Jani Parva, Vanza Jigar, Pandya Nilima, Tandel Hemal
Faculty of Pharmacy, The Maharaja Sayajirao University of Baroda, Kalabhavan Campus, Vadodara 390001, Gujarat, India.
Ther Deliv. 2019 Nov;10(11):683-696. doi: 10.4155/tde-2019-0060. Epub 2019 Nov 20.
The manuscript describes the performance of nanoparticles loaded with antidepressant drug for nose-to-brain drug delivery. Poly-lactic-co-glycolic acid-loaded nanoparticles of agomelatine were prepared by nanoprecipitation method using poloxamer 407 as stabilizer. The process parameters were optimized using factorial design. The drug-loaded nanoparticles having low particle size (<200 nm) with narrow size distribution and required zeta potential (-22.7 mV) to avoid aggregation showed sustained release profile and were found to have higher permeability as observed from studies when compared with plain drug suspension. Histopathology test showed that the optimized formulation was free from nasal toxicity on the goat nasal mucosa. Pharmacodynamic study showed significant reduction in immobility time in rats treated with the formulation which indicated antidepressant activity of the formulation. The prepared agomelatin-loaded poly-lactic-co-glycolic acid nanoparticles showed prominent antidepressant activity by nose-to-brain delivery as observed from various studies.
该手稿描述了负载抗抑郁药物的纳米颗粒用于鼻脑给药的性能。以泊洛沙姆407为稳定剂，通过纳米沉淀法制备了负载阿戈美拉汀的聚乳酸-羟基乙酸共聚物纳米颗粒。采用析因设计对工艺参数进行了优化。载药纳米颗粒粒径小（<200nm）、粒径分布窄且具有所需的zeta电位（-22.7mV）以避免聚集，显示出缓释特性，与普通药物悬浮液相比，研究表明其具有更高的渗透性。组织病理学测试表明，优化后的制剂对山羊鼻黏膜无鼻毒性。药效学研究表明，用该制剂治疗的大鼠的不动时间显著减少，这表明该制剂具有抗抑郁活性。从各项研究中可以看出，所制备的负载阿戈美拉汀的聚乳酸-羟基乙酸共聚物纳米颗粒通过鼻脑给药显示出显著的抗抑郁活性。
