Unidad de Investigación y Desarrollo en Tecnología Farmacéutica (UNITEFA), CONICET, Edificio Ciencias 2, Cuidad Universitaria, Córdoba, X5000HUA, Argentina.
Departamento de Ciencias Farmacéuticas, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Edificio Ciencias 2, Cuidad Universitaria, Córdoba, X5000HUA, Argentina.
Int J Cosmet Sci. 2020 Dec;42(6):548-556. doi: 10.1111/ics.12638. Epub 2020 Aug 29.
The aim of the present study was to evaluate the influence of the incorporation of caffeine as a model active ingredient on the quality attributes of a bioadhesive emulgel formulation previously optimized by Quality by Design (QbD) tools. Emulgels are emerging topical drug delivery systems for cosmetic or pharmaceutical uses, which combine the advantages of both emulsions and gels.
In this work, the observed and predicted values for spreadability, phase separation by centrifugation and detachment forces performed by texturometer were compared with those of the control and active-containing emulgel formulations. In addition, rheological properties, release of caffeine and comparative in vitro/ex vivo bioadhesion properties were evaluated using human skin.
The flow curves of emulgel formulations showed the typical pseudoplastic and no thixotropic flow with yield stress. The incorporation of active ingredient did not produce significant changes. All emulgels were uniformly spread and no significant differences in spreadability values between control and caffeine containing formulations and neither respect to those predicted values from experimental design optimization were found. Emulgel formulations showed appropriate detachment forces values and no significant differences between caffeine loading and control emulgel formulations were observed.
Caffeine was successfully vehiculized in this optimized bioadhesive emulgel formulation, which showed high robustness regarding the process variability. There were no significant changes in the critical quality attributes after the incorporation of the active ingredient and a promising stability was observed for at least one year. Results suggested that the optimized emulgel is an interesting topical biodhesive delivery system for cosmetic applications, including agents for skin conditioning, not present in gels formulations.
本研究旨在评估将咖啡因作为模型活性成分掺入对先前通过质量源于设计（QbD）工具优化的生物粘附型乳凝胶制剂的质量属性的影响。乳凝胶是一种新兴的局部药物传递系统，用于化妆品或药物用途，结合了乳液和凝胶的优点。
在这项工作中，比较了可铺展性、离心相分离和质构仪测定的剥离力的观察值和预测值与对照和含活性成分的乳凝胶制剂的这些值。此外，还使用人体皮肤评估了流变性能、咖啡因释放以及体外/体内比较生物粘附性能。
乳凝胶制剂的流动曲线表现出典型的假塑性和无触变性流动，并具有屈服应力。加入活性成分不会产生显著变化。所有乳凝胶制剂均均匀铺展，在可铺展性值方面，对照和含咖啡因制剂之间没有显著差异，也与实验设计优化的预测值没有显著差异。乳凝胶制剂显示出适当的剥离力值，并且在咖啡因负载和对照乳凝胶制剂之间没有观察到显著差异。
成功地将咖啡因包封在这种优化的生物粘附型乳凝胶制剂中，该制剂对工艺变异性具有高稳健性。在加入活性成分后，关键质量属性没有发生显著变化，并且至少在一年内观察到良好的稳定性。结果表明，优化的乳凝胶是一种用于化妆品应用的有前途的局部生物粘附性传递系统，包括用于皮肤调理的制剂，这些制剂在凝胶制剂中不存在。
