Preparation of mPEG-b-PLA/TM-2 Micelle Lyophilized Products by Mixed Lyoprotectors and Antitumor Effect In Vivo.

The objective of this study was to encapsulate the poorly water-soluble drug TM-2 into polymer micelles using mPEG2k-b-PLA2.4k to increase its aqueous solubility and improve its therapeutic effect for liver cancer. Furthermore, in order to achieve long-term storage, the micelle solution was successfully freeze-dried. This study theoretically clarified the possibility of enhancing the water solubility of TM-2 using mPEG2k-b-PLA2.4k micelles as well as the protective effects of mixed lyoprotectants. Differential scanning calorimetry (DSC), X-ray diffraction (XRD), and scanning electron microscopy (SEM) were performed, which showed that the drug has a good affinity with the polymer (χ = 0.489) according to Flory-Huggins theory and that lyoprotectants reduced the crystallinity of PEG in mPEG2k-b-PLA2.4k and played a space-protective role in the lyophilization process. In vivo experiments showed that micellization could improve the drug bioavailability and give a high therapeutic effect with a tumor inhibition rate of 84.5% under the tolerated dose.