Hyaluronic acid-coated nanostructured lipid carriers for targeting paclitaxel to cancer

The aim of our study was to develop hyaluronic acid-coated, paclitaxel-loaded, nanostructured lipid carriers (HA-NLCs) prepared via electrostatic attraction for delivering paclitaxel (PTX) to tumors overexpressing CD44. First, cationic PTX-NLC was prepared by melt emulsion technology. Then, PTX-NLC were coated with hyaluronic acid (HA). The in vitro release of PTX was evaluated by the dialysis method. This analysis showed that PTX was released more slowly from HA-NLC than from Taxol®. The in vitro cytotoxicity of HA-NLC was investigated using the MTT method in B16, CT26 and HCT116 cell lines. The results showed that the cytotoxicity of HA-NLC against these three cancer cell lines was superior to that of Taxol®. The in vivo antitumor effect, the pharmacokinetics and the tissue distribution of HA-NLC were all evaluated in B16-bearing Kunming mice. The results showed that HA-NLC was better tolerated and had increased antitumor activity in B16-bearing Kunming mice compared with Taxol®. Furthermore, HA-NLC could prolong the circulation time of PTX in blood and increase the accumulation of PTX in the tumor. Therefore, HA-NLC prepared via electrostatic attraction was an effective carrier for delivering PTX to tumors overexpressing CD44.

► We successfully prepared hyaluronic acid coated, paclitaxel loaded, nanostructured lipid carriers (HA-NLCs) via electrostatic attraction.
► The in vitro cytotoxicity of HA-NLCs was superior to that of Taxol® in B16, CT26 and HCT116 cell lines.
► The in vivo antitumor effect of HA-NLCs in B16-bearing Kunming mice was extremely promising.
► HA-NLC prepared via electrostatic attraction was an effective carrier for delivering paclitaxel PTX to tumors overexpressing CD44.