title: Recent advances in chitosan-based nanoparticles for oral delivery of macromolecules.
abstract: 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.
authors.affiliation: Department of Chemical Engineering, National Cheng Kung University, Tainan, Taiwan ROC.
authors.forename: Mei-Chin
authors.initials: MC
authors.lastname: Chen
authors.forename: Fwu-Long
authors.initials: FL
authors.lastname: Mi
authors.forename: Zi-Xian
authors.initials: ZX
authors.lastname: Liao
authors.forename: Chun-Wen
authors.initials: CW
authors.lastname: Hsiao
authors.forename: Kiran
authors.initials: K
authors.lastname: Sonaje
authors.forename: Min-Fan
authors.initials: MF
authors.lastname: Chung
authors.forename: Li-Wen
authors.initials: LW
authors.lastname: Hsu
authors.forename: Hsing-Wen
authors.initials: HW
authors.lastname: Sung
mesh_terms: D000277:Adjuvants, Pharmaceutic / Q000737:chemistry / Q000493:pharmacokinetics; D000284:Administration, Oral; D001682:Biological Availability; D001692:Biological Transport / Q000502:physiology; D002626:Chemistry, Pharmaceutical; D048271:Chitosan / Q000737:chemistry*; D004337:Drug Carriers / Q000008:administration & dosage / Q000493:pharmacokinetics; D041981:Gastrointestinal Tract / Q000378:metabolism; D006801:Humans; D007408:Intestinal Absorption / Q000502:physiology; D046911:Macromolecular Substances / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D053758:Nanoparticles / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry / Q000493:pharmacokinetics; D011506:Proteins / Q000008:administration & dosage / Q000493:pharmacokinetics; D011956:Receptors, Cell Surface / Q000378:metabolism
chemical_list: D000277:Adjuvants, Pharmaceutic; D004337:Drug Carriers; D046911:Macromolecular Substances; D011108:Polymers; D011506:Proteins; D011956:Receptors, Cell Surface; D048271:Chitosan