Merck
  • Home
  • Search Results
  • Balancing polymer hydrophobicity for ligand presentation and siRNA delivery in dual function CXCR4 inhibiting polyplexes.

Balancing polymer hydrophobicity for ligand presentation and siRNA delivery in dual function CXCR4 inhibiting polyplexes.

Biomaterials science (2015-07-07)
Y Wang, J Li, Y Chen, D Oupický
ABSTRACT

In the present study, a series of copolymers (PAMD-Ch) was synthesized by grafting polymeric Plerixafor/AMD3100 (PAMD) with different amounts of cholesterol and the effect of cholesterol modification on siRNA delivery was investigated. PAMD-Ch/siRNA polyplexes exhibited improved colloidal and enzymatic stability when compared with PAMD/siRNA polyplexes containing no cholesterol. PAMD-Ch with low (17 wt%) and medium (25 wt%) cholesterol content exhibited CXCR4 antagonism comparable to unmodified PAMD. Cholesterol modification increased cell uptake of siRNA polyplexes and significantly decreased sensitivity of siRNA transfection to the presence of serum. When used to deliver anticancer siRNA against polo-like kinase 1 (PLK1), polyplexes based on PAMD-Ch with 17 wt% cholesterol exhibited the highest cancer cell killing activity both in serum-free and serum-containing conditions. Overall, the results of this study validate cholesterol modified PAMD as dual-function delivery vectors suitable for efficient delivery of anticancer siRNA and simultaneous CXCR4 inhibition for combined anticancer therapies.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
N,N-Diisopropylethylamine, ReagentPlus®, ≥99%
SAFC
Cholesterol, Plant-Derived, SyntheChol®, NF, Ph. Eur., JP
Sigma-Aldrich
N,N-Diisopropylethylamine, purified by redistillation, 99.5%
Sigma-Aldrich
HMBA, ≥98% (HPLC), solid
Sigma-Aldrich
Sodium acetate, anhydrous, BioUltra, for luminescence, for molecular biology, ≥99.0% (NT)
Sigma-Aldrich
Sodium acetate solution, BioUltra, for molecular biology, ~3 M in H2O
Sigma-Aldrich
Sodium acetate, 99.995% trace metals basis
Sigma-Aldrich
Sodium Acetate Anhydrous, >99%, FCC, FG
Sigma-Aldrich
Cholesteryl chloroformate, 95%
Sigma-Aldrich
N,N′-Hexamethylene bis(acetamide), 98%
Sigma-Aldrich
Sodium acetate, powder, BioReagent, suitable for electrophoresis, suitable for cell culture, suitable for insect cell culture, ≥99%
Sigma-Aldrich
Sodium acetate, meets USP testing specifications, anhydrous
Sigma-Aldrich
Sodium acetate, BioXtra, ≥99.0%
Sigma-Aldrich
Sodium acetate, anhydrous, for molecular biology, ≥99%
Sigma-Aldrich
Cholesterol, powder, BioReagent, suitable for cell culture, ≥99%
Sigma-Aldrich
Cholesterol, from sheep wool, ≥92.5% (GC), powder
Sigma-Aldrich
Cholesterol, Sigma Grade, ≥99%
Sigma-Aldrich
SyntheChol® NS0 Supplement, 500 ×, synthetic cholesterol, animal component-free, aqueous solution, sterile-filtered, suitable for cell culture
SAFC
Cholesterol, from sheep wool, Controlled origin, meets USP/NF testing specifications