insights for advancing natural polysaccharides in drug delivery research.