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    Interfacial properties and micellization of triblock poly(ethylene glycol)-poly(epsilon-caprolactone)-polyethyleneimine copolymers

    Year: 2020

    Journal: Acta Pharm. Sin. B, Volume 10, JUN, page 1122–1133

    Authors: Li, J; Du, YT; Su, HT; Cheng, SX; Zhou, YX; Jin, YG; Qi, XR

    Organizations: NSFC (China)National Natural Science Foundation of China (NSFC) [81673365, 81973258, 81473156]; Fangzheng Foundation (China)

    Keywords: Block copolymers; Langmuir films; Molecular arrangement; Self-assembly; Nanostructure

    This study aimed to explore the link between block copolymers' interfacial properties and nanoscale carrier formation and found out the influence of length ratio on these characters to optimize drug delivery system. A library of diblock copolymers of PEG-PCL and triblock copolymers with additional PEI (PEG-PCL-PEI) were synthesized. Subsequently, a systematic isothermal investigation was performed to explore molecular arrangements of copolymers at air/water interface. Then, structural properties and drug encapsulation in self-assembly were investigated with DLS, SLS and TEM. We found the additional hydrogen bond in the PEG-PCL-PEI contributes to film stability upon the hydrophobic interaction compared with PEG-PCL. PEG-PCL-PEI assemble into smaller micelle-like (such as PEG-PCL4006-PEI) or particle-like structure (such as PEG-PCL8636-PEI) determined by their hydrophilic and hydrophobic block ratio. The distinct structural architectures of copolymer are consistent between interface and self-assembly. Despite the disparity of constituent ratio, we discovered the arrangement of both chains guarantees balanced hydrophilic-hydrophobic ratio in self-assembly to form stable construction. Meanwhile, the structural differences were found to have significant influence on model drugs incorporation including docetaxel and siRNA. Taken together, these findings indicate the correlation between molecular arrangement and self-assembly and inspire us to tune block compositions to achieve desired nanostructure and drug loading. (C) 2020 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.
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