Polyethylene glycol hexadecyl ether modified heparin for paclitaxel nano-delivery system

A paclitaxel (PTX) nano-delivery system using modified heparin and polyethylene glycol hexadecyl ether (Brij 58) was developed in this study. Brij 58 was conjugated to the heparin backbone via the cystamine bridge, denoted as Hep-Brij 58, to facilitate self-assembly into stable nanoparticles in an aqueous environment. The self-assembled formation of Hep-Brij nanoparticles was demonstrated through dynamic light scattering and TEM, while the iodine method identified the critical concentration for the self-assembled process. PTX was incorporated into Hep-Brij nanoparticles through physical entrapment. The PTX-loaded Hep-Brij nanoparticles were then characterized according to particle size and size distribution, drug-loading content, and efficiency. Compared to Brij 58, Hep-Brij 58 was more effective in terms of the amount of PTX loaded. Hep-Brij 58/PTX was stable over two weeks of storage in distilled water.<i>In vitro</i>release of PTX from Hep-Brij 58 exhibited a controlled drug release effect following the diffusion kinetics. Furthermore, Hep-Brij 58 was non-toxic to primary healthy cells and cancer cells. The<i>in vitro</i>anticancer test with Hela cells indicated remarkable anticancer activity of PTX-loaded Hep-Brij 58 nanoparticles compared to free PTX. In summary, Hep-Brij 58 nanoparticles hold considerable potential for use as a delivery system for managing PTX therapy.