PotM: Limited Offer - Polysarcosine Bundles

Published on 02/05/2023

From beginning of May until end of July 2023 we offer special polysarcosine bundles each containing three functionalized PSars of different molecular weight (5 kDa, 10 kDa, 15 kDa), 100 mg each.

PotM: Limited Offer - Polysarcosine Bundles

Modern drug development technologies such as combinatorial chemistry and automated high-throughput screening have led to the identification of numerous potential new active pharmaceutical ingredients (APIs). However, many of those promising new molecules never reach market approval because they are not sufficiently soluble, cannot reach the desired target, are attacked by the immune system, are degraded by endogenous enzymes, or suffer from rapid renal clearance.

To overcome these restrictions, first attempts with polymers were made already in the 1960s – either by attaching the therapeutic agent covalently to a polymer or by entrapping it non-covalently in a polymer nanoparticle. The first polymer-drug conjugates that showed promising results contained poly(ethylene glycol) (PEG), and until today, PEG is the most widely used standard.

However, PEG is made of monomer units connected via an ether bond. This is a rather rare chemical bond in living nature and not used in natural biopolymers. Consequently, the human body does not possess suitable enzymes to degrade polyether molecules – leading to undesired accumulation of large PEG molecules in cells upon long-term treatment with high doses of PEG.

Besides, the increasing use of PEGs and PEGylated products in pharmaceutical research led to additional insights:

PEGs, which were originally thought to be non-immunogenic, turned out to provoke immune reactions in several individuals.
Adverse side effects in the body can be provoked by the polymer itself or by side products formed during synthesis that may lead to hypersensitivity.
Unexpected changes in the pharmacokinetic behavior can occur with PEG-based carriers.

Biodegradable poly(amino acids) appear very attractive in this context. As with PEGs, the termini of these polymers can be equipped with various functionalizations to make the polymer more hydrophilic or more hydrophobic, inert, or reactive.

Poly(sarcosine) (PSar) – originating from the natural, non-toxic amino acid sarcosine (N-methylglycine) – is the simplest polypeptoid and a newly rediscovered biocompatible and degradable polymer. PSar is hydrophilic and shows excellent non-fouling properties, leading to protein-repellent surfaces and long-circulating polymers or polymer nanoparticles.

→ Don’t allow your creativity to be limited! Try out poly(sarcosine) for PEG replacement and discover its unique properties.
→ To support your research efforts, we offer special trial bundles at a discounted price (valid from beginning of May till end of July 2023).

Mal-PSar-OMe Bundle PSB1000

Iris Code	Structure	MW (kDa)	Unit
PSR1740		5	100 mg
PSR1750		10	100 mg
PSR1760		15	100 mg

NHS-PSar-OMe Bundle PSB1010

Iris Code	Structure	MW (kDa)	Unit
PSR1770		5	100 mg
PSR1780		10	100 mg
PSR1790		15	100 mg

MeO-PSar-COOH Bundle PSB1020

Iris Code	Structure	MW (kDa)	Unit
PSR1840		5	100 mg
PSR1850		10	100 mg
PSR1860		15	100 mg

N3-PSar-Ac Bundle PSB1030

Iris Code	Structure	MW (kDa)	Unit
PSR1870		5	100 mg
PSR1880		10	100 mg
PSR1890		15	100 mg

Alkyne-PSar-Ac Bundle PSB1040

Iris Code	Structure	MW (kDa)	Unit
PSR1900		5	100 mg
PSR1910		10	100 mg
PSR1920		15	100 mg

Find many poly(amino acid) derivatives in our section Drug Delivery
For more detailed information, download our brochure Polymer Therapeutics

References:

Suppressive immune response of poly-(sarcosine) chains in peptide-nanosheets in contrast to polymeric micelles; E. Hara, M. Ueda, C. J. Kim, A. Makino, I. Hara, E. Ozeki, S. Kimura; J. Pept. Sci. 2014; 20: 570-577. https://doi.org/10.1002/psc.2655.

Thermoresponsive release from poly(Glu(OMe))-block-poly(Sar) microcapsules with surface-grafting of poly(N-isopropylacrylamide); T. Kidchob, S. Kimura, Y. Imanishi; J. Control. Release 1998; 50: 205-14. https://doi.org/10.1016/s0168-3659(97)00135-1.

Amphiphilic poly(Ala)-b-poly(Sar) microspheres loaded with hydrophobic drug; T. Kidchob, S. Kimura, Y. Imanishi; J. Control. Release 1998; 51: 241-248. https://doi.org/10.1016/s0168-3659(97)00176-4.

On the biodegradability of polyethylene glycol, polypeptoids and poly(2-oxazoline)s; J. Ulbricht, R. Jordan, R. Luxenhofer; Biomaterials 2014; 35: 4848-4861. https://doi.org/10.1016/j.biomaterials.2014.02.029.

Polypeptoids: A Perfect Match for Molecular Definition and Macromolecular Engineering? R. Luxenhofer, C. Fetsch, A. Grossmann; J. Polym. Sci.: Part A: Polym. Chem. 2013; 51: 2731-2752. https://doi.org/10.1002/pola.26687.

Polysarcosine as an Alternative to PEG for Therapeutic Protein Conjugation; Y. Hu, Y. Hou, H. Wang, H. Lu; Bioconjugate Chem. 2018; 29(7): 2232-2238. https://doi.org/10.1021/acs.bioconjchem.8b00237.

Polysarcosine-containing copolymers: Synthesis, characterization, self-assembly, and applications; A. Birke, J. Ling, M. Barz; Prog. Polym. Sci. 2018; 81: 163-208; https://doi.org/10.1016/j.progpolymsci.2018.01.002.

Polysarcosine-Functionalized Lipid Nanoparticles for Therapeutic mRNA Delivery; S. Nogueira, A. Schlegel, K. Maxeiner, B. Weber, M. Barz, M. A. Schroer, C. E. Blanchet, D. Svergun, S. Ramishetti, D. Peer, P. Langguth, U. Sahin, H. Haas; ACS Appl. Nano Mater. 2020; 3(11): 10634-10645. https://doi.org/10.1021/acsanm.0c01834.