Two novel nanoscale preparations of micelle and thermosensitive hydrogel for docetaxel to treat malignant tumor.

In this paper, two nanoscale preparations were described for docetaxel encapsulation using poly(epsilon-caprolactone)poly(ethylene glycol)-poly(epsilon-caprolactone) (PCEC) copolymer as carrier for treating malignant tumor. The first formulation was docetaxel-loaded PCEC micelle (D-M), which was characterized by XRD, TEM and Malvern laser particle size and drug release studies. The highest drug-loading of docetaxel in micelle was about 22.1 +/- 1.9%, optimized average diameter and polydispersity index was 25.2 +/- 1.1 nm, 0.13 +/- 0.12, respectively. Another formulation was docetaxel-loaded PCEC thermosensitive hydrogel (D-H), which displayed special gel-sol transition behavior with body temperature. We studied the cytotoxicity and in vitro hemolytic test of blank PCEC copolymer, the result was superiority. The data of relative body weight (RW), relative tumor volume (RV) and micrographs of hematoxylin and eosin (H&E)-stained histological sections showed D-M and D-H had significant antitumor effect and exhibited different characteristics of antitumor activity. Thus, the experiments signified that the combination therapy of intravenous (i.v.) and intratumoral administration using the two formulations maybe an effective way to treat malignant tumor.