Senapati Samir, Youssef Ahmed Adel Ali, Sweeney Corinne, Cai Chuntian, Dudhipala Narendar, Majumdar Soumyajit
Department of Pharmaceutics and Drug Delivery, School of Pharmacy, University of Mississippi, Oxford, MS 38677, USA.
Department of Pharmaceutical Technology, Faculty of Pharmacy, Kafrelsheikh University, Kafrelsheikh 33516, Egypt.
Pharmaceutics. 2022 Nov 24;14(12):2585. doi: 10.3390/pharmaceutics14122585.
Cannabidiol (CBD) is the major non-psychoactive and most widely studied of the cannabinoid constituents and has great therapeutic potential in a variety of diseases. However, contradictory reports in the literature with respect to CBD's effect on intraocular pressure (IOP) have raised concerns and halted research exploring its use in ocular therapeutics. Therefore, the current investigation aimed to further evaluate CBD's impact on the IOP in the rabbit model. CBD nanoemulsions, containing Carbopol 940 NF as a mucoadhesive agent (CBD-NEC), were prepared using hot-homogenization followed by probe sonication. The stability of the formulations post-moist-heat sterilization, in terms of physical and chemical characteristics, was studied for three different storage conditions. The effect of the formulation on the intraocular pressure (IOP) profile in normotensive Dutch Belted male rabbits was then examined. The lead CBD-NEC formulation (1% / CBD) exhibited a globule size of 259 ± 2.0 nm, 0.27 ± 0.01 PDI, and 23.2 ± 0.4 cP viscosity, and was physically and chemically stable for one month (last time point tested) at 4 °C, 25 °C, and 40 °C. CBD-NEC significantly lowered the IOP in the treated eyes for up to 360 min, with a peak drop in IOP of 4.5 mmHg observed at the 150 min time point, post-topical application. The IOP of the contralateral eye (untreated) was also observed to be lowered significantly, but the effect lasted up to the 180 min time point only. Overall, topically administered CBD, formulated in a mucoadhesive nanoemulsion formulation, reduced the IOP in the animal model studied. The results support further exploration of CBD as a therapeutic option for various inflammation-based ocular diseases.
大麻二酚（CBD）是大麻素成分中主要的非精神活性成分，也是研究最为广泛的成分，在多种疾病中具有巨大的治疗潜力。然而，文献中关于CBD对眼压（IOP）影响的相互矛盾的报道引发了关注，并停止了探索其在眼科治疗中应用的研究。因此，当前的研究旨在进一步评估CBD对兔模型眼压的影响。使用热均质化然后探针超声处理制备了含有卡波姆940 NF作为粘膜粘附剂的CBD纳米乳剂（CBD-NEC）。研究了三种不同储存条件下湿热灭菌后制剂在物理和化学特性方面的稳定性。然后检查了该制剂对正常血压的荷兰带雄兔眼压曲线的影响。主要的CBD-NEC制剂（1%/CBD）的球粒尺寸为259±2.0 nm，多分散指数（PDI）为0.27±0.01，粘度为23.2±0.4 cP，在4°C、25°C和40°C下在物理和化学上稳定一个月（测试的最后时间点）。局部应用后，CBD-NEC在长达360分钟的时间内显著降低了治疗眼的眼压，在150分钟时间点观察到眼压峰值下降4.5 mmHg。对侧未治疗眼的眼压也观察到显著降低，但这种效果仅持续到180分钟时间点。总体而言，以粘膜粘附纳米乳剂形式配制的局部应用CBD降低了所研究动物模型中的眼压。这些结果支持进一步探索CBD作为各种基于炎症的眼部疾病的治疗选择。
