Gupta Bijay Kumar, Kumar Shobhit, Kaur Harleen, Ali Javed, Baboota Sanjula
1 Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard (Hamdard University) , New Delhi, India .
2 Department of Computer Science and Engineering, Faculty of Engineering and Technology, Jamia Hamdard (Hamdard University) , New Delhi, India .
Rejuvenation Res. 2018 Jun;21(3):232-248. doi: 10.1089/rej.2017.1959. Epub 2017 Oct 10.
Coenzyme Q (CoQ) is a well-known antioxidant molecule which is used in the treatment of neurodegenerative disorders, but due to poor solubility it suffers with the drawback of low oral bioavailability. The aim of present study was to prepare and characterize CoQ loaded nanoemulsion to improve the oral bioavailability. Prepared formulation was studied for droplet size, polydispersity index (PDI), percentage transmittance, refractive index, viscosity, zeta potential, surface morphology by transmission electron microscopy, and in vitro release study. Optimized formulation (A10) showed spherical droplets with mean diameter of 60.00 ± 15 nm, PDI of 0.121 ± 0.053, and zeta potential values of -24.40 ± 0.16 mV. Prepared nanoemulsion exhibited good transmittance (100.50% ± 0.86%), refractive index (1.41 ± 0.02), and viscosity (30.54 ± 2.86 cP). Various behavioral tests like forced swimming test, locomotor activity test, catalepsy, muscle coordination test, and akinesia test performed in haloperidol challenged rats and treated with CoQ nanoemulsion significantly improved the behavioral activities in comparison to CoQ suspension by reducing nigrostriatal dopamine depletion and thereby helping in the treatment of Parkinson's disease. Biochemical estimation data showed that CoQ nanoemulsion was helpful in elevating the decreased content of glutathione and reducing the increased content of thiobarbituric acid reactive substances. Improved CoQ release was obtained with nanoemulsions. Pharmacokinetic study results revealed that nanoemulsion exhibited 1.81 times enhancement in bioavailability in comparison to CoQ suspension.
辅酶Q（CoQ）是一种著名的抗氧化分子，用于治疗神经退行性疾病，但由于其溶解性差，存在口服生物利用度低的缺点。本研究的目的是制备并表征负载辅酶Q的纳米乳剂，以提高其口服生物利用度。对制备的制剂进行了粒径、多分散指数（PDI）、透光率、折射率、粘度、zeta电位、透射电子显微镜表面形态以及体外释放研究。优化后的制剂（A10）呈现出平均直径为60.00±15nm的球形液滴，PDI为0.121±0.053，zeta电位值为-24.40±0.16mV。制备的纳米乳剂具有良好的透光率（100.50%±0.86%）、折射率（1.41±0.02）和粘度（30.54±2.86cP）。在氟哌啶醇激发的大鼠中进行了各种行为测试，如强迫游泳试验、运动活性试验、僵住症、肌肉协调性试验和运动不能试验，并用辅酶Q纳米乳剂治疗，与辅酶Q混悬液相比，通过减少黑质纹状体多巴胺耗竭，显著改善了行为活动，从而有助于帕金森病的治疗。生化评估数据表明，辅酶Q纳米乳剂有助于提高谷胱甘肽降低的含量，并降低硫代巴比妥酸反应性物质增加的含量。纳米乳剂实现了辅酶Q释放的改善。药代动力学研究结果显示，与辅酶Q混悬液相比，纳米乳剂的生物利用度提高了1.81倍。
