Areses-Huete Teresa, Cordoba-Diaz Damian, Torres-Suárez Ana Isabel, Cordoba-Diaz Manuel
Department of Pharmaceutics and Food Technology, Faculty of Pharmacy, Complutense University of Madrid, E-28040 Madrid, Spain.
University Institute of Industrial Pharmacy (IUFI), Complutense University of Madrid, E-28040 Madrid, Spain.
Pharmaceutics. 2024 May 24;16(6):705. doi: 10.3390/pharmaceutics16060705.
Cannabidiol (CBD) is a safe and non-psychotropic phytocannabinoid with a wide range of potential therapeutic anti-inflamatory and antioxidant activities. Due to its lipophilicity, it is normally available dissolved in oily phases. The main aim of this work was to develop and characterize a new formulation of a microemulsion with potential anti-inflammatory and antioxidant activity for the topical treatment of inflammatory skin disorders. The microemulsion system was composed of a 20% CBD oil, which served as the hydrophobic phase; Labrasol/Plurol Oleique (1:1), which served as surfactant and cosurfactant (S/CoS), respectively; and an aqueous vegetal extract obtained from L. () ripe fruits, which has potential anti-oxidant and anti-inflammatory activity and which served as the aqueous phase. A pseudo-ternary phase diagram was generated, leading to the selection of an optimal proportion of 62% (S/CoS), 27% CBD oil and 11% water and, after its reproducibility was tested, the aqueous phases were replaced by the vegetal hydrophilic extract. The defined systems were characterized in terms of conductivity, droplet size (by laser scattering), compatibility of components (by differential scanning calorimetry) and rheological properties (using a rotational rheometer). The designed microemulsion showed good stability and slight pseudo-plastic behavior. The release properties of CBD from the oil phase and caffeic acid from the aqueous phase of the microemulsion were studied via in vitro diffusion experiments using flow-through diffusion cells and were compared to those of a CBD oil and a microemulsion containing only CBD as an active substance. It was found that the inclusion of the original oil in microemulsions did not result in a significant modification of the release of CBD, suggesting the possibility of including hydrophilic active compounds in the formulation and establishing an interesting strategy for the development of future formulations.
大麻二酚(CBD)是一种安全且无精神活性的植物大麻素,具有广泛的潜在治疗性抗炎和抗氧化活性。由于其亲脂性,它通常以溶解于油相的形式存在。这项工作的主要目的是开发并表征一种具有潜在抗炎和抗氧化活性的微乳新制剂,用于局部治疗炎症性皮肤病。微乳体系由20%的CBD油组成,其作为疏水相;Labrasol/聚甘油油酸酯(1:1),分别作为表面活性剂和助表面活性剂(S/CoS);以及从L.()成熟果实中获得的植物水提取物,其具有潜在的抗氧化和抗炎活性,并作为水相。绘制了伪三元相图,从而选择了62%(S/CoS)、27%的CBD油和11%的水的最佳比例,在测试其重现性后,水相被植物亲水性提取物取代。通过电导率、液滴大小(通过激光散射)、组分相容性(通过差示扫描量热法)和流变学性质(使用旋转流变仪)对确定的体系进行了表征。所设计的微乳显示出良好的稳定性和轻微的假塑性行为。通过使用流通扩散池的体外扩散实验研究了微乳中CBD从油相的释放特性以及水相中咖啡酸的释放特性,并将其与CBD油和仅含有CBD作为活性物质的微乳的释放特性进行了比较。结果发现,在微乳中加入原始油不会导致CBD释放的显著改变,这表明在制剂中加入亲水性活性化合物的可能性,并为未来制剂的开发建立了一种有趣的策略。