J Biomed Nanotechnol. 2014 Jan;10(1):109-19. doi: 10.1166/jbn.2014.1791.
A pentablock copolymer of Poly(Lactide-co-Glycolide) and Pluronic F68 was synthesized using ring-opening polymerization and characterized by NMR and FTIR for confirming the structure of the block copolymer. TG-DTA studies showed PLGA:Pluronic ratio to be 4:1. As the PLGA-PEO-PPO-PEO-PLGA Pentablock Copolymer (PPPC) prepared is amphiphilic, its Critical Vesicular Concentration, was measured, which was lower at 37 degrees C than at 25 degrees C, which could provide better stability to the system at physiological temperature. The nanoparticles of PPPC vary in topographyand range from 150 to 500 nm in size, according to the synthesis route used viz Emulsion Solvent Evaporation and simple dialysis. Pentablock copolymer nanoparticles were found to entrap about 84% of hydrophobic drug, docetaxel. Drug release profile of docetaxel showed about 50% release in first 2 hours at pH 4.6 and about 80% docetaxel was released at pH 7.4, at the end of 2 days. The PPPC nanoparticles was found to be biocompatible to L929 cell lines up to 1 mg/ml concentration. Preliminary in vitro cytotoxic effect of docetaxel loaded PPPC nanoparticles against four different cancer cell lines showed 50% inhibitory concentration of 6 nM in A431 (Squamous cell carcinoma), 250 nM in HeLa (Cervical carcinoma), 800 nM in PC3 (Prostate carcinoma) and 1 microM in KB (Epidermoid carcinoma) cells.
聚（丙交酯-乙交酯）和泊洛沙姆 F68 的五嵌段共聚物是通过开环聚合合成的，并通过 NMR 和 FTIR 进行了表征，以确认嵌段共聚物的结构。TG-DTA 研究表明 PLGA：Pluronic 的比例为 4：1。由于所制备的 PLGA-PEO-PPO-PEO-PLGA 五嵌段共聚物（PPPC）是两亲性的，因此测量了其临界囊泡浓度，在 37°C 时比在 25°C 时低，这可以为生理温度下的系统提供更好的稳定性。根据使用的合成路线，即乳液溶剂蒸发和简单透析，PPPC 的纳米粒子的形貌不同，大小从 150nm 到 500nm 不等。发现 PPPC 嵌段共聚物纳米粒子可以包裹约 84%的疏水性药物，多西紫杉醇。多西紫杉醇的药物释放曲线显示，在 pH4.6 下的前 2 小时内释放了约 50%，在 pH7.4 下的 2 天结束时释放了约 80%的多西紫杉醇。发现 PPPC 纳米粒子在 1mg/ml 浓度下对 L929 细胞系是生物相容的。载有多西紫杉醇的 PPPC 纳米粒子对四种不同癌细胞系的初步体外细胞毒性作用表明，A431（鳞状细胞癌）中的 50%抑制浓度为 6nM，HeLa（宫颈癌）中的 250nM，PC3（前列腺癌）中的 800nM 和 KB（表皮样癌）中的 1μM。
