Department of Pharmaceutics and Pharmaceutical Technology, Ramanbhai Patel College of Pharmacy, Charotar University of Science and Technology, Changa, Gujarat, India.
Int J Nanomedicine. 2018 Mar 15;13(T-NANO 2014 Abstracts):35-38. doi: 10.2147/IJN.S124703. eCollection 2018.
Agomelatine (AGM) is a new antidepressant drug with a novel mechanism of action and fewer side effects compared with older antidepressants. AGM is a melatonin receptor (MT1 and MT2) agonist and 5-hydroxytryptamine receptor (5-HT) antagonist. In the present study, the enhancement of the oral bioavailability of AGM was formulated and loaded into nanostructured lipid carriers (NLCs), using ultrasonication method. In vitro and ex vivo drug release was performed using a dialysis bag and rat duodenum, respectively. Our pharmacodynamic study showed that AGM-NLCs are more efficacious than a pure drug and marketed product, and confocal microscopy revealed lymphatic uptake of AGM-NLCs. The present study concluded that the NLCs enhanced the oral bioavailability of AGM (6.5-fold) by avoiding its first-pass metabolism by way of lymphatic uptake.
阿戈美拉汀（AGM）是一种新型抗抑郁药，与旧的抗抑郁药相比，具有作用机制新颖、副作用少的特点。AGM 是褪黑素受体（MT1 和 MT2）激动剂和 5-羟色胺受体（5-HT）拮抗剂。在本研究中，采用超声法将 AGM 的口服生物利用度进行制剂化并负载到纳米结构脂质载体（NLC）中。体外和离体药物释放分别使用透析袋和大鼠十二指肠进行。我们的药效学研究表明，AGM-NLC 比纯药物和市售产品更有效，共聚焦显微镜显示 AGM-NLC 被淋巴管摄取。本研究得出结论，NLC 通过淋巴管摄取避免了 AGM 的首过代谢，从而提高了 AGM 的口服生物利用度（6.5 倍）。
