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

Abstract 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 and donated as Hep-Brij 58 to facilitate the self-assembly into stable nanoparticles in aqueous. The self-assembled formation of Hep-Brij nanoparticles was demonstrated through DLS and TEM, whereas the iodine method identified the critical concentration for the self-assembled process. PTX was incorporated into Hep-Brij nanoparticles through the 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 outperformed in term of the amount PTX loaded. Hep-Brij 58/PTX was stable during 2 weeks of storage in distilled water. In vitro release of PTX from Hep-Brij 58 exhibited a control drug release effect following the diffusion kinetic. Furthermore, Hep-Brij 58 was non-toxic to primary healthy cells and cancer cells. The in vitro anticancer with Hela cell indicated remarkable anticancer activity of PTX-loaded Hep-Brij 58 nanoparticles compared to free PTX. Altogether, Hep-Brij 58 nanoparticles holds considerable potential for delivery system for managing PTX therapy