New N-acyl amino acid-functionalized biodegradable polyesters for pharmaceutical and biomedical applications

Abstract

A novel class of biodegradable polyesters has been generated by coupling poly(glycerol adipate) with N-acyl aromatic amino acids. This new set of polymers from this highly versatile polymeric platform may offer unprecedented new opportunities to produce biodegradable and biocompatible polymers with tailorable physical-chemical properties.

High‐Throughput Miniaturized Screening of Nanoparticle Formation via Inkjet Printing

“…In particular, it has been further modified with biological molecules such as fatty acids and amino acids in order to enhance drug protein or nucleic acids interactions or encapsulation, or simply to tailor its hydrophobic–hydrophilic balance . PGA derivatives, including the bare polymer, showed molecular weights in the order of 20 000 Da and all the materials were found to present an amorphous behaviour with T g transitions ranging from −33 to 49 °C (see also Table ) . Full characterization of these polymers has been published in the past and for this reason is not included in this present work.…”

“…PGA derivatives, including the bare polymer, showed molecular weights in the order of 20 000 Da and all the materials were found to present an amorphous behaviour with T g transitions ranging from −33 to 49 °C (see also Table ) . Full characterization of these polymers has been published in the past and for this reason is not included in this present work.…”

“…Therefore, the high‐throughput method of directly transferring the formulations in the well plates to any cell‐based assays required, including cytotoxicity assays, has been validated. It should be noted that previous literature has shown that PGA and its derivatives are not toxic (although different cell lines have been used in previous works) …”

“…Polymers, with different architectures, linear block copolymers, and grafted copolymers (polymer properties described in Table 1 ), were screened by using only microamounts/volumes (for a final NP concentration of 500 µg mL −1 only 100 µg of polymer was required in 10 µL of DMSO dispensed in around 10 s in 200 µL of water) to evaluate their ability to self‐assemble and to measure their size in different concentrations. All the concentrations were chosen based on previously published methods shown to allow polymer chains to self‐assemble in water, and the data for these polymers were compared against appropriate control materials …”

Exploring the enzymatic degradation of poly(glycerol adipate)

“…PGA self-assembles to form nanoparticles [5] which, with varying levels of stearic acid modification, have been shown to have low cytotoxicity in HL-60 and HepG 2 cells [6,7]. Unmodified PGA and PGA with a range of amino acid modifications have also been shown to have negligible lytic activity in a haemolytic assay [8]. The presence of the pendant eOH group in the polymer backbone allows for the conjugation of molecules with a variety of functional groups through simple coupling reactions, influencing the physicochemical properties of PGA and its ability to encapsulate a variety of drugs [6,[8][9][10].…”