Kheawfu Kantaporn, Chittasupho Chuda, Pikulkaew Surachai, Chaisri Wasana, Junmahasathien Taepin
Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, Thailand.
Faculty of Veterinary Medicine, Chiang Mai University, Chiang Mai 50100, Thailand.
Pharmaceutics. 2025 Jul 31;17(8):997. doi: 10.3390/pharmaceutics17080997.
Holy basil ( L.) essential oil exhibits antioxidant, antimicrobial, and anesthetic activities, mainly due to eugenol, methyl eugenol, and β-caryophyllene. However, its clinical application is limited by poor water solubility, instability, and low bioavailability. This study developed and compared two delivery systems, self-nanoemulsifying drug delivery systems (SNEDDS) and microemulsions (ME), to enhance their stability and fish anesthetic efficacy. The optimized SNEDDS (25% basil oil, 8.33% coconut oil, 54.76% Tween 80, 11.91% PEG 400) and ME (12% basil oil, 32% Tween 80, 4% sorbitol, 12% ethanol, 40% water) were characterized for droplet size, PDI, zeta potential, pH, and viscosity. Stability was evaluated by monitoring droplet size and PDI over time and by determining the retention of eugenol, methyl eugenol, and β-caryophyllene after storage at 45 °C. Fish anesthetic efficacy was tested in koi carp ( var. koi). SNEDDS maintained a small droplet size (~22.78 ± 1.99 nm) and low PDI (0.188 ± 0.088 at day 60), while ME showed significant size enlargement (up to 177.10 ± 47.50 nm) and high PDI (>0.5). After 90 days at 45 °C, SNEDDS retained 94.45% eugenol, 94.08% methyl eugenol, and 88.55% β-caryophyllene, while ME preserved 104.76%, 103.53%, and 94.47%, respectively. In vivo testing showed that SNEDDS achieved faster anesthesia (114.70 ± 24.80 s at 120 ppm) and shorter recovery (379.60 ± 15.61 s) than ME (134.90 ± 4.70 s; 473.80 ± 16.94 s). Ethanol failed to induce anesthesia at 40 ppm and performed poorly compared to SNEDDS and ME at other concentrations ( < 0.0001). SNEDDS demonstrated superior physical stability and fish anesthetic performance compared to ME. These findings support SNEDDS as a promising formulation for delivering holy basil essential oil in biomedical and aquaculture applications.
罗勒（Ocimum sanctum L.）精油具有抗氧化、抗菌和麻醉活性，主要归因于丁香酚、甲基丁香酚和β-石竹烯。然而，其临床应用受到水溶性差、稳定性低和生物利用度低的限制。本研究开发并比较了两种给药系统，即自纳米乳化药物递送系统（SNEDDS）和微乳剂（ME），以提高其稳定性和鱼类麻醉效果。对优化后的SNEDDS（25%罗勒油、8.33%椰子油、54.76%吐温80、11.91%聚乙二醇400）和ME（12%罗勒油、32%吐温80、4%山梨醇、12%乙醇、40%水）的粒径、多分散指数（PDI）、zeta电位、pH值和粘度进行了表征。通过随时间监测粒径和PDI以及测定在45℃储存后丁香酚、甲基丁香酚和β-石竹烯的保留率来评估稳定性。在锦鲤（Cyprinus carpio var. koi）中测试了鱼类麻醉效果。SNEDDS保持较小的粒径（约22.78±1.99nm）和较低的PDI（第60天时为0.188±0.088），而ME则显示出显著的粒径增大（高达177.10±47.50nm）和较高的PDI（>0.5）。在45℃下储存90天后，SNEDDS保留了94.45%的丁香酚、94.08%的甲基丁香酚和88.55%的β-石竹烯，而ME分别保留了104.76%、103.53%和94.47%。体内试验表明，SNEDDS比ME实现了更快的麻醉（120ppm时为114.70±24.80秒）和更短的恢复时间（379.60±15.61秒）（ME为134.90±4.70秒；473.80±16.94秒）。乙醇在40ppm时未能诱导麻醉，且在其他浓度下与SNEDDS和ME相比表现较差（P<0.0001）。与ME相比，SNEDDS表现出优异的物理稳定性和鱼类麻醉性能。这些发现支持SNEDDS作为一种有前途的制剂，可用于生物医学和水产养殖应用中递送罗勒精油。
