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Preparation of Mixed Micelles Carrying Folates and Stable Radicals Through PLA Stereocomplexation for Drug Delivery

Yingchun Liu, Chenfang Xu, Xiaoshan Fan, Xian Jun Loh, Yun-Long Wu, Zibiao Li

Mater Sci Eng C Mater Biol Appl. 2020 Mar;108:110464.

PMID: 31923976

Abstract:

Multifunctional mixed micelles possessing targeting folates on the periphery and stable radicals in the core were prepared from the mixture of folate-poly(ethylene glycol)-block-poly(d-lactide) (FA-PEG-b-PDLA) and poly(ethylene glycol) methyl ether-block-poly(l-lactide)- 2,2,6,6-tetramethylpiperidine-1-oxyl (mPEG-b-PLLA-TEMPO). FA-PEG-b-PDLA and mPEG-b-PLLA-TEMPO were prepared by combining ring-opening polymerization (ROP) of lactide with a series of conversion of the end functional groups. The synthesized block copolymers and their intermediates were well characterized by gel permeation chromatography (GPC) and 1H nuclear magnetic resonance (1H NMR) spectroscopy. The mixture of FA-PEG-b-PDLA and mPEG-b-PLLA-TEMPO self-assembled into spherical micelles with the average diameter about 200 nm through PLA stereocomplexation, which were characterized by dynamic light scattering (DLS), transmission electron microscopy (TEM) and differential scanning calorimetry (DSC). The formed micelles were confirmed to emit electron paramagnetic resonance (EPR) signals by EPR spectroscopy. Additionally, the formed micelles exhibited high loading capacity of hydrophobic anticancer drug, controlled in vitro drug release, satisfied biocompatibility and a significantly higher cellular uptake, indicating promising applications in smart drug delivery.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
LS74301 Poly(L-lactide)-block-poly(ethylene glycol)methyl ether Poly(L-lactide)-block-poly(ethylene glycol)methyl ether Price
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