Paclitaxel-loaded polymeric micelles based on poly(ɛ-caprolactone)-poly(ethylene glycol)-poly(ɛ-caprolactone) triblock copolymers: in vitro and in vivo evaluation.

The purpose of this study was to develop polymeric nanoscale drug-delivery system (nano-DDS) for paclitaxel (PTX) from poly(ɛ-caprolactone)-poly(ethylene glycol)-poly(ɛ-caprolactone) (PCL-PEG-PCL, PCEC) copolymers, intended to be intravenously administered, able to improve the therapeutic efficacy of the drug and devoid of the adverse effects of Cremophor EL. Both of the PTX-loaded polymeric micelles and polymersomes were successfully prepared from PCEC copolymers. The obtained PTX-loaded micelles exhibited core-shell morphology with satisfactory size (93 nm), and were favorable for intravenous injection. In vitro cytotoxicity demonstrated that the cytotoxic effect of PTX-loaded micelles was lower than that of Taxol (Bristol-Myers Squibb, Princeton, New Jersey). Pharmacokinetic results indicated that the PTX-loaded micelles had longer systemic circulation time and slower plasma elimination rate than those of Taxol. Furthermore, PTX-loaded micelles showed greater tumor growth-inhibition effect in vivo on EMT6 breast tumor, in comparison with Taxol. Therefore, the prepared polymeric micelles might be potential nano-DDS for PTX delivery in cancer chemotherapy.

Zhang L ，He Y ，Ma G ，Song C ，Sun H ... -  《-》

Enhanced anti-glioblastoma efficacy by PTX-loaded PEGylated poly(ɛ-caprolactone) nanoparticles: In vitro and in vivo evaluation.

The aim of this work was to investigate the anti-tumor effect of paclitaxel (PTX)-loaded methoxy poly(ethylene glycol)-poly(ɛ-caprolactone) nanoparticles (MPEG-NP/PTX) against glioblastoma multiforme (GBM). MPEG-NP/PTX was prepared by the emulsion and evaporation technique with particle size of 72.5±2.2nm and did not change remarkably during the period of 21-day storage at 4°C. The drug-loading coefficient and encapsulation ratio of optimized formulation were 8.2±0.6% and 90.4±2.3%, respectively. The in vitro release behavior exhibits a biphase release manner and was affected by PEG segment. In vitro cytotoxicity was assessed using C6 cell lines and was compared to Taxol and PTX-loaded poly(ɛ-caprolactone) conventional nanoparticles (NP/PTX). Cell viability assay against C6 cells exhibited higher or at least comparable cytotoxicity than that of Taxol and NP/PTX. More importantly, in vivo real-time fluorescence imaging analysis in intracranial C6 glioblastoma bearing mice showed that the methoxy poly(ethylene glycol)-poly(ɛ-caprolactone) nanoparticles (MPEG-NP) displayed much stronger fluorescence signal and 3-fold larger Area-Under-Curve (AUC) than poly(ɛ-caprolactone) conventional nanoparticles (NP) in tumor-bearing brain. Furthermore, in vivo anti-glioblastoma effect exhibited the mean survive time of MPEG-NP/PTX (28 days) was much longer than those of Taxol injection (20 days) and NP/PTX (23 days). Therefore, MPEGylated poly(ɛ-caprolactone) nanoparticles significantly enhanced the anti-glioblastoma activity of PTX and might be considered a promising drug delivery system against advanced glioblastoma.

Xin H ，Chen L ，Gu J ，Ren X ，Wei Z ，Luo J ，Chen Y ，Jiang X ，Sha X ，Fang X ... -  《-》

Improving anti-tumor activity with polymeric micelles entrapping paclitaxel in pulmonary carcinoma.

Gong C ，Xie Y ，Wu Q ，Wang Y ，Deng S ，Xiong D ，Liu L ，Xiang M ，Qian Z ，Wei Y ... -  《-》

Polysorbate 80 coated poly (ɛ-caprolactone)-poly (ethylene glycol)-poly (ɛ-caprolactone) micelles for paclitaxel delivery.

In this article, polysorbate 80 coated poly (ɛ-caprolactone)-poly (ethylene glycol)-poly (ɛ-caprolactone) (PCEC) micelles were successfully prepared for paclitaxel (PTX) delivery. The particle size distribution, morphology, drug loading, encapsulation efficiency and sustained release profile of the micelles were studied in detail. The safety of the micelle formulation was evaluated by MTT assay on HEK293 cells. And the encapsulated PTX in the micelles remained potent antitumor effect on C6 glioma cells. The pharmacokinetic study showed that the PCEC micelles coated with polysorbate 80 altered the biodistribution pattern and increased PTX concentration in the brain significantly compared to the uncoated micelles and the free drug after intravenous injection. The results indicated that polysorbate 80 coated PCEC micelles might be a candidate for PTX delivery for brain tumor chemotherapy.

Wang Y ，Wang C ，Gong C ，Wang Y ，Guo G ，Luo F ，Qian Z ... -  《-》

Novel self-assembling PEG-p-(CL-co-TMC) polymeric micelles as safe and effective delivery system for paclitaxel.

Danhier F ，Magotteaux N ，Ucakar B ，Lecouturier N ，Brewster M ，Préat V ... -  《-》