In Situ Functionalized Polymers for siRNA Delivery.
A new method is reported herein for screening the biological activity of functional polymers across a consistent degree of polymerization and in situ, that is, under aqueous conditions and without purification/isolation of candidate polymers. In brief, the chemical functionality of a poly(acryloyl hydrazide) scaffold was activated under aqueous conditions using readily available aldehydes to obtain amphiphilic polymers. The transport activity of the resulting polymers can be evaluated in situ using model membranes and living cells without the need for tedious isolation and purification steps. This technology allowed the rapid identification of a supramolecular polymeric vector with excellent efficiency and reproducibility for the delivery of siRNA into human cells (HeLa-EGFP). The reported method constitutes a blueprint for the high-throughput screening and future discovery of new polymeric functional materials with important biological applications.
Departamento de Química Orgánica, Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares (CIQUS), Universidade de Santiago de Compostela, E-15782, Spain.
Juan M
0000-0001-8045-6144
JM
Priegue
School of Chemistry, University of Birmingham, B15 2TT, UK.
Daniel N
0000-0001-6938-3765
DN
Crisan
Departamento de Bioquimica y Biología Molecular, Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares (CIQUS), Universidade de Santiago de Compostela, E-15782, Spain.
José
0000-0002-8877-7775
J
Martínez-Costas
Departamento de Química Orgánica, Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares (CIQUS), Universidade de Santiago de Compostela, E-15782, Spain.
Juan R
0000-0002-5842-7504
JR
Granja
School of Chemistry, University of Birmingham, B15 2TT, UK. f.fernandez-trillo@bham.ac.uk.
Francisco
0000-0002-6680-5683
F
Fernandez-Trillo
Departamento de Química Orgánica, Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares (CIQUS), Universidade de Santiago de Compostela, E-15782, Spain. javier.montenegro@usc.es.
Javier
0000-0001-6503-2095
J
Montenegro
D016503:Drug Delivery Systems; D006367:HeLa Cells; D006801:Humans; D011108:Polymers / Q000737:chemistry* / Q000494:pharmacology; D034741:RNA, Small Interfering / Q000494:pharmacology*; D015203:Reproducibility of Results
D011108:Polymers; D034741:RNA, Small Interfering
lipid bilayer membranes; polymers; siRNA delivery; supramolecular chemistry; vesicles