Journal
COLLOIDS AND SURFACES B-BIOINTERFACES
Volume 153, Issue -, Pages 220-228Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.colsurfb.2017.02.022
Keywords
High loading capacity; Electrostatic interaction; Hydrophobic interaction; Mercaptan acid; Thiol-ene reaction; Micelle
Funding
- Natural Science Foundation of Hubei Province of China [2014CFB696]
- Opening Project of Key Laboratory of Biomedical Polymers of Ministry of Education at Wuhan University [20150102]
- National Natural Science Foundation of China [21074098]
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In this paper, four different kinds of mercaptan acids modified amphiphilic copolymers mPEG-b-PATMC-g-SRCOOH (R=CH2-, -CH2CH2-, -(CH2)(10)- and -CH(COOH)CH2-) were successfully synthesized by thiol-ene click reaction between pendent carbon-carbon double bonds of PEG-b-PATMC and thiol groups of thioglycolic acid, 3-mercaptopropionic acid, 11-mercaptoundecanoic acid or 2-mercaptosuccinic acid. DLS and TEM measurements showed that all the mPEG-b-PATMC-g-SRCOOH copolymers could self-assemble to form micelles which dispersed in spherical shape with nano-size before and after DOX loading. The positively-charged DOX could effectively load into copolymer micelles via synergistic hydrophobic and electrostatic interactions. All DOX-loaded mPEG-b-PATMC-g-SRCOOH micelles displayed sustained drug release behavior without an initial burst which could be further adjusted by the conditions of ionic strength and pH. Especially in the case of mPEG-b-PATMC-g-S(CH2)(10)COOH (P3) micelles, the suitable hydrophobility and charge density were not only beneficial to improve the DOX-loading efficiency, they were also good for obtaining smaller particle size, higher micelle stability and more timely drug delivery. Confocal laser scanning microscopy (CLSM) and MTF assays further demonstrated efficient cellular uptake of DOX delivered by mPEG-b-PATMC-g-SRCOOH micelles and potent cytotoxic activity against cancer cells. (C) 2017 Elsevier B.V. All rights reserved.
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