Abstract

We report that the co-solvent polarity can precisely control the TPE-buried amphiphile 1 to self-assemble into nanoparticles (NPs) in water with size range from ∼21–32 nm to 55–68 nm to 95–106 nm. Excepted for size, these TPE-buried amphiphile fabricated NPs hold identical physical properties such as spherical shape, surface charge, and luminescent properties, and moreover, after covalent capture of the acrylate hydrophilic heads, the resulting cross-linked NPs (cNPs I–III) own excellent in vivo stability, which thus would be an ideal platform for investigating the size effects on tumor accumulation and penetration.

Highlights

  • The particle size plays a vital role in accumulation and penetration of nanoparticles (NPs) entering tumors [1, 2]

  • Since the polymeric micelle was developed as drug delivery system (PMDDSs) in 1980s, numerous good nanocarriers such as polymer micelles, Au nanoparticles and porous SiO2 nanoparticles have been used widely in drug delivery [3,4,5,6]

  • We report for the first time that the co-solvent polarity can precisely control the rotation degree of TPE skeleton buried in amphiphile 1, and lead it to self-assemble into nanoparticles in water with different sizes ranging from $21–32 nm to 55–68 nm to 95–106 nm to investigate the size effect (Scheme 1)

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Summary

Introduction

The particle size plays a vital role in accumulation and penetration of nanoparticles (NPs) entering tumors [1, 2]. The size effects of them have been extensively studied, the best sized NPs to improve tumor diagnostics and therapeutics were still in controversial These controversies were mainly ascribed to the different chemical structures and physical properties of NPs used for the size studies such as particle components, stability, surface charge, shape, and so on [7,8,9,10,11,12,13]. Such as polymer micelles, the size was regularly controlled by changing the polymer composition. For systematic investigation of the size effects in cancer drug delivery, the development of ideal platform that has exactly the same chemical structures and similar physical properties except for size would be highly valuable

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