Drug Carrier-Oriented Polygeline for Preparing Novel Polygeline-Bound Paclitaxel Nanoparticles

Polygeline is a highly promising drug carrier-oriented material for important applications in pharmacy field due to its low-cost and unique properties similar to albumin. In this study, polygeline-bound paclitaxel nanoparticles (Npb-PTXS) were fabricated through a combination of low-pressure emulsification and high-pressure homogenization. The effects of a series of production parameters on mean particle size, particle size distribution and drug loading of Npb-PTXS were systematically evaluated. The characteristics of Npb-PTXS, such as surface morphology, physical status of paclitaxel (PTX) in Npb-PTXS, redispersibility of Npb-PTXS in purified water and bioavailability in vivo were also investigated. It is revealed that the optimal preparation conditions included an aqueous phase pH value of about 6.5, protein mass concentration of 0.33%, with mass ratio of PTX to protein of 30%, high pressure of 1200 bar, high-pressure passes of 25 times and low-pressure emulsifying passes of 20 times. Obtained Npb-PTXS shows good resolubility compared to commercially available Abraxane^®, containing round or oval shaped particles with mean particle size of around 188.3 nm, polydispersity index of 0.163 and zeta potential of -31.1 mV. PTX in Npb-PTX is amorphous, and its content is approximately 12.04%. Encapsulation efficiency of Npb-PTXS reaches 81.2%. Moreover, in vivo pharmacokinetic studies showed that the intravenous relative bioavailability of Npb-PTXS to Abraxane was 83.89%.