University of Oslo, School of Pharmacy, Department of Pharmacy, Division Pharmaceutics, Norway.
Eur J Pharm Sci. 2011 Jun 14;43(3):180-7. doi: 10.1016/j.ejps.2011.04.004. Epub 2011 Apr 20.
The influence of four nonionic Pluronic block copolymers (L44, F68, P123 and F127) on the solubilization and aggregation of the novel anionic amphiphilic photosensitizer TPCS(2a), intended for use in the technology of photochemical internalization (PCI), was evaluated in aqueous media as part of pharmaceutical preformulation studies. The evaluation was performed by use of UV-Vis spectroscopy for diluted samples of TPCS(2a) (3×10(-6)M), and capillary viscosimetry, freezing point depression measurements and atomic force microscopy (AFM) at pharmaceutical relevant concentrations (2; 10 or 30 mg/ml TPCS(2a)). The critical micelle concentration (CMC) of the Pluronics in presence of TPCS(2a) was determined spectrophotometrically. The Pluronic block copolymers solubilized the photosensitizer above CMC at ambient temperature by formation of vehicle-drug complexes apparently organized in networks of varying viscosity and morphology, which were sensitive towards the addition of neutral and charged excipients.
作为药物预配方研究的一部分，评估了四种非离子型 Pluronic 嵌段共聚物（L44、F68、P123 和 F127）对新型阴离子两亲性光敏剂 TPCS(2a) 的增溶和聚集的影响，该光敏剂拟用于光化学内化（PCI）技术。通过使用紫外-可见分光光度法对稀释的 TPCS(2a)（3×10(-6)M）样品进行评估，并在药物相关浓度（2；10 或 30 mg/ml TPCS(2a)）下使用毛细管黏度计、冰点降低测量和原子力显微镜（AFM）进行评估。在存在 TPCS(2a) 的情况下，通过光散射法确定了 Pluronic 的临界胶束浓度（CMC）。Pluronic 嵌段共聚物在环境温度下通过形成药物载体复合物来增溶光敏剂，高于 CMC，这些复合物显然以不同黏度和形态的网络形式存在，对中性和带电赋形剂的添加敏感。
