Jump to main content
Jump to site search


Structural exploration of hydrophobic core in polycationic micelles for improving siRNA delivery efficiency and cell viability

Author affiliations

Abstract

Improving siRNA delivery efficiency often encounters a dilemma with poor or decreased biocompatibility for polycationic micelles. To address this dilemma, this work focused on a structural exploration of the hydrophobic core in amphiphilic polycationic micelles by preparing two amphiphilic polycations with block or random hydrophobic segments, poly(ethylene glycol)-block-poly(aminoethyl methacrylate)-block-poly(2-diamylamine ethyl methacrylate)-block-poly(2-diethylamine ethyl methacrylate) (mPEG–PAMA–PD5A–PDEA, PADE) and poly(ethylene glycol)-block-poly(aminoethyl methacrylate)-block-poly(2-diamylamine ethyl methacrylate-co-2-diethylamine ethyl methacrylate) (mPEG–PAMA–P(D5A/DEA), PA(D/E)). The properties of the two copolymers and their self-assembly micelles were characterized, including structure, morphology, size and zeta potential. Cytotoxicity, siRNA silencing efficiency and cellular uptake of PADE/siRNA and PA(D/E)/siRNA complexes were evaluated in HepG2 and MDA-MB-231 cells in vitro. The endosome escape and intracellular distribution of PADE/siRNA and PA(D/E)/siRNA in HepG2 cells were also observed by CLSM. Significantly, the results indicated that PA(D/E)/siRNA showed not only better gene silencing efficiency but also lower cytotoxicity, which may be attributed to the homogeneous morphology of the hydrophobic core of PA(D/E) micelles. Therefore, this work provides a new pathway to overcome the dilemma between siRNA delivery efficiency and biocompatibility for the development of efficient polycation carriers.

Graphical abstract: Structural exploration of hydrophobic core in polycationic micelles for improving siRNA delivery efficiency and cell viability

Back to tab navigation

Supplementary files

Publication details

The article was received on 14 Oct 2018, accepted on 07 Jan 2019 and first published on 14 Jan 2019


Article type: Paper
DOI: 10.1039/C8TB02706D
Citation: J. Mater. Chem. B, 2019, Advance Article
  •   Request permissions

    Structural exploration of hydrophobic core in polycationic micelles for improving siRNA delivery efficiency and cell viability

    W. Huang, X. Wang, C. Wang, L. Du, J. Zhang, L. Deng, H. Cao and A. Dong, J. Mater. Chem. B, 2019, Advance Article , DOI: 10.1039/C8TB02706D

Search articles by author

Spotlight

Advertisements