Improving systemic circulation of paclitaxel nanocrystals by surface hybridization of DSPE-PEG2000.

This paper aims to improve the systemic circulation of paclitaxel (PTX) by modifying nanocrystals with DSPE-PEG 2000. PTX nanocrystals (PNCs) were prepared by an anti-solvent method and DSPE-PEG 2000 was inserted into PNCs by hybridization. The average size of DSPE-PEG-PNCs did not change obviously compared to the naked PNCs, but the negative charge increased after hybridization. The saturated attachment ratio of DSPE-PEG 2000 was 0.4%. In vitro release rate of DSPE-PEG-PNCs was significantly slower than that of PTX solution and the naked PNCs, which indicated that DSPE-PEG 2000 hindered the release of PTX. Moreover, pharmacokinetics results showed that DSPE-PEG-PNCs achieved a higher area-under-the-curve (AUC, 4.43 ± 0.19 mg/L*h) and lower clearance rate (1.08 ± 0.16 L/h/kg) compared to PNCs with an AUC of 2.48 ± 0.18 mg/L*h and a clearance rate of 1.89 ± 0.15 L/h/kg. Therefore, DSPE-PEG-PNCs could have a significant potential in clinical use by improving the systemic circulation of the drug.