Pharmaceutical Research Laboratory, Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi, 110062, India.
Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi, 110062, India.
J Psychiatr Res. 2018 Apr;99:83-95. doi: 10.1016/j.jpsychires.2018.01.015. Epub 2018 Jan 31.
Duloxetine is a well-known antidepressant molecule which is used in the treatment of depression but due to poor solubility it suffers with the drawback of low oral bioavailability. The objective of present work was to formulate and characterize duloxetine loaded microemulsion to enhance the oral bioavailability. Prepared microemulsion was studied for droplet size, zeta potential, refractive index, polydispersity index (PDI), percentage transmittance, viscosity and in vitro release study. Optimized microemulsion (D1) showed spherical droplets with mean diameter of 35.40 ± 3.11 nm, PDI of 0.170 and zeta potential values of -25.8 mV. Formulation showed good transmittance (greater than 99%), viscosity (0.205 Pa s) and refractive index (1.43 ± 0.01). Increased duloxetine release was obtained with microemulsion in comparison to drug suspension. Behavioral tests like mobility test, tail suspension test and forced swimming test performed in depressed and treated rats with duloxetine microemulsion significantly improved the behavioral activities in comparison to duloxetine suspension. Pharmacokinetic studies showed that microemulsion exhibited 1.8 times increment in bioavailability in comparison to duloxetine suspension.
度洛西汀是一种众所周知的抗抑郁药分子，用于治疗抑郁症，但由于溶解度差，其口服生物利用度较低。本工作的目的是制备和表征度洛西汀微乳，以提高口服生物利用度。研究了制备的微乳的粒径、Zeta 电位、折射率、多分散指数（PDI）、透光率、粘度和体外释放研究。优化的微乳（D1）显示出平均直径为 35.40±3.11nm、PDI 为 0.170 和 Zeta 电位值为-25.8mV 的球形液滴。制剂表现出良好的透光率（大于 99%）、粘度（0.205Pa·s）和折射率（1.43±0.01）。与药物混悬剂相比，微乳能使度洛西汀释放增加。在给予度洛西汀微乳的抑郁和治疗大鼠中进行的行为测试，如移动性测试、悬尾测试和强迫游泳测试，与度洛西汀混悬剂相比，显著改善了行为活动。药代动力学研究表明，与度洛西汀混悬剂相比，微乳的生物利用度提高了 1.8 倍。
