Amalraj Augustine, Jacob Joby, Varma Karthik, Gopi Sreeraj
R&D Centre, Aurea Biolabs Private Limited, Kolenchery, Cochin, 682 311 Kerala, India.
ACS Omega. 2020 Sep 8;5(37):24045-24056. doi: 10.1021/acsomega.0c03456. eCollection 2020 Sep 22.
Delayed onset muscle soreness (DOMS) is a complex spreading out, which is related to swelling of muscles, tenderness, rigidity, pain, disruption of muscle fiber, alteration in the kinematics of joint, acute tissue damage, and reduction in power and strength. β-Caryophyllene (BCP), a potent phytocannabinoid, could play an important role in managing DOMS because of its wide diversity of biological activities, particularly its anti-inflammatory activity; however, its poor stability in light, temperature, high volatility, and insolubility can restrict the medical practices. In this study, liposomal β-caryophyllene (Rephyll) was designed and established in powder form constructed by the nanofiber weaving technology to improve the bioavailability of BCP with improved stability. Rephyll was characterized by Fourier transform infrared spectroscopy, transmission electron microscopy, and differential scanning calorimetry studies. Encapsulation efficiency, loading capacity, and in vitro release studies revealed that Rephyll can be an auspicious drug delivery arrangement for BCP. The effects of Rephyll were evaluated by a randomized, double-blinded, crossover-designed, placebo-controlled study. The oral consumption of Rephyll significantly reduced the pain visual assessment score, revealing that Rephyll effectively reduced DOMS with improved recovery without any side effects due to the bioavailable form of the phytocannabinoid BCP in the liposomal powder formulation.
延迟性肌肉酸痛(DOMS)是一种复杂的症状,与肌肉肿胀、压痛、僵硬、疼痛、肌纤维断裂、关节运动学改变、急性组织损伤以及力量和体能下降有关。β-石竹烯(BCP)是一种有效的植物大麻素,由于其具有广泛的生物活性,特别是抗炎活性,可能在管理DOMS方面发挥重要作用;然而,其在光照、温度下稳定性差、挥发性高以及不溶性会限制其医学应用。在本研究中,设计并制备了脂质体β-石竹烯(Rephyll)粉末,采用纳米纤维编织技术构建,以提高BCP的生物利用度并改善其稳定性。通过傅里叶变换红外光谱、透射电子显微镜和差示扫描量热法研究对Rephyll进行了表征。包封率、载药量和体外释放研究表明,Rephyll可能是一种用于BCP的良好药物递送制剂。通过随机、双盲、交叉设计、安慰剂对照研究评估了Rephyll的效果。口服Rephyll显著降低了疼痛视觉评估评分,表明Rephyll有效减轻了DOMS,且由于脂质体粉末制剂中植物大麻素BCP的生物可利用形式,恢复情况得到改善,且无任何副作用。