Waqar Muhammad Ahsan, Zaman Muhammad, Hameed Huma, Jamshaid Muhammad, Irfan Ali, Shazly Gamal A, Paiva-Santos Ana Cláudia, Bin Jardan Yousef A
Faculty of Pharmaceutical Sciences, University of Central Punjab, Lahore 54000, Pakistan.
Department of Chemistry, Government College University Faisalabad, Faisalabad 38000, Pakistan.
ACS Omega. 2023 Oct 3;8(41):38191-38203. doi: 10.1021/acsomega.3c04444. eCollection 2023 Oct 17.
St. John's wort in western Europe has been extensively utilized for the treatment of mild to moderate depression. Hypericin, a red pigment, is found to be responsible for its antidepressant activity. The aim of the current study was to prepare a nanoemulsion (O/W) of hypericin designed for immediate delivery of the drug to the brain for the treatment of depression. The nanoemulsion was prepared by means of a homogenization technique, and that was followed by its physicochemical evaluation. Tween-80, Span-80, β-cyclodextrin, ethanol, and eucalyptus oil were utilized for the manufacturing of the nanoemulsion. Morphological studies have revealed globular structures of nanosize that were confirmed by the zeta analysis. The consistency of particles was revealed by the low polydispersity values. pH values of all formulations lay within the range of nasal pH. The viscosity of the prepared formulations was affected by the increase in concentrations of β-cyclodextrin. After passing from the centrifugation and freeze-thaw studies, the prepared formulations showed good stability. Formulation F2 having a composition of oil phase (0.125 mL), aqueous phase (1.25 mL), and β-cyclodextrin (8%) showed the best results out of all the formulations, and F2 had a pH of 5.7, 5.35 cP viscosity, 1.332 refractive index, 148.8 globule size, and -10.8 zeta potential. The mean percentage drug release and and percentage drug permeations were observed to be 71.75, 76, and 75.07%, respectively. Meanwhile, formulation F2 showed the maximum drug release and permeation. behavior studies including the open field test, elevated plus maze test, and tail suspension test were conducted to see the antidepressant effect of hypericin along with comparison with a commercially available treatment. In conclusion, the prepared formulation shows good efficacy as an antidepressant and can be considered as a natural alternative over synthetic drugs.
在西欧，圣约翰草已被广泛用于治疗轻至中度抑郁症。人们发现，红色色素金丝桃素具有抗抑郁活性。本研究的目的是制备一种金丝桃素纳米乳剂（水包油型），旨在将药物立即递送至大脑以治疗抑郁症。该纳米乳剂采用均质技术制备，随后进行了理化性质评估。吐温80、司盘80、β-环糊精、乙醇和桉叶油被用于制备纳米乳剂。形态学研究揭示了纳米尺寸的球状结构，这一点通过zeta分析得到了证实。低多分散性值表明颗粒具有一致性。所有制剂的pH值均在鼻腔pH值范围内。所制备制剂的粘度受β-环糊精浓度增加的影响。经过离心和冻融研究后，所制备的制剂显示出良好的稳定性。在所有制剂中，油相组成为0.125 mL、水相组成为1.25 mL且β-环糊精含量为8%的制剂F2表现出最佳效果，F2的pH值为5.7，粘度为5.35 cP，折射率为1.332，球粒尺寸为148.8，zeta电位为 -10.8。观察到药物释放的平均百分比以及药物渗透百分比分别为71.75%、76%和75.07%。同时，制剂F2显示出最大的药物释放和渗透。进行了包括旷场试验、高架十字迷宫试验和悬尾试验在内的行为学研究，以观察金丝桃素的抗抑郁作用，并与市售治疗药物进行比较。总之，所制备的制剂作为抗抑郁药显示出良好的疗效，可被视为合成药物的天然替代品。
