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Synthesis of Polylactide‐Based Core–Shell Interface Cross‐Linked Micelles for Anticancer Drug Delivery
Author(s) -
Chen ChihKuang,
Lin WeiJen,
Hsia Yu,
Lo LeuWei
Publication year - 2017
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.201600191
Subject(s) - micelle , nile red , amphiphile , ethylene glycol , chemistry , doxorubicin , drug delivery , biophysics , polymerization , cytotoxicity , peg ratio , polyester , organic chemistry , polymer , biochemistry , copolymer , in vitro , finance , chemotherapy , quantum mechanics , aqueous solution , economics , fluorescence , biology , medicine , physics , surgery
Well‐defined poly(ethylene glycol)‐ b ‐allyl functional polylactide‐ b ‐polylactides (PEG‐APLA‐PLAs) are synthesized through sequential ring‐opening polymerization. PEG‐APLA‐PLAs that have amphiphilic properties and reactive allyl side chains on their intermediate blocks are successfully transferred to core–shell interface cross‐linked micelles (ICMs) by micellization and UV‐initiated irradiation. ICMs have demonstrated enhanced colloidal stability in physiological‐mimicking media. Hydrophobic molecules such as Nile Red or doxorubicin (Dox) are readily loaded into ICMs; the resulting drug‐ICM formulations possess slow and sustained drug release profiles under physiological‐mimicking conditions. ICMs exhibit negligible cytotoxicity in human uterine sarcoma cancer cells by using biodegradable aliphatic polyester as the hydrophobic segments. Relative to free Dox, Dox‐loaded ICMs show a reduced cytotoxicity due to the late intracellular release of Dox from ICMs. Overall, ICMs represent a new type of biodegradable cross‐linked micelle and can be employed as a promising platform for delivering a broad variety of hydrophobic drugs.