Efficient Dual siRNA and Drug Delivery Using Engineered Lipoproteoplexes

Biomacromolecules. 2017 Sep 11;18(9):2688-2698. doi: 10.1021/acs.biomac.7b00203. Epub 2017 Aug 4.

Abstract

An engineered supercharged coiled-coil protein (CSP) and the cationic transfection reagent Lipofectamine 2000 are combined to form a lipoproteoplex for the purpose of dual delivery of siRNA and doxorubicin. CSP, bearing an external positive charge and axial hydrophobic pore, demonstrates the ability to condense siRNA and encapsulate the small-molecule chemotherapeutic, doxorubicin. The lipoproteoplex demonstrates improved doxorubicin loading relative to Lipofectamine 2000. Furthermore, it induces effective transfection of GAPDH (60% knockdown) in MCF-7 breast cancer cells with efficiencies comparing favorably to Lipofectamine 2000. When the lipoproteoplex is loaded with doxorubicin, the improved doxorubicin loading (∼40 μg Dox/mg CSP) results in a substantial decrease in MCF-7 cell viability.

MeSH terms

  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / chemistry*
  • Doxorubicin / administration & dosage
  • Doxorubicin / chemistry*
  • Drug Carriers / chemistry*
  • Humans
  • Lipids / chemistry
  • MCF-7 Cells
  • RNA, Small Interfering / chemistry*

Substances

  • Antineoplastic Agents
  • Drug Carriers
  • Lipids
  • Lipofectamine
  • RNA, Small Interfering
  • Doxorubicin