Faculty of Pharmaceutical Science, Burapha University, Chonburi, Thailand.
Pharmaceutical Biopolymer Group (PBiG), Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, Thailand.
AAPS PharmSciTech. 2022 Mar 15;23(3):87. doi: 10.1208/s12249-022-02235-7.
Recently, monolaurin (ML) has received great interest due to its possible use as an alternative antifungal. However, the limited water solubility of ML is still a major obstacle to its formulation and application. Gel-like microemulsions are one of the promising carriers for low-water-solubility substances due to both the advantages of gels and microemulsions and may be applied for ML. In this study, ML was incorporated into gel-like microemulsions and evaluated for its physicochemical and antifungal properties. The results indicated that the properties of gel-like microemulsion changed after the incorporation of ML, suggesting that ML can induce the transition of internal structure. When simulating the oral cavity environment, changes in the microstructure were observed and depended on the times of dilution. The lamellar structure was formed at 1.5-2 times dilution. However, this structure was disrupted after dilution five times or more. The structural change following dilution was associated with the release profiles. After contacting the formulations with the medium, ML was promptly released, with the majority of ML being released within 2 h. Regarding the antifungal assay, the ML-loaded gel-like microemulsions decreased the survival of Candida albicans within 3 h, although ML was immediately released, suggesting that the ML-loaded in oil droplets required time to permeate through the fungal cell wall. Additionally, the gel-like microemulsions possessed acceptable stability after the temperature cycling test. Therefore, gel-like microemulsions can be a possible carrier for ML loading, and ML-loaded gel-like microemulsions may be applied as an alternative antifungal preparation in the future. Graphical abstract.
最近,由于可能被用作替代抗真菌药物,月桂酸单甘酯(ML)受到了极大的关注。然而,ML 的水溶性有限仍然是其制剂和应用的主要障碍。胶状微乳液由于凝胶和微乳液的优点,是低水溶性物质的有前途的载体之一,并且可能适用于 ML。在这项研究中,将 ML 掺入胶状微乳液中,并评估其物理化学和抗真菌性质。结果表明,掺入 ML 后胶状微乳液的性质发生了变化,表明 ML 可以诱导内部结构的转变。在模拟口腔环境时,观察到微结构的变化,并且取决于稀释次数。在 1.5-2 倍稀释时形成层状结构。然而,稀释五倍或更多次后,这种结构被破坏。稀释后的结构变化与释放曲线有关。与介质接触后,ML 立即释放,大部分 ML 在 2 小时内释放。关于抗真菌测定,载 ML 的胶状微乳液在 3 小时内降低了白色念珠菌的存活率,尽管 ML 立即释放,但这表明油滴中载 ML 需要时间渗透真菌细胞壁。此外,在温度循环测试后,胶状微乳液具有可接受的稳定性。因此,胶状微乳液可以是 ML 负载的一种可能载体,并且载 ML 的胶状微乳液将来可能被用作替代抗真菌制剂。