PDF(Pubmed)
Abstract：
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 Sambucus ebulus L. (S. ebulus) 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.
摘要：
大麻二酚（CBD）是一种安全且非精神性的植物大麻素，具有广泛的潜在治疗性抗炎和抗氧化活性。由于它的亲脂性,它通常溶解在油相中。这项工作的主要目的是开发和表征具有潜在抗炎和抗氧化活性的微乳液的新制剂，用于局部治疗炎症性皮肤病。微乳液系统由20％的CBD油组成，作为疏水相；Labrasol/PlurolOleique（1：1），用作表面活性剂和助表面活性剂(S/CoS)，分别；和从接骨木中获得的水性植物提取物(S.ebulus)成熟的水果，具有潜在的抗氧化和抗炎活性，并作为水相。生成了伪三元相图，导致选择62%的最佳比例(S/CoS)，27%的CBD油和11%的水，在其再现性测试后，水相被植物亲水提取物代替。定义的系统以电导率为特征，液滴大小（通过激光散射），组分的相容性(通过差示扫描量热法)和流变性质(使用旋转流变仪)。设计的微乳液具有良好的稳定性和轻微的假塑性行为。通过使用流通式扩散池的体外扩散实验研究了CBD从油相中和咖啡酸从微乳液的水相中的释放特性，并将其与仅包含CBD作为活性物质的CBD油和微乳液的释放特性进行了比较。发现在微乳液中包含原始油不会导致CBD释放的显着改变，建议在制剂中包括亲水性活性化合物的可能性，并为开发未来的制剂建立一个有趣的策略。
