Release Time:2019-03-12  Hits:

Indexed by: Journal Article

Date of Publication: 2017-09-22

Journal: JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION

Included Journals: Scopus、PubMed、EI、SCIE

Volume: 28

Issue: 14

Page Number: 1525-1537

ISSN: 0920-5063

Key Words: Word; hydroxyethyl starch; N-acetyl-cysteine; pH-responsive; oral delivery; drug release

Abstract: In this study, a novel type of pH-responsive polymer PyHES-NAC (2-hydroxy-3-(2-propynyloxy) propyl hydroxyethyl starch (PyHES)) - (N-acetyl-cysteine (NAC)) was synthesized. First, PyHES was prepared via hydrophobic modification of hydroxyl groups in hydroxyethyl starch (HES) with propynylglycidyl ether (PGE), and then pH-responsive carboxylic acid group was connected to propynyl group via thiol-yne click reaction with NAC. Aqueous PyHES-NAC solutions exhibited a good transference between hydrophobic (or self-assembly) and hydrophilic static along with the change of pH value and protective properties of drugs under acidic conditions. 10.0% DOX was released under artificial gastric fluid after 2h, whereas an immediate release (above 80%) was observed under artificial intestinal fluid. Drug loading capacity of PyHES-NAC was increased by the increase of degree of substitution (DS) of hydrophobic propynyl groups in PyHES, and 41 wt% DOX Loading capacity was the highest value in our study area.