Synthesis and properties of non-cytotoxic poly(L-malic acid acetate-co-L-lysine ester)s with thermo-sensitivity as hydrophobic drug nanocarrier

摘要

In this investigation, a group of poly(L-malic acid acetate-co-L-lysine ester)s (PMALs) with excellent thermo-sensitivity and non-cytotoxicity were prepared by an optimized synthetic route from natural L-malic acid and L-lysine. The structure and properties of PMALs including monomers were systematically characterized by FTIR, H-1 NMR, UV, gel permeation chromatograph, scanning electron microscope, contact angle measurement, cell counting kit assess (CCK-8), and confocal laser scanning microscopy (CLSM). Three PMALs show a reversible lower critical solution temperature of 8-36 degrees C depending on their chemical structure. The contact angle measurement revealed a considerable discrepancy in the hydrophilicity/hydrophobicity of PMALs and further influence on their thermo-sensitivity. The viability of HeLa cells exposed to 0.2-100 mu g/mL PMALs solution was found to be in a range 80-103% after 24, 48, and 72 h of incubation, indicating no cytotoxicity. Moreover, a spherical nanocarrier with core-shell structure was facilely fabricated via the thermo-sensitivity of PMALs and hydrophobicity of drug. CLSM observations manifested that the hydrophobic-curcumin-enwrapped nanocarriers can clearly internalize into the cellular inside. The sustained release of curcumin from nanocarriers in vitro provided a possibility of depressing fast hydrolytic degradation at physiological pH or other side-effects. (C) 2017 Wiley Periodicals, Inc.