期刊
ADVANCED DRUG DELIVERY REVIEWS
卷 65, 期 6, 页码 865-879出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.addr.2012.10.010
关键词
Oral drug delivery; Transcellular pathway; Paracellular pathway; Bioavailability; Mucoadhesion; Tight junction
资金
- National Science Council of the Republic of China, Taiwan [NSC 100-2120-M-007-003]
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. (C) 2012 Elsevier B.V. All rights reserved.
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