Diblock Copolymer Hydrophobicity Facilitates Efficient Gene Silencing and Cytocompatible Nanoparticle-Mediated siRNA Delivery to Musculoskeletal Cell Types

Biomacromolecules. 2017 Nov 13;18(11):3753-3765. doi: 10.1021/acs.biomac.7b01349. Epub 2017 Oct 11.

Abstract

pH-responsive diblock copolymers provide tailorable nanoparticle (NP) architecture and chemistry critical for siRNA delivery. Here, diblock polymers varying in first (corona) and second (core) block molecular weight (Mn), corona/core ratio, and core hydrophobicity (%BMA) were synthesized to determine their effect on siRNA delivery in murine tenocytes (mTenocyte) and murine and human mesenchymal stem cells (mMSC and hMSCs, respectively). NP-mediated siRNA uptake, gene silencing, and cytocompatibility were quantified. Uptake is positively correlated with first block Mn in mTenocytes and hMSCs (p ≤ 0.0005). All NP resulted in significant gene silencing that was positively correlated with %BMA (p < 0.05) in all cell types. Cytocompatibility was reduced in mTenocytes compared to MSCs (p < 0.0001). %BMA was positively correlated with cytocompatibility in MSCs (p < 0.05), suggesting stable NP are more cytocompatible. Overall, this study shows that NP-siRNA cytocompatibility is cell type dependent, and hydrophobicity (%BMA) is the critical diblock copolymer property for efficient gene silencing in musculoskeletal cell types.

MeSH terms

  • Animals
  • Gene Silencing
  • Gene Transfer Techniques*
  • HeLa Cells
  • Humans
  • Hydrogen-Ion Concentration
  • Hydrophobic and Hydrophilic Interactions / drug effects
  • Mesenchymal Stem Cell Transplantation
  • Mice
  • Muscle, Skeletal / cytology
  • Muscle, Skeletal / metabolism*
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry
  • Polyethylene Glycols / chemistry
  • Polymers / administration & dosage*
  • Polymers / chemistry
  • RNA, Small Interfering / administration & dosage*
  • RNA, Small Interfering / chemistry
  • RNA, Small Interfering / genetics

Substances

  • Polymers
  • RNA, Small Interfering
  • Polyethylene Glycols