Self-assembled micelles of well-defined pentaerythritol-centered amphiphilic A4B8 star-block copolymers based on PCL and PEG for hydrophobic drug delivery |
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Authors: | Mohammad Reza Nabid Seyed Jamal Tabatabaei Rezaei Hassan Niknejad Hossein Abdi Oskooie |
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Affiliation: | a Department of Chemistry, Shahid Beheshti University, G.C, 1983963113, Tehran, Iran b Department of Chemistry, School of Science, Azzahra University, Vanak, Tehran, Iran c Nanomedicine and Tissue Engineering Research Center, Shaheed Beheshti Medical University, Tehran, Iran d Lab of Polymer, Faculty of Chemistry, University of Tabriz, Tabriz, Iran |
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Abstract: | Biodegradable star-shaped poly(?-caprolactone) (PCL) with four arms were synthesized by ring-opening polymerization (ROP) from a symmetric pentaerythritol core via the ‘‘core-first’’ strategy. Subsequently, two samples of the amphiphilic A4B8 star-block copolymers with symmetrical topologies [4s(PCL-b-2sPEG)] were synthesized by a macromolecular coupling reaction between carboxyl-terminated poly(ethylene glycol) (PEG) and 4-arm star-shaped PCL macromers with eight -OH end groups. The latter was prepared by attaching 3-hydroxy-2-(hydroxymethyl)-2-methylpropanoic acid (HHMPA) to 4sPCL using a simple two-step reaction sequence. The in vitro cytotoxicity test indicated no apparent cytotoxicity. The amphiphilic star-block copolymers are capable of self-assembling into spherical micelles in water at room temperature, and they possess low critical micelle concentrations (CMCs) of 2∼8 mg/L in aqueous solution which was determined by fluorescence spectroscopy using pyrene as a probe. Transmission electron microscopy (TEM) measurement demonstrated that the micelles exhibit a spherical shape with a size range of 30∼50 nm in diameter. In addition, the hydrophobic and anticancer drug, quercetin, is loaded effectively in the polymeric micelles, suggesting that these new materials are appropriate candidates as hydrophobic drug nanocarriers. |
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Keywords: | Star-block copolymers Amphiphiles Hydrophobic drug nanocarriers |
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