title: Hyaluronic acid L-cysteine conjugate exhibits controlled-release potential for mucoadhesive drug delivery.
abstract: Hyaluronic acid-L-cysteine conjugate, a novel thiolated polymer, was synthesized and characterized for mucoadhensive drug delivery. L-Cysteine was covalently attached to hyaluronic acid via the formation of an amide bond. Adhesion studies on the mucosa indicated a 4.82-fold increase in the adhesion force of the obtained conjugate (containing 210.58 micromol thiol groups per gram polymer) versus unmodified hyaluronic acid. The results of a peptidase inhibition study revealed that the inhibitory effect of hyaluronic acid toward trypsin and chymotrypsin was significantly improved compared to hyaluronic acid. Permeation studies utilizing a MDCK cell monolayer system demonstrated a sustained drug release. Based on these features the novel thiolated polymer might represent a promising multifunctional excipient for various drug delivery systems.
authors.affiliation: Key Laboratory of Drug Targeting and Drug Delivery Systems, Ministry of Education, West China School of Pharmacy, Sichuan University, PR China.
authors.forename: Xiaosi
authors.initials: X
authors.lastname: Li
authors.forename: Gonglong
authors.initials: G
authors.lastname: Yu
authors.forename: Ke
authors.initials: K
authors.lastname: Jin
authors.forename: Zongning
authors.initials: Z
authors.lastname: Yin
mesh_terms: D000818:Animals; D002460:Cell Line; D002463:Cell Membrane Permeability / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002918:Chymotrypsin / Q000037:antagonists & inhibitors; D004396:Coloring Agents; D003545:Cysteine / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D003692:Delayed-Action Preparations; D004285:Dogs; D016503:Drug Delivery Systems; D005079:Excipients; D006820:Hyaluronic Acid / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D007422:Intestines / Q000201:enzymology; D009092:Mucous Membrane; D011480:Protease Inhibitors / Q000494:pharmacology; D013438:Sulfhydryl Compounds / Q000737:chemistry; D013778:Tetrazolium Salts; D013844:Thiazoles; D014014:Tissue Adhesives; D014361:Trypsin Inhibitors / Q000494:pharmacology
chemical_list: D004396:Coloring Agents; D003692:Delayed-Action Preparations; D005079:Excipients; D011480:Protease Inhibitors; D013438:Sulfhydryl Compounds; D013778:Tetrazolium Salts; D013844:Thiazoles; D014014:Tissue Adhesives; D014361:Trypsin Inhibitors; D006820:Hyaluronic Acid; D002918:Chymotrypsin; C022616:thiazolyl blue; D003545:Cysteine