Recent advances in chitosan-based nanoparticles for oral delivery of macromolecules

Mei Chin Chen, Fwu Long Mi, Zi Xian Liao, Chun Wen Hsiao, Kiran Sonaje, Min Fan Chung, Li Wen Hsu, Hsing Wen Sung

Research output: Contribution to journalReview articlepeer-review

387 Citations (Scopus)


Chitosan (CS), a cationic polysaccharide, is widely regarded as a safe and efficient intestinal absorption enhancer of therapeutic macromolecules, owing to its inherent mucoadhesive feature and ability to modulate the integrity of epithelial tight junctions reversibly. By using CS-based nanoparticles, many studies have attempted to protect the loaded macromolecules against acidic denaturation and enzymatic degradation, prolong their intestinal residence time, and increase their absorption by the intestinal epithelium. Derivatives of CS such as quaternized CS, thiolated CS and carboxylated CS have also been examined to further enhance its effectiveness in oral absorption of macromolecular drugs. This review article describes the synthesis of these CS derivatives and their characteristics, as well as their potential transport mechanisms of macromolecular therapeutics across the intestinal biological membrane. Recent advances in using CS and its derivatives as carriers for oral delivery of hydrophilic macromolecules and their effects on drug transport are also reviewed.

Original languageEnglish
Pages (from-to)865-879
Number of pages15
JournalAdvanced Drug Delivery Reviews
Issue number6
Publication statusPublished - Jun 15 2013


  • Bioavailability
  • Mucoadhesion
  • Oral drug delivery
  • Paracellular pathway
  • Tight junction
  • Transcellular pathway

ASJC Scopus subject areas

  • Pharmaceutical Science


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