Functionalized PEI Development Service

Polyethyleneimine (PEI) is used as the gold standard for non-viral gene delivery. Our company is committed to providing customers with a variety of chemical modification strategies to obtain functionalized PEI and PEI derivatives for use as small interfering RNA (siRNA) and DNA gene carriers. Our specialized non-viral vector development services will contribute to accelerating the development of gene therapies for rare diseases.

Background

PEI has become the most widely studied cationic polymer for non-viral vector design and is available in both linear (l-PEI) and branched (b-PEI) topologies. PEI can form polyplexes with nucleic acids through electrostatic self-assembly. Furthermore, PEI-based delivery systems offer excellent transfection efficiency because of the high buffering capacity of PEI, which facilitates the endosomal escape of the gene payload.

In recent years, considerable progress has been made in the use of PEI-based vectors for the delivery of gene drugs. However, the drawbacks of PEI lacking specificity, being non-degradable, generating inherently unstable complexes, and aggregating in the bloodstream have limited their use in gene therapy. Gene delivery is a multi-step process that requires carriers capable of overcoming each obstacle in the delivery trajectory. Advances in bio-conjugation chemistry and appropriate functionalization of PEI polymers promise to open up new avenues for the diagnosis and therapeutics of human rare diseases.

Fig. 1 Schematic illustrations of the formation of PEI-FPBA-DopaChol micelles (PFCDM)/siRNA cationic micelles (a) and intracellular siRNA delivery by PFCDM/siRNA (b). (Jiang C, et al., 2019)

Our Services

Our researchers focus on establishing a variety of ways to improve this promising vector to undertake polynucleotide delivery. We offer multiple modification strategies, such as the use of various crosslinkers, different polymers, and ligands to design degradable PEI derivatives and improve transfection efficiency and target specificity. Our services include, but are not limited to:

Modifications of PEI by polymer functionalization
- PEGylation of PEI
  Starting with low molecular weight (MW) PEI and PEG, our research group has designed water-soluble, biodegradable, biocompatible, low cytotoxicity, and long circulation time cationic copolymers for gene delivery.
- Saccharides conjugation on PEI
  We enhanced transfection efficiency by attaching modified derivatives, such as glycol chitosan, to PEI polymers. In addition to polysaccharides, we also use oligosaccharides to change the pharmacokinetic characteristics of PEI, such as the development of oligomaltose-grafted PEI.
- PEI modification with polylactide
  We help customers prepare triblock copolymers composed of linear PEI, PEG, and poly(l-lactide) (PLLA) to improve cell penetration and biodegradability.
Grafting targeting ligands on PEI
We increase cell uptake by incorporating target-specific ligands including RGD and HIV-1 Tat peptide, epidermal growth factor (EGF), hyaluronic acid (HA), transferrin (Tf), and folic acid (FA), thus improving the efficiency of PEI-based vectors.
Chemically modified PEI
- We help customers prepare PEI derivatives containing ester bonds through Michael addition of PEI to diacrylates acting as cross-linkers to improve cellular gene delivery efficiency.
- We help customers improve DNA delivery and transfection efficiency by cross-linking PEI with low MW cross-linking reagent, dithiobis(succinimidyl propionate) (DSP), to produce reducible disulfide bonds.
Development of smart PEIs for controlled gene delivery
We assist customers in developing intelligent gene carriers that release gene cargoes precisely and at the right time at the pathological target site.
- Development of endogenous stimuli-responsive vectors, including pH-responsive vectors, reactive oxygen species (ROS)-responsive vectors, redox-responsive vectors, and biomolecule-responsive vectors.
- Development of exogenous stimuli-responsive vectors, including thermo-responsive vectors, light-responsive vectors, and magnetic-responsive vectors.
- Development of dual-responsive vectors.

With our extensive experience and advanced technology in the field of gene delivery vector development, our company is able to offer customers the development of functionalized PEIs for gene delivery. We meet a wide range of needs in gene therapy through the rational modification of PEIs or the development of stimuli-responsive PEIs. Please contact us for more details and to get a formal quote.

Reference

Jiang, C.; et al. Recent advances in the development of polyethyleneimine-based gene vectors for safe and efficient gene delivery. Expert Opinion on Drug Delivery, 2019, 16(4): 363-376.

All of our services and products are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.

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