当前位置: X-MOL 学术Neurol. Sci. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Pharmacokinetic and pharmacodynamic evaluation of Solid self-nanoemulsifying delivery system (SSNEDDS) loaded with curcumin and duloxetine in attenuation of neuropathic pain in rats.
Neurological Sciences ( IF 2.7 ) Pub Date : 2020-09-03 , DOI: 10.1007/s10072-020-04628-7
Bimlesh Kumar 1 , Sachin Kumar Singh 1 , T Prakash 2 , Amit Bhatia 3 , Monica Gulati 1 , Varun Garg 1 , Narendra Kumar Pandey 1 , Saurabh Singh 1 , Indu Melkani 1
Affiliation  

The present investigation is focused on improving oral bioavailability of poorly soluble and lipophilic drugs, curcumin (CRM) and duloxetine (DXH), through the solid self-nanoemulsifying drug delivery system (S-SNEDDS) and identifying their potential against attenuation of NP in chronic constriction injury (CCI)–induced rats through the solid self-nanoemulsifying drug delivery system (S-SNEDDS). The optimized batch of S-SNEDDS reported was containing CRM and DXH (30 mg each), castor oil (20% w/w), tween-80 (40% w/w), transcutol-P (40% w/w), and syloid 244 FP (1 g). The high dose of each of naïve CRM (NCH), naïve DXH (NDH), physical mixture of DXH and CRM (C-NCM-DXH), S-SNEDDS-CRM (SCH), S-SNEDDS-DXH (SDH), and S-SNEDDS-CRM-DXH (C-SCH-SDH) was subjected for MTT assay. The developed formulations were subjected to pharmacokinetic studies and results showed about 8 to 11.06 and 2-fold improvement in oral bioavailability of CRM and DXH through S-SNEDDS. Furthermore, CCI-induced male Wistar rats were treated with SSNEDDS containing CRM and DXH, S-SNEDDS containing individual drug, individual naïve forms, and their combination from the day of surgery for 14 days and evaluated for behavioral at pre-determined time intervals. On the terminal day, animals were sacrificed to assess tissue myeloperoxidase, superoxide anion, protein, tumor necrosis factor-α, total calcium levels, and histopathological changes. Pronounced effect was observed in rats treated with S-SNEDDS containing both drugs with respect to rats receiving any of other treatments owing to enhanced oral bioavailability through S-SNEDDS. Therefore, it can be concluded that S-SNEDDS of both drugs and their coadministration can accelerate the prevention of NP.



中文翻译:

装有姜黄素和度洛西汀的固体自纳米乳化递送系统(SSNEDDS)在减轻大鼠神经性疼痛中的药代动力学和药效学评价。

本研究的重点是通过固体自纳米乳化药物递送系统(S-SNEDDS)改善难溶性和亲脂性药物,姜黄素(CRM)和度洛西汀(DXH)的口服生物利用度,并确定其对慢性NP衰减的潜力收缩性损伤(CCI)诱导的大鼠通过固体自纳米乳化药物递送系统(S-SNEDDS)。报告的S-SNEDDS的优化批次包含CRM和DXH(各30 mg),蓖麻油(20%w / w),tween-80(40%w / w),transcutol-P(40%w / w)和糖浆244 FP(1克)。高剂量的天真CRM(NCH),天真DXH(NDH),DXH和CRM的物理混合物(C-NCM-DXH),S-SNEDDS-CRM(SCH),S-SNEDDS-DXH(SDH),对S-SNEDDS-CRM-DXH(C-SCH-SDH)进行MTT分析。所开发的制剂进行了药代动力学研究,结果表明,通过S-SNEDDS,CRM和DXH的口服生物利用度提高了约8至11.06,并且提高了2倍。此外,自手术当天起,将CCI诱导的雄性Wistar大鼠用含有CRM和DXH的SSNEDDS,含有个别药物,个别初次使用的形式及其组合的S-SNEDDS处理,手术时间为14天,并在预定的时间间隔内评估其行为。在最后一天,处死动物以评估组织髓过氧化物酶,超氧阴离子,蛋白质,肿瘤坏死因子-α,总钙水平和组织病理学变化。由于通过S-SNEDDS提高的口服生物利用度,在接受包含两种药物的S-SNEDDS治疗的大鼠中,相对于接受任何其他治疗的大鼠,观察到了显着的效果。因此,

更新日期:2020-09-03
down
wechat
bug