a Faculty of Pharmacy , DIT University , Dehradun , India.
Drug Dev Ind Pharm. 2019 Aug;45(8):1351-1360. doi: 10.1080/03639045.2019.1619760. Epub 2019 May 28.
Depression is one of the most frequent psychiatric and potentially life-threatening disorders. This research work can offer a potential for delivery of selegiline moiety via ocular route in bio-nanosuspension mode for the effective management of depression after preclinical performance screening. The selegiline-loaded bio-nanosuspension was prepared using novel bio-retardant isolated from fruit pulp of (Sapodilla) by sonication solvent evaporation method with different ratios (0.05%, 0.1%, 0.2%, 0.3%, 0.4%, 0.5%, and 1%) and with standard polymer HPMC (0.1%, 0.2%, 0.3%, 0.4%, and 0.5%). The prepared formulations were evaluated for pH stability studies, %entrapment efficiency, drug release, particle size, polydispersity index (PDI), zeta potential, and stability studies. The prepared bio-nanosuspension was subjected to the best formulation based on comparison of above-mentioned evaluation parameters, so Fb2 (0.1%) formulation was found to be the best formulation showing an value of 0.9814, T50% of 29.7 h, and T80% of 65.25 h. According to the release kinetics, the best fit model was found to be the Korsmeyer-Peppas with the Fickian diffusion (Higuchi matrix) as the mechanism of drug release. (Sapodilla) provided excellent stability for the formulation and resulting particle size for the best formulation was found to be 252 nm. The bio-nanosuspension had PDI of 0.35 with zeta potential of -8.91 mV. The prepared bio-nanosuspension was found to be safe and compatible with the ophthalmic delivery for treatment of depression.
抑郁症是最常见的精神疾病之一，也是潜在的危及生命的疾病之一。这项研究工作为通过眼部生物纳米混悬液途径传递司来吉兰提供了一种可能性，可用于在临床前性能筛选后有效管理抑郁症。采用超声溶剂蒸发法，从（人心果）果肉中分离出新型生物缓控释剂，制备载有司来吉兰的生物纳米混悬剂，并用不同比例（0.05%、0.1%、0.2%、0.3%、0.4%、0.5%和 1%）和标准聚合物 HPMC（0.1%、0.2%、0.3%、0.4%和 0.5%）。对所制备的制剂进行 pH 稳定性研究、%包封效率、药物释放、粒径、多分散指数（PDI）、Zeta 电位和稳定性研究。根据上述评价参数的比较，对所制备的生物纳米混悬剂进行最佳制剂筛选，结果表明 Fb2（0.1%）制剂为最佳制剂，其 值为 0.9814，T50%为 29.7 小时，T80%为 65.25 小时。根据释放动力学，发现最佳拟合模型为 Korsmeyer-Peppas 模型，药物释放机制为菲克扩散（Higuchi 基质）。（人心果）为制剂提供了优异的稳定性，最佳制剂的粒径为 252nm。生物纳米混悬剂的 PDI 为 0.35，Zeta 电位为-8.91mV。所制备的生物纳米混悬剂被发现是安全的，与治疗抑郁症的眼部给药兼容。
