Lin Zhu, Anton Taigind, and Vladimir P Torchilin
Center for Pharmaceutical Biotechnology and Nanomedicine, Northeastern University, Boston, MA 02115
To increase the solubility, bioavailablity and targetability of the water insoluble drug, paclitaxel (PTX), we synthesized a novel amphiphilic PEG-PTX conjugate with the matrix metalloprotease 2-sensitive peptide link between PEG and PTX, which was incorporated into novel nanocarrier system. Our system is a self-assembled micellar nanocarrier (Fig.1) containing three amphiphilic PEGbased conjugates, PEG(2000)-peptide- PTX, PEG(1000)-PE, and TATp-PEG(1000)- DOPE. Compared to conventional micellar drug delivery systems, this design ensures: i) a high drug loading efficiency, ii) an increased micelle stability, iii) an increased drug targetability, and iv) an enhanced drug internalization by the tumor cells.