Research Scholar, Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi-110062, India.
Nanotechnology. 2016 Oct 28;27(43):435101. doi: 10.1088/0957-4484/27/43/435101. Epub 2016 Sep 22.
Selegiline is a monoamine oxidase B (MAO-B) inhibitor and is used in the treatment of Parkinson's disease. The main problem associated with its oral administration is its low oral bioavailability (10%) due to its poor aqueous solubility and extensive first pass metabolism. The aim of the present research work was to develop a nanoemulsion loaded with selegiline for direct nose-to-brain delivery for the better management of Parkinson's disease. A quality by design (QbD) approach was used in a statistical multivariate method for the preparation and optimization of nanoemulsion. In this study, four independent variables were chosen, in which two were compositions and two were process variables, while droplet size, transmittance, zeta potential and drug release were selected as response variables. The optimized formulation was assessed for efficacy in Parkinson's disease using behavioural studies, namely forced swimming, locomotor, catalepsy, muscle coordination, akinesia and bradykinesia or pole test in Wistar rats. The observed droplet size, polydispersity index (PDI), refractive index, transmittance, zeta potential and viscosity of selegiline nanoemulsion were found to be 61.43 ± 4.10 nm, 0.203 ± 0.005, 1.30 ± 0.01, 99.80 ± 0.04%, -34 mV and 31.85 ± 0.24 mPas respectively. Surface characterization studies demonstrated a spherical shape of nanoemulsion which showed 3.7 times enhancement in drug permeation as compared to drug suspension. The results of behaviour studies showed that treatment of haloperidol induced Parkinson's disease in rats with selegiline nanoemulsion (administered intranasally) showed significant improvement in behavioural activities in comparison to orally administered drug. These findings demonstrate that nanoemulsion could be a promising new drug delivery carrier for intranasal delivery of selegiline in the treatment of Parkinson's disease.
司来吉兰是一种单胺氧化酶 B（MAO-B）抑制剂，用于治疗帕金森病。其口服给药的主要问题是由于其较差的水溶性和广泛的首过代谢，导致其口服生物利用度低（10%）。本研究工作的目的是开发一种载有司来吉兰的纳米乳剂，用于直接通过鼻腔递送至大脑，以更好地治疗帕金森病。采用质量源于设计（QbD）方法，采用统计多元方法制备和优化纳米乳剂。在这项研究中，选择了四个独立变量，其中两个是组成，两个是工艺变量，而粒径、透光率、zeta 电位和药物释放被选为响应变量。使用行为研究，即强迫游泳、运动、僵住、肌肉协调、运动不能和运动缓慢或杆试验，评估帕金森病中优化配方的疗效，在 Wistar 大鼠中。观察到的司来吉兰纳米乳的粒径、多分散指数（PDI）、折射率、透光率、zeta 电位和粘度分别为 61.43±4.10nm、0.203±0.005、1.30±0.01、99.80±0.04%、-34mV 和 31.85±0.24mPas。表面特征研究表明纳米乳呈球形，与药物混悬液相比，药物渗透增强了 3.7 倍。行为研究的结果表明，用司来吉兰纳米乳（经鼻腔给药）治疗大鼠的氟哌啶醇诱导的帕金森病，与口服给药的药物相比，行为活动有显著改善。这些发现表明，纳米乳可能是一种有前途的新型药物传递载体，可用于经鼻腔递送至大脑的司来吉兰治疗帕金森病。
