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载姜黄素和度洛西汀的固体自微乳化给药系统(SSNEDDS)的药代动力学和药效学评价及其在大鼠神经性疼痛缓解中的作用。

Pharmacokinetic and pharmacodynamic evaluation of Solid self-nanoemulsifying delivery system (SSNEDDS) loaded with curcumin and duloxetine in attenuation of neuropathic pain in rats.

机构信息

School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, 144411, India.

Department of Physiology and Pharmacology, Acharya and B.M. Reddy College of Pharmacy, Soladeuanahalli Hesargatta Road, Chikkabanawara Post, Bangalore, Karnataka, 560 090, India.

出版信息

Neurol Sci. 2021 May;42(5):1785-1797. doi: 10.1007/s10072-020-04628-7. Epub 2020 Sep 3.

Abstract

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.

摘要

本研究旨在通过固体自乳化药物传递系统(S-SNEDDS)提高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,并通过固体自乳化药物传递系统(S-SNEDDS)鉴定其对慢性缩窄性损伤(CCI)诱导的大鼠 NP 衰减的潜在作用。报告的优化批 S-SNEDDS 含有 CRM 和 DXH(各 30mg)、蓖麻油(20wt%)、吐温-80(40wt%)、Transcutol-P(40wt%)和西洛宾 244 FP(1g)。每个 naive CRM(NCH)、naive DXH(NDH)、DXH 和 CRM 的物理混合物(C-NCM-DXH)、S-SNEDDS-CRM(SCH)、S-SNEDDS-DXH(SDH)和 S-SNEDDS-CRM-DXH(C-SCH-SDH)的高剂量均进行了 MTT 测定。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 的口服生物利用度分别提高了 8 至 11.06 倍和 2 倍。此外,CCI 诱导的雄性 Wistar 大鼠从手术当天开始用含有 CRM 和 DXH 的 SSNEDDS、含有单一药物的 S-SNEDDS、单一 naive 形式及其组合治疗 14 天,并在预定的时间间隔评估行为。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 S-SNEDDS 提高了口服生物利用度,用含有两种药物的 S-SNEDDS 治疗的大鼠与接受其他任何治疗的大鼠相比,效果明显。因此,可以得出结论,两种药物的 S-SNEDDS 及其联合应用可以加速 NP 的预防。

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