Department of Pharmaceutical Technology, Faculty of Pharmacy, Ege University, Bornova, Izmir, Turkey.
Pharm Dev Technol. 2011 Nov-Dec;16(6):627-36. doi: 10.3109/10837450.2010.508074. Epub 2010 Aug 17.
This study described the thermosensitive formulations composed of poloxamer mixtures for use as drug delivery platform via mucosal route. It also characterized the poloxamer mixtures' rheological, mechanical and mucoadhesive properties. Poloxamer (Plx) 407 and Plx 188 were used alone and together for preparing the mucosal drug delivery platform. The mixtures of Plx 407 and Plx 188 in ratio of 15:15 (F5); 15:20 (F6); 20:10 (F7) existed liquid at room temperature, but gelled at physiological temperature. Flow rheometry studies and oscillatory analysis of each formulation were performed at 20 ± 0.1°C and 37 ± 0.1°C. F5 and F7 formulations exhibited typical gel-type mechanical spectra (G' > G″) after the determined frequency value at 37°C whereas F6 behaved as weakly cross-linked gel. Texture profile analysis presented that F5 and F7 showed similar mechanical properties and can be used as base for mucosal dosage form. Mucoadhesion studies indicated the difference among the formulations and the effect of the mucosal surface on mucoadhesive properties. Mucin disc, bovine vaginal and buccal mucosa were used as mucosal platform for mucoadhesion studies. It is suggested that these investigations may be usefully combined to provide a more rational basis for selecting the ratio of Plx to prepare a topical thermosensitive drug delivery system for mucosal administration.
本研究描述了由泊洛沙姆混合物组成的热敏制剂，用作通过粘膜途径的药物传递平台。它还表征了泊洛沙姆混合物的流变学、机械和粘膜粘附特性。泊洛沙姆（Plx）407 和 Plx 188 单独和一起用于制备粘膜药物传递平台。Plx 407 和 Plx 188 的混合物以 15:15（F5）; 15:20（F6）; 20:10（F7）的比例存在于室温下为液体，但在生理温度下凝胶化。在 20±0.1°C 和 37±0.1°C 下对每种制剂进行流动流变学研究和振荡分析。F5 和 F7 制剂在 37°C 下经过确定的频率值后表现出典型的凝胶型机械谱（G' > G″），而 F6 表现为弱交联凝胶。质地分析表明，F5 和 F7 具有相似的机械性能，可以用作粘膜剂型的基础。粘膜粘附研究表明了制剂之间的差异以及粘膜表面对粘膜粘附特性的影响。粘蛋白盘、牛阴道和颊粘膜被用作粘膜粘附研究的粘膜平台。研究表明，这些研究可以结合使用，为选择 Plx 的比例制备用于粘膜给药的局部热敏药物传递系统提供更合理的基础。
