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Novel Therapeutic Platform of Micelles and Nanogels from Dopa‐Functionalized Triblock Copolymers
Author(s) -
Zhang Yuning,
Olofsson Kristina,
Fan Yanmiao,
Sánchez Carmen C.,
Andrén Oliver C. J.,
Qin Liguo,
Fortuin Lisa,
Jonsson Eva Malmström,
Malkoch Michael
Publication year - 2021
Publication title -
small
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 3.785
H-Index - 236
eISSN - 1613-6829
pISSN - 1613-6810
DOI - 10.1002/smll.202007305
Subject(s) - micelle , copolymer , amphiphile , drug delivery , nanomedicine , nanoparticle , materials science , combinatorial chemistry , biophysics , chemistry , nanotechnology , aqueous solution , polymer , organic chemistry , biology
Multi‐drug delivery systems constructed from a basic polymeric scaffold, and which have the ability to target a variety of biomedical applications, can streamline the development of nanomedicine to provide both environmental and economical relief. Herein, amphiphilic ABA‐triblock copolymers are synthesized and assembled sequentially into micelles and nanogels as drug delivery systems following a thorough evaluation on advanced in vitro models to explore their potential for the treatment of cancer and bacterial infections. Short blocks of 5‐methyl‐5‐allyloxycarbonyl‐1,3‐dioxan‐2‐one (MAC) are oligomerized from PEG6k and thereafter functionalized with dihydroxyphenylalanine (dopa)‐functional thiols using thiol‐ene coupling (TEC) click chemistry. The copolymers self‐assemble into well‐defined micelles in aqueous solution and are further formulated into nanogels via UV‐induced TEC. The resulting spherical micelles and nanogels are stable nanoparticles, with sizes ranging between 100 and 200 nm. The nanogels are found to be non‐toxic to a panel of cell lines and mask the toxicity of the potent drugs until their release. The nanogels would be superior to micelles for the elimination of cancer cells supported by both 2D cell culture and a 3D spheroid model. The opposite conclusion could be drawn for bacteria inhibition.